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List of works by Nathanael Gray

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

scientific article published on 7 November 2017

A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification

scientific article published on 20 December 2018

A Discovery Strategy for Selective Inhibitors of c-Src in Complex with the Focal Adhesion Kinase SH3/SH2-binding Region

scientific article published on 28 November 2014

A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing

scientific article published on 21 September 2018

A Next Generation Connectivity Map: L1000 Platform and the First 1,000,000 Profiles.

scientific article published in November 2017

A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate

scientific article

A Quantitative Tissue-Specific Landscape of Protein Redox Regulation during Aging

scientific article published on 27 February 2020

A Simple Method to Identify Kinases That Regulate Embryonic Stem Cell Pluripotency by High-throughput Inhibitor Screening

scientific article

A UV-Independent Topical Small-Molecule Approach for Melanin Production in Human Skin

scientific article published on June 2017

A benzo[b]thiophene-based selective type 4 S1P receptor agonist

scientific article published on 18 November 2016

A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas.

scientific article published on 12 January 2017

A broad-spectrum antiviral molecule, QL47, selectively inhibits eukaryotic translation

scientific article published on 30 December 2019

A ceramide-1-phosphate analogue, PCERA-1, simultaneously suppresses tumour necrosis factor-alpha and induces interleukin-10 production in activated macrophages

scientific article

A combinatorial scaffold approach toward kinase-directed heterocycle libraries

scientific article

A general strategy for creating "inactive-conformation" abl inhibitors

scientific article

A genome-wide overexpression screen in yeast for small-molecule target identification

scientific article

A kinase-independent role for CDK8 in BCR-ABL1+ leukemia

scientific article published on 18 October 2019

A landscape of pharmacogenomic interactions in cancer.

scientific article published on 05 July 2016

A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model

scientific article published in November 2006

A multitargeted probe-based strategy to identify signaling vulnerabilities in cancers.

scientific article

A mutation in MYD88 (L265P) supports the survival of lymphoplasmacytic cells by activation of Bruton tyrosine kinase in Waldenström macroglobulinemia.

scientific article published on 8 July 2013

A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation

scientific article published on 05 November 2018

A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors

scientific article

A public-private partnership to unlock the untargeted kinome

scientific article published in January 2013

A small molecule with osteogenesis-inducing activity in multipotent mesenchymal progenitor cells

scientific article

A small-molecule inducer of the antioxidant response element

scientific article published on May 2010

A structure-guided approach to creating covalent FGFR inhibitors

scientific article

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl

scientific article

A unifying model for mTORC1-mediated regulation of mRNA translation.

scientific article

A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.

scientific article published on 7 September 2014

A-770041 reverses paclitaxel and doxorubicin resistance in osteosarcoma cells.

scientific article

Abemaciclib is a potent inhibitor of DYRK1A and HIP kinases involved in transcriptional regulation

scientific article published on 16 November 2021

Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency

scientific article

Acquired resistance to dasatinib in lung cancer cell lines conferred by DDR2 gatekeeper mutation and NF1 loss

scientific article published on 02 December 2013

Activating mutations in ALK provide a therapeutic target in neuroblastoma

scientific article

Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors.

scientific article

Activation of tyrosine kinases by mutation of the gatekeeper threonine

scientific article

Acute pharmacological degradation of Helios destabilizes regulatory T cells

scientific article published on 25 May 2021

Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations

scientific article published in February 2018

Allosteric Activators of Protein Phosphatase 2A Display Broad Antitumor Activity Mediated by Dephosphorylation of MYBL2

scientific article published on 14 April 2020

Allosteric inhibitors of Bcr-abl-dependent cell proliferation

scientific article published on 15 January 2006

Allosteric interactions between the myristate- and ATP-site of the Abl kinase

scientific article

An Embryonic Diapause-like Adaptation with Suppressed Myc Activity Enables Tumor Treatment Persistence

scientific article published on 05 January 2021

An amino-indazole scaffold with spectrum selective kinase inhibition of FLT3, PDGFRα and kit ⬇️

scientific article published on June 6, 2012

An efficient rapid system for profiling the cellular activities of molecular libraries.

scientific article published on 21 February 2006

Anti-SARS-CoV-2 activity of targeted kinase inhibitors: Repurposing clinically available drugs for COVID-19 therapy

scientific article published in January 2023

Antimitotic agents of natural origin

scientific article

BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner

scientific article

BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models

scientific article published on 01 May 2019

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment.

scientific article published on 23 June 2017

BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer

scientific article published on 16 July 2018

BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells

scientific article published on 07 August 2019

BTKCys481Ser drives ibrutinib resistance via ERK1/2 and protects BTKwild-type MYD88-mutated cells by a paracrine mechanism.

scientific article

Benzopyrimidodiazepinone inhibitors of TNK2

scientific article published on 07 January 2020

Brain Penetrant LRRK2 Inhibitor

scientific article

Broad spectrum alkynyl inhibitors of T315I Bcr-Abl

scientific article published on 19 May 2010

Bruton tyrosine kinase degradation as a therapeutic strategy for cancer

scientific article published on 13 December 2018

CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation

article

CDK13 cooperates with CDK12 to control global RNA polymerase II processivity

scientific article published on 29 April 2020

CDK4/6 Inhibition Augments Anti-Tumor Immunity by Enhancing T Cell Activation.

scientific article published on 3 November 2017

CDK7 Inhibition Potentiates Genome Instability Triggering Anti-tumor Immunity in Small Cell Lung Cancer

scientific article published on 26 December 2019

CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer.

scientific article

CDK7-dependent transcriptional addiction in triple-negative breast cancer.

scientific article

Catalytic Domain Plasticity of MKK7 Reveals Structural Mechanisms of Allosteric Activation and Diverse Targeting Opportunities

scientific article published on 04 August 2020

Cell-based optimization of novel benzamides as potential antimalarial leads

scientific article published on 29 October 2009

Characterization of DDR2 Inhibitors for the Treatment of DDR2 Mutated Nonsmall Cell Lung Cancer

scientific article

Characterization of TAE684 as a potent LRRK2 kinase inhibitor

scientific article

Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.

scientific article published on 22 February 2013

Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases

scientific article published on January 2014

Characterization of a highly selective inhibitor of the Aurora kinases.

scientific article published on 10 August 2017

Characterization of a selective inhibitor of the Parkinson's disease kinase LRRK2.

scientific article published on 6 March 2011

Chemical Biology Toolkit for DCLK1 Reveals Connection to RNA Processing

scientific article published on 04 August 2020

Chemical interrogation of the malaria kinome

scientific article

Chemical proteomics identifies unanticipated targets of clinical kinase inhibitors

scientific article published in October 2007

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).

scientific article published on 16 April 2018

Cheminformatics Tools for Analyzing and Designing Optimized Small-Molecule Collections and Libraries

scientific article published on 04 April 2019

Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase

scientific article published on 18 July 2008

Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR-Mutant Lung Cancer

scientific article published on 2 June 2015

Conformational disturbance in Abl kinase upon mutation and deregulation

scientific article

Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4)

scientific article published on 24 January 2019

Correction to "Synthesis and Structure-Activity Relationships of DCLK1 Kinase Inhibitors Based on a 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one Scaffold"

scientific article published on 13 August 2020

Correction to Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein

scientific article published on 01 November 2019

Correction to Discovery of a Potent and SelectiveDDR1 Receptor Tyrosine Kinase Inhibitor.

scientific article

Correction: An ATP-competitive mammalian target of rapamycin inhibitor reveals rapamycin-resistant functions of mTORC1

scientific article published on 28 February 2020

Correction: Evaluation of ERK as a therapeutic target in acute myelogenous leukemia

scientific article published on 06 March 2020

Correction: MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.

scientific article

Corrigendum: A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.

scientific article

Corrigendum: SIKs control osteocyte responses to parathyroid hormone

scientific article published on 22 February 2017

Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors

scientific article published on 20 February 2017

Covalent Guanosine Mimetic Inhibitors of G12C KRAS.

scientific article

Covalent Targeting of Fibroblast Growth Factor Receptor Inhibits Metastatic Breast Cancer.

scientific article published on July 2016

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors

scientific article published on 29 August 2016

Crystal structure of human IRAK1.

scientific article published on 5 December 2017

Crystal structure of pyridoxal kinase in complex with roscovitine and derivatives

scientific article published on 28 June 2005

Current Therapies Under Investigation for COVID-19

scientific article published on 08 July 2020

DEPTOR is an mTOR inhibitor frequently overexpressed in multiple myeloma cells and required for their survival

scientific article

DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors

scientific article

Defining and Targeting Adaptations to Oncogenic KRASG12C Inhibition Using Quantitative Temporal Proteomics

scientific article published on 01 March 2020

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 1.

scientific article published on 3 February 2006

Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2

scientific article published on 09 March 2006

Development and Characterization of a Wee1 Kinase Degrader

scientific article published on 14 November 2019

Development of ATP-competitive mTOR inhibitors

scientific article published on January 2012

Development of Chemical Probes for Investigation of Salt-Inducible Kinase Function in Vivo

scientific article published on 25 May 2016

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6

scientific article published on 29 March 2019

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8

scientific article published on 18 March 2018

Development of Selective Covalent Janus Kinase 3 Inhibitors.

scientific article published on 10 August 2015

Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype

scientific article published on 21 March 2019

Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors

scientific article

Development of small molecules targeting the pseudokinase Her3.

scientific article published on 11 May 2015

Development of ‘DFG-out’ inhibitors of gatekeeper mutant kinases ⬇️

scientific article published on June 23, 2012

Discoidin domain receptor 2 mediates collagen-induced activation of membrane-type 1 matrix metalloproteinase in human fibroblasts.

scientific article

Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors

scientific article published on 22 October 2019

Discovery and Structure-Activity Relationship Study of (Z)-5-Methylenethiazolidin-4-one Derivatives as Potent and Selective Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors

scientific article published on 16 April 2020

Discovery and characterization of novel mutant FLT3 kinase inhibitors

scientific article published on 31 August 2010

Discovery and optimization of potent and selective benzonaphthyridinone analogs as small molecule mTOR inhibitors with improved mouse microsome stability.

scientific article published on 7 May 2011

Discovery and resistance mechanism of a selective CDK12 degrader

scientific article published on 22 March 2021

Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors

scientific article

Discovery of 1-(4-(4-propionylpiperazin-1-yl)-3-(trifluoromethyl)phenyl)-9-(quinolin-3-yl)benzo[h][1,6]naphthyridin-2(1H)-one as a highly potent, selective mammalian target of rapamycin (mTOR) inhibitor for the treatment of cancer

scientific article

Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors ⬇️

scientific article published on March 15, 2011

Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.

scientific article published on 15 February 2011

Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator

scientific article

Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity

scientific article published on 28 March 2019

Discovery of Covalent MKK4/7 Dual Inhibitor

scientific article published on 07 September 2020

Discovery of EGFR selective 4,6-disubstituted pyrimidines from a combinatorial kinase-directed heterocycle library

scientific article

Discovery of Immunologically Inspired Small Molecules That Target the Viral Envelope Protein

scientific article published on 29 August 2018

Discovery of Inhibitors That Overcome the G1202R Anaplastic Lymphoma Kinase Resistance Mutation

scientific article

Discovery of MFH290: A Potent and Highly Selective Covalent Inhibitor for Cyclin-Dependent Kinase 12/13

scientific article published on 05 June 2020

Discovery of Potent and Selective Covalent Inhibitors of JNK

scientific article published on 27 January 2012

Discovery of Type II Inhibitors of TGFβ-Activated Kinase 1 (TAK1) and Mitogen-Activated Protein Kinase Kinase Kinase Kinase 2 (MAP4K2)

scientific article

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor

scholarly article by Jaebong Jang et al published 3 September 2018 in Angewandte Chemie International Edition

Discovery of a Highly Potent and Selective Indenoindolone Type 1 Pan-FLT3 Inhibitor

scientific article published on 8 March 2016

Discovery of a Highly Selective STK16 Kinase Inhibitor

scientific article

Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor

scientific article

Discovery of a Pyrrolopyrimidine (JH-II-127), a Highly Potent, Selective, and Brain Penetrant LRRK2 Inhibitor

scientific article published on 7 April 2015

Discovery of a Selective, Covalent IRAK1 Inhibitor with Antiproliferative Activity in MYD88 Mutated B-Cell Lymphoma

scientific article published on 09 October 2020

Discovery of a Series of 5,11-Dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-ones as Selective PI3K-δ/γ Inhibitors

scientific article published on 2 August 2016

Discovery of a Series of Benzopyrimidodiazepinone TNK2 Inhibitors via Scaffold Morphing

scientific article published on 30 July 2020

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.

scientific article published on 12 January 2011

Discovery of a potent dual ALK and EGFR T790M inhibitor

scientific article

Discovery of a potent, covalent BTK inhibitor for B-cell lymphoma

scientific article published on 17 March 2014

Discovery of a selective inhibitor of doublecortin like kinase 1

scientific article published on 06 April 2020

Discovery of a selective irreversible BMX inhibitor for prostate cancer.

scientific article published on 26 April 2013

Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

scientific article

Discovery of allosteric BCR-ABL inhibitors from phenotypic screen to clinical candidate

scientific article

Discovery of an AKT Degrader with Prolonged Inhibition of Downstream Signaling

scientific article published on 16 December 2019

Discovery of host-targeted covalent inhibitors of dengue virus

scientific article (publication date: March 2017)

Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials

scientific article published on 2 June 2010

Discovery of pyrimidine benzimidazoles as Lck inhibitors: part I.

scientific article

Discovery of pyrimidine benzimidazoles as Src-family selective Lck inhibitors. Part II.

scientific article published on 12 October 2009

Discovery of selective aminothiazole aurora kinase inhibitors

scientific article

Discovery of selective irreversible inhibitors for EGFR-T790M.

scientific article

Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold

scientific article published on 13 September 2019

Dual inhibition of Fes and Flt3 tyrosine kinases potently inhibits Flt3-ITD+ AML cell growth

scientific article

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors

scientific article published on 6 May 2015

EML4-ALK fusion gene and efficacy of an ALK kinase inhibitor in lung cancer

scientific article

EPHA2 Blockade Overcomes Acquired Resistance to EGFR Kinase Inhibitors in Lung Cancer

scientific article published on 7 January 2016

EPHA2 is a mediator of vemurafenib resistance and a novel therapeutic target in melanoma

scientific article

ER stress signaling promotes the survival of cancer 'persister cells' tolerant to EGFR tyrosine kinase inhibitors

scientific article published on 19 December 2017

ERK5 is activated by oncogenic BRAF and promotes melanoma growth

scientific article published on 27 February 2018

EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma

scientific article published on 18 January 2018

Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs

scientific article published on 12 August 2013

Enhancer profiling identifies critical cancer genes and characterizes cell identity in adult T-cell leukemia

scientific article published on 4 October 2017

Erk5 Is a Key Regulator of Naive-Primed Transition and Embryonic Stem Cell Identity

scientific article

Erratum: Corrigendum: The promise and peril of chemical probes

scientific article published in November 2015

Evaluation of ERK as a therapeutic target in acute myelogenous leukemia

scientific article published on 27 August 2019

Expanding the Diversity of Allosteric Bcr-Abl Inhibitors ⬇️

scientific article published on October 14, 2010

Exploration of type II binding mode: A privileged approach for kinase inhibitor focused drug discovery?

scientific article

Exploring Targeted Degradation Strategy for Oncogenic KRASG12C

scientific article published on 26 December 2019

Extracellular signal-regulated kinase 5 promotes acute cellular and systemic inflammation

scientific article published on 25 August 2015

Extracellular-regulated protein kinase 5-mediated control of p21 expression promotes macrophage proliferation associated with tumor growth and metastasis

scientific article published on 19 June 2020

FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML.

scientific article published on 20 May 2009

Factors underlying sensitivity of cancers to small-molecule kinase inhibitors

scientific article

Fibroblast growth factor receptor 1-transformed mammary epithelial cells are dependent on RSK activity for growth and survival

scientific article

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia

scientific article published on 11 September 2018

Fluorescent visualization of Src by using dasatinib-BODIPY

scientific article published on 14 May 2014

Functional Characterization of an Isoform-Selective Inhibitor of PI3K-p110β as a Potential Anticancer Agent ⬇️

scientific article published on April 12, 2012

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins

scientific article published on 01 January 2021

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

scientific article published on 5 March 2018

GNF-2 Inhibits Dengue Virus by Targeting Abl Kinases and the Viral E Protein

scientific article

GSK2578215A; a potent and highly selective 2-arylmethyloxy-5-substitutent-N-arylbenzamide LRRK2 kinase inhibitor

scientific article

Gemcitabine and Chk1 Inhibitor AZD7762 Synergistically Suppress the Growth of Lkb1-Deficient Lung Adenocarcinoma

scientific article published on 28 July 2017

Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility

scientific article

Genetic and pharmacologic inhibition of EPHA2 promotes apoptosis in NSCLC.

scientific article published on 8 April 2014

Genomic alterations of anaplastic lymphoma kinase may sensitize tumors to anaplastic lymphoma kinase inhibitors

scientific article

Genomic and pathological heterogeneity in clinically diagnosed small cell lung cancer in never/light smokers identifies therapeutically targetable alterations

scientific article published on 19 March 2020

Golgicide A reveals essential roles for GBF1 in Golgi assembly and function

scientific article

HCK is a survival determinant transactivated by mutated MYD88, and a direct target of ibrutinib.

scientific article published on 3 May 2016

High MITF Expression is Associated with Super-enhancers and Suppressed by CDK7 Inhibition in Melanoma.

scientific article

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors

scientific article

Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML

scientific article published on 27 December 2018

How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion

scientific article published on 12 July 2018

Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells

scientific article published on 5 September 2015

Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation

scientific article published on 10 September 2016

Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis

scientific article

Identification and characterization of small-molecule inducers of epidermal keratinocyte differentiation.

scientific article

Identification of Existing Drugs That Effectively Target NTRK1 and ROS1 Rearrangements in Lung Cancer

scientific article

Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.

scholarly article

Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase

scientific article published on 5 June 2015

Identification of Wee1 as a novel therapeutic target for mutant RAS-driven acute leukemia and other malignancies

scientific article

Identification of a novel protein regulating microtubule stability through a chemical approach

scientific article published in January 2004

Identification of a potent and selective covalent Pin1 inhibitor

scientific article published on 01 June 2020

Identification of compounds with anti-human cytomegalovirus activity that inhibit production of IE2 proteins

scientific article published on 09 December 2016

Identification of coumarin derivatives as a novel class of allosteric MEK1 inhibitors

scientific article

Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling

scholarly article

Identification of homeodomain proteins, PBX1 and PREP1, involved in the transcription of murine leukemia virus

scientific article

Identification of human kinases involved in hepatitis C virus replication by small interference RNA library screening.

scientific article

Identification of novel therapeutic targets in acute leukemias with NRAS mutations using a pharmacologic approach

scientific article published on April 2015

Identification of small molecule inhibitors targeting the Zika virus envelope protein

scientific article published on 13 February 2019

In Situ Kinase Profiling Reveals Functionally Relevant Properties of Native Kinases ⬇️

scientific article published on June 24, 2011

In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen

scholarly article

In situ selectivity profiling and crystal structure of SML-8-73-1, an active site inhibitor of oncogenic K-Ras G12C

scientific article

Increased lysosomal biomass is responsible for the resistance of triple-negative breast cancers to CDK4/6 inhibition

scientific article published on 17 June 2020

Inhibiting fungal multidrug resistance by disrupting an activator-Mediator interaction

scientific article published on 17 February 2016

Inhibition of ALK, PI3K/MEK, and HSP90 in murine lung adenocarcinoma induced by EML4-ALK fusion oncogene

scientific article

Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein

scientific article published on 21 June 2018

Inhibition of IKKα by BAY61-3606 Reveals IKKα-Dependent Histone H3 Phosphorylation in Human Cytomegalovirus Infected Cells

scientific article

Inhibition of USP10 induces degradation of oncogenic FLT3.

scientific article

Inhibition of the deubiquitinase USP10 induces degradation of SYK

scientific article published on 04 February 2020

Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer

scientific article

Inhibitor-sensitive FGFR2 and FGFR3 mutations in lung squamous cell carcinoma

scientific article published on 20 June 2013

Inhibitors of the Abl kinase directed at either the ATP- or myristate-binding site

scientific article published in March 2010

Interleukin-6 secretion by astrocytes is dynamically regulated by PI3K-mTOR-calcium signaling

scientific article

Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model.

scientific article

It Takes Two To Target: A Study in KRAS Dimerization

scientific article published on 12 April 2018

JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells

scientific article published on 17 May 2019

KRAS G12C Drug Development: Discrimination between Switch II Pocket Configurations Using Hydrogen/Deuterium-Exchange Mass Spectrometry.

scientific article published on 25 July 2017

Kinase inhibitors: the road ahead

scientific article published on 16 March 2018

Kinome-wide selectivity profiling of ATP-competitive mammalian target of rapamycin (mTOR) inhibitors and characterization of their binding kinetics

scientific article published on 5 January 2012

LG-47TYPE II RAF INHIBITORS INHIBIT BRAF MUTATIONS AND TRUNCATED FUSIONS IN PEDIATRIC LOW-GRADE GLIOMAS.

scientific article published on 30 May 2016

Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 – 2011) ⬇️

scientific article published on November 6, 2012

Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome

scientific article published on 11 April 2019

Leveraging Gas-Phase Fragmentation Pathways for Improved Identification and Selective Detection of Targets Modified by Covalent Probes.

scientific article published on 30 November 2016

Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy

scientific article published on October 2012

Light-induced control of protein destruction by opto-PROTAC

scientific article published on 21 February 2020

MEK1 mutations confer resistance to MEK and B-RAF inhibition

scientific article

MELK is an oncogenic kinase essential for mitotic progression in basal-like breast cancer cells.

scientific article

MELK is not necessary for the proliferation of basal-like breast cancer cells

scientific article published on 19 September 2017

Mammalian cell proliferation requires noncatalytic functions of O-GlcNAc transferase

scientific article published on 01 January 2021

Mapping the Degradable Kinome Provides a Resource for Expedited Degrader Development

scientific article published on 01 December 2020

Metabolic and functional genomic studies identify deoxythymidylate kinase as a target in LKB1-mutant lung cancer

scientific article published on 28 May 2013

Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation

scientific article

Mitotic MELK-eIF4B signaling controls protein synthesis and tumor cell survival

scientific article

Modulation of TNFalpha, IL-10 and IL-12p40 levels by a ceramide-1-phosphate analog, PCERA-1, in vivo and ex vivo in primary macrophages.

scientific article published on 29 January 2009

Molecular rationale for the use of PI3K/AKT/mTOR pathway inhibitors in combination with crizotinib in ALK-mutated neuroblastoma

scientific article published on September 2014

Mutations in the DDR2 kinase gene identify a novel therapeutic target in squamous cell lung cancer

scientific article

Myeloid ERK5 deficiency suppresses tumor growth by blocking protumor macrophage polarization via STAT3 inhibition.

scientific article published on 5 March 2018

N-myristoylated c-Abl tyrosine kinase localizes to the endoplasmic reticulum upon binding to an allosteric inhibitor.

scientific article published on 13 August 2009

NVP-TAE684 reverses multidrug resistance (MDR) in human osteosarcoma by inhibiting P-glycoprotein (PGP1) function.

scientific article published on 25 November 2015

Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors

scientific article published on 23 August 2018

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

scientific article

Oncogenic PIK3CA-driven mammary tumors frequently recur via PI3K pathway-dependent and PI3K pathway-independent mechanisms

scientific article

Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma

scientific article published on 05 October 2020

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors

scientific article published on 15 December 2017

PIM kinases are essential for chronic lymphocytic leukemia cell survival (PIM2/3) and CXCR4-mediated microenvironmental interactions (PIM1).

scientific article published on 21 March 2014

Partitioning of cancer therapeutics in nuclear condensates

scientific article published on 01 June 2020

Pathophysiological significance and therapeutic targeting of germinal center kinase in diffuse large B-cell lymphoma

scientific article published on 05 May 2016

Peptide-based covalent inhibitors of MALT1 paracaspase

scientific article published on 29 March 2019

Pharmacological Inhibition of BMK1 Suppresses Tumor Growth through Promyelocytic Leukemia Protein ⬇️

scientific article published on September 14, 2010

Pharmacological cyclin-dependent kinase inhibitors inhibit replication of wild-type and drug-resistant strains of herpes simplex virus and human immunodeficiency virus type 1 by targeting cellular, not viral, proteins

scientific article

Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice

scientific article published on 01 July 2019

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.

scientific article

Pharmacological targeting of kinases MST1 and MST2 augments tissue repair and regeneration

scientific article

Pharmacological targeting of the pseudokinase Her3

scientific article

Phosphorylation of CRTC3 by the salt-inducible kinases controls the interconversion of classically activated and regulatory macrophages

scientific article

Plasticity in binding confers selectivity in ligand-induced protein degradation

scientific article published on 11 June 2018

Potent and Selective Covalent Quinazoline Inhibitors of KRAS G12C.

scientific article published on 27 July 2017

Progress on Covalent Inhibition of KRAS(G12C).

scientific article

Progress towards a public chemogenomic set for protein kinases and a call for contributions

scientific article

Protected amine labels: a versatile molecular scaffold for multiplexed nominal mass and sub-Da isotopologue quantitative proteomic reagents.

scientific article published on 05 February 2014

Protein kinase IKKβ-catalyzed phosphorylation of IRF5 at Ser462 induces its dimerization and nuclear translocation in myeloid cells.

scientific article

Purine-based inhibitors of inositol-1,4,5-trisphosphate-3-kinase

scientific article published on September 2002

Pyrazolopyridines as inhibitors of the kinase LRRK2: a patent evaluation (WO2011141756)

scientific article published on 21 May 2012

Quinoline and thiazolopyridine allosteric inhibitors of MALT1

scientific article published on 20 May 2019

RAS-MAPK reactivation facilitates acquired resistance in FGFR1-amplified lung cancer and underlies a rationale for upfront FGFR-MEK blockade

scientific article published on 13 April 2018

Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

scientific article published on 18 September 2020

Rationally Designed Covalent BCL6 Inhibitor That Targets a Tyrosine Residue in the Homodimer Interface

scientific article published on 03 April 2020

Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors.

scientific article

Recent Advances in Selective and Irreversible Covalent Ligand Development and Validation

scientific article published on 17 October 2019

Resin-capture and release strategy toward combinatorial libraries of 2,6,9-substituted purines

scientific article

Resistance to irreversible EGF receptor tyrosine kinase inhibitors through a multistep mechanism involving the IGF1R pathway

scientific article

Response and acquired resistance to everolimus in anaplastic thyroid cancer

scientific article

Roscovitine targets, protein kinases and pyridoxal kinase

scientific journal article

SIKs control osteocyte responses to parathyroid hormone

scientific article published on 19 October 2016

SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform

scientific article published on 14 February 2018

STRIPAK directs PP2A activity toward MAP4K4 to promote oncogenic transformation of human cells

scientific article published on 08 January 2020

SYK is activated by mutated MYD88 and drives pro-survival signaling in MYD88 driven B-cell lymphomas

scientific article published on 31 January 2020

Salt-Inducible Kinase 2 Couples Ovarian Cancer Cell Metabolism with Survival at the Adipocyte-Rich Metastatic Niche

scientific journal article

Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo

scientific article published on 01 January 2020

Screening of DUB activity and specificity by MALDI-TOF mass spectrometry

scientific article

Selective ATP-competitive inhibitors of TOR suppress rapamycin-insensitive function of TORC2 in Saccharomyces cerevisiae.

scientific article

Selective Akt inhibitors synergize with tyrosine kinase inhibitors and effectively override stroma-associated cytoprotection of mutant FLT3-positive AML cells

scientific article

Selective Aurora Kinase Inhibitors Identified Using a Taxol-Induced Checkpoint Sensitivity Screen

scientific article

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

scientific article published on 31 August 2020

Selective Mediator dependence of cell-type-specifying transcription

scientific article published on 01 June 2020

Selective inhibition of the myeloid Src-family kinase Fgr potently suppresses AML cell growth in vitro and in vivo.

scientific article

Single and Dual Targeting of Mutant EGFR with an Allosteric Inhibitor

scientific article published on 15 May 2019

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

scientific article published on 01 August 2019

Small molecules targeting the flavivirus E protein with broad-spectrum activity and antiviral efficacy in vivo

scientific article published on 14 January 2019

Small molecules that induce cardiomyogenesis in embryonic stem cells

scientific article published in February 2004

Small-Molecule Inhibitors of LRRK2.

scientific article published in January 2017

Small-Molecule Inhibitors of the c-Fes Protein-Tyrosine Kinase

scientific article

Small-molecule inhibitors of USP1 target ID1 degradation in leukemic cells.

scientific article

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function

scientific article

Small-molecule screening identifies inhibition of salt-inducible kinases as a therapeutic strategy to enhance immunoregulatory functions of dendritic cells

scientific article

Small-molecule studies identify CDK8 as a regulator of IL-10 in myeloid cells.

scientific article published on 14 August 2017

Small-molecule targeting of brachyury transcription factor addiction in chordoma

scientific article published on 21 January 2019

SnapShot: Kinase Inhibitors I.

scientific article published on May 2015

SnapShot: Kinase Inhibitors II.

scientific article published on May 2015

Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth

scientific article published on 19 July 2018

Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate

scientific article

Src Family Kinases: Potential Targets for the Treatment of Human Cancer and Leukemia ⬇️

scientific article published on January 1, 2003

Structural Mechanisms Determining Inhibition of the Collagen Receptor DDR1 by Selective and Multi-Targeted Type II Kinase Inhibitors

scientific article

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains

scientific article published on 31 August 2018

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

scientific article published on 04 November 2019

Structural determinants for ERK5 (MAPK7) and leucine rich repeat kinase 2 activities of benzo[e]pyrimido-[5,4-b]diazepine-6(11H)-ones

scientific article published on 29 October 2013

Structure and Characterization of a Covalent Inhibitor of Src Kinase

scientific article published on 19 May 2020

Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance

scientific article published on 01 July 2018

Structure-Activity Relationship Study of Covalent Pan-phosphatidylinositol 5-Phosphate 4-Kinase Inhibitors

scientific article published on 03 November 2019

Structure-Activity Relationship Study of QL47: A Broad-Spectrum Antiviral Agent

scientific article published on 3 February 2017

Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine

scientific article published on 30 January 2020

Structure-activity relationship investigation for benzonaphthyridinone derivatives as novel potent Bruton's tyrosine kinase (BTK) irreversible inhibitors

scientific article published on 9 June 2017

Structure-guided development of covalent TAK1 inhibitors

scientific article published on 9 December 2016

Studies of TAK1-centered polypharmacology with novel covalent TAK1 inhibitors

scientific article published on 7 December 2016

Sulfopin is a covalent inhibitor of Pin1 that blocks Myc-driven tumors in vivo

scientific article published on 10 May 2021

Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression.

scientific article

Suppression of interferon β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members

scientific article

Sustained Akt Activity Is Required to Maintain Cell Viability in Seborrheic Keratosis, a Benign Epithelial Tumor

scientific article published on 28 December 2015

Synergistic interactions with PI3K inhibition that induce apoptosis.

scientific article

Synthesis and structure activity relationships of DCLK1 kinase inhibitors based on a 5,11-dihydro-6H-benzo[e]pyrimido[5,4-b][1,4]diazepin-6-one scaffold

scientific article published on 12 June 2020

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14

scientific article published on 23 May 2019

Synthesis and target identification of hymenialdisine analogs

scientific article

Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,

scientific article published on 26 June 2013

Synthetic Lethal Interaction of SHOC2 Depletion with MEK Inhibition in RAS-Driven Cancers

scientific article published on 01 October 2019

Synthetic small molecules that control stem cell fate

scientific article

Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency

scientific article published on 22 August 2014

Systematic Identification of Culture Conditions for Induction and Maintenance of Naive Human Pluripotency.

scientific article

Systematic analysis of BRAF(V600E) melanomas reveals a role for JNK/c-Jun pathway in adaptive resistance to drug-induced apoptosis

scientific article

Systematic identification of culture conditions for induction and maintenance of naive human pluripotency

scientific article

Systematic kinome shRNA screening identifies CDK11 (PITSLRE) kinase expression is critical for osteosarcoma cell growth and proliferation

scientific article

THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors

scientific article published on 30 January 2017

TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma

scientific article published on 29 July 2021

TSC1 involvement in bladder cancer: diverse effects and therapeutic implications

scientific article published on 21 March 2013

TYK2-STAT1-BCL2 pathway dependence in T-cell acute lymphoblastic leukemia

scientific article published on 7 March 2013

Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma

article

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models

scientific article published on 25 March 2019

Targeting Bcr–Abl by combining allosteric with ATP-binding-site inhibitors

scientific article

Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13

scientific article published on 13 November 2018

Targeting Myddosome Assembly in Waldenstrom Macroglobulinaemia

scientific article published on 13 April 2016

Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells

Targeting the PI5P4K Lipid Kinase Family in Cancer Using Covalent Inhibitors

scientific article published on 03 March 2020

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor

scientific article

Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor

scientific article

The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma

scientific article published in July 2012

The Dawn of Allosteric BCR-ABL1 Drugs: From a Phenotypic Screening Hit to an Approved Drug

scientific article published in 2022

The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling

scientific article

The LKB1-salt-inducible kinase pathway functions as a key gluconeogenic suppressor in the liver

scientific article

The Library of Integrated Network-Based Cellular Signatures NIH Program: System-Level Cataloging of Human Cells Response to Perturbations

scientific article published on 24 November 2017

The Neuroblastoma-Associated F1174L ALK Mutation Causes Resistance to an ALK Kinase Inhibitor in ALK-Translocated Cancers ⬇️

scientific article published on October 28, 2010

The dTAG system for immediate and target-specific protein degradation.

scientific article published on 26 March 2018

The evolving war on cancer

scientific article published on 01 April 2011

The ins and outs of selective kinase inhibitor development

scientific article published on October 2015

The kinase ALK stimulates the kinase ERK5 to promote the expression of the oncogene MYCN in neuroblastoma

scientific article published on 28 October 2014

The mTOR-regulated phosphoproteome reveals a mechanism of mTORC1-mediated inhibition of growth factor signaling.

scientific article

The mechanism of activation of IRAK1 and IRAK4 by interleukin-1 and Toll-like receptor agonists.

scientific article

The mitogen-activated protein kinase ERK5 regulates the development and growth of hepatocellular carcinoma.

scientific article published on 2 September 2014

The promise and peril of chemical probes

scientific article

Therapeutic targeting of oncogenic K-Ras by a covalent catalytic site inhibitor

scientific article published on 20 November 2013

Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines

scientific article published on 29 August 2014

Torin2 Exploits Replication and Checkpoint Vulnerabilities to Cause Death of PI3K-Activated Triple-Negative Breast Cancer Cells

scientific article published on 04 December 2019

Torin2 Suppresses Ionizing Radiation-Induced DNA Damage Repair

scientific article published on 02 May 2016

Treatment-Induced Tumor Dormancy through YAP-Mediated Transcriptional Reprogramming of the Apoptotic Pathway

scientific article published on 01 January 2020

Tubulin Resists Degradation by Cereblon-Recruiting PROTACs

scientific article published on 27 April 2020

Tuning microtubule dynamics to enhance cancer therapy by modulating FER-mediated CRMP2 phosphorylation.

scientific article

ULK1 inhibition overcomes compromised antigen presentation and restores antitumor immunity in LKB1 mutant lung cancer

scientific article published on 17 May 2021

Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R

scientific article

Verification of a designed intramolecular hydrogen bond in a drug scaffold by nuclear magnetic resonance spectroscopy

scientific article

Vomocytosis of live pathogens from macrophages is regulated by the atypical MAP kinase ERK5

scientific article published on 16 August 2017

X-ray Crystal Structure of ERK5 (MAPK7) in Complex with a Specific Inhibitor

scientific article

YAP Drives Growth by Controlling Transcriptional Pause Release from Dynamic Enhancers

scientific article

YY1 Is a Structural Regulator of Enhancer-Promoter Loops

scientific article published on 30 November 2017

mTOR Mediated Anti-Cancer Drug Discovery

scientific article published on January 2009

mTORC1 phosphorylation sites encode their sensitivity to starvation and rapamycin

scientific article

p42/p44 MAPKs are intracellular targets of the CDK inhibitor purvalanol

scientific article

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