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List of works by Stefan Knapp

10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acids are selective inhibitors of DYRK1A.

scientific article published on 23 March 2015

19 F NMR isotropic chemical shift for efficient screening of fluorinated fragments which are racemates and/or display multiple conformers

scientific article published in August 2017

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands

scientific article

7,8-Dichloro-1-oxo-β-carbolines as a Versatile Scaffold for the Development of Potent and Selective Kinase Inhibitors with Unusual Binding Modes

scientific article

A Chemical Probe for Dark Kinase STK17B Derives Its Potency and High Selectivity through a Unique P-Loop Conformation

scientific article published on 20 November 2020

A Highly Selective Chemical Probe for Activin Receptor-like Kinases ALK4 and ALK5

scientific article published on 20 March 2020

A Novel Biphenyl-based Chemotype of Retinoid X Receptor Ligands Enables Subtype and Heterodimer Preferences

scientific article published on 16 August 2019

A chemical toolbox for the study of bromodomains and epigenetic signaling

scientific article published on 23 April 2019

A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination

scientific article (publication date: 2014)

A core of kinase-regulated interactomes defines the neoplastic MDSC lineage

scientific article

A public-private partnership to unlock the untargeted kinome

scientific article published in January 2013

A series of potent CREBBP bromodomain ligands reveals an induced-fit pocket stabilized by a cation-π interaction

scientific article published on 12 May 2014

A small-molecule inhibitor of Haspin alters the kinetochore functions of Aurora B

scientific article

A structure-based approach towards identification of inhibitory fragments for eleven-nineteen-leukemia protein (ENL)

scientific article published on 26 November 2018

A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases

scientific article

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

scientific article published on 7 September 2014

A versatile spectrophotometric protein tyrosine phosphatase assay based on 3-nitrophosphotyrosine containing substrates.

scientific article

Accurate calculation of the absolute free energy of binding for drug molecules

scientific article

Activation by substoichiometric inhibition

scientific article published on 06 January 2020

Activation segment dimerization: a mechanism for kinase autophosphorylation of non-consensus sites

scientific article

Activation segment exchange: a common mechanism of kinase autophosphorylation?

scientific article published on 12 July 2007

An Unusual Binding Model of the Methyl 9-Anilinothiazolo[5,4-f] quinazoline-2-carbimidates (EHT 1610 and EHT 5372) Confers High Selectivity for Dual-Specificity Tyrosine Phosphorylation-Regulated Kinases

scientific article

Analysis of conditions affecting auto-phosphorylation of human kinases during expression in bacteria

scientific article

Analysis of the flanking regions from different haemolysin determinants of Escherichia coli

scientific article published on 01 January 1985

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching

scientific article

Atad2 is a generalist facilitator of chromatin dynamics in embryonic stem cells

scientific article

BET inhibition as a new strategy for the treatment of gastric cancer

scientific article

BRD4 localization to lineage-specific enhancers is associated with a distinct transcription factor repertoire.

scientific article published on 19 September 2016

BRD4 promotes p63 and GRHL3 expression downstream of FOXO in mammary epithelial cells

scientific article

Benzodiazepines and benzotriazepines as protein interaction inhibitors targeting bromodomains of the BET family

scientific article

Benzoselenadiazole-based responsive long-lifetime photoluminescent probes for protein kinases.

scientific article published in April 2014

Binding Kinetics Survey of the Drugged Kinome

scientific article published on 06 November 2018

Biochemical characterization of TASSELSEED 2, an essential plant short-chain dehydrogenase/reductase with broad spectrum activities

scientific article

Bisubstrate inhibitor approach for targeting mitotic kinase Haspin

scientific article published on 29 January 2015

Bromo-deaza-SAH: a potent and selective DOT1L inhibitor

scientific article published on 30 January 2013

Bromodomain protein BRD4 is required for estrogen receptor-dependent enhancer activation and gene transcription

scientific article published on 10 July 2014

Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells

scientific article

Bromodomain-peptide displacement assays for interactome mapping and inhibitor discovery

scientific article published in 2011

Bromodomains as therapeutic targets

scientific article published on 13 September 2011

CBP/p300 Bromodomains Regulate Amyloid-like Protein Aggregation upon Aberrant Lysine Acetylation

scientific article (publication date: 19 January 2017)

CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses

scientific article

Cancer Genomics and Biology 2015 – Meeting Report

scientific article

Cardiac myosin light chain is phosphorylated by Ca2+/calmodulin-dependent and -independent kinase activities

scientific article published on 20 June 2016

Citrullination-acetylation interplay guides E2F-1 activity during the inflammatory response

scientific article published on 05 February 2016

Co-crystal structures of the protein kinase haspin with bisubstrate inhibitors

scientific article published on 22 April 2016

Comprehensive characterization of the Published Kinase Inhibitor Set

scientific article

Conservation of structure, function and inhibitor binding in UNC-51-like kinase 1 and 2 (ULK1/2)

scientific article published on 12 March 2019

Construction of human activity-based phosphorylation networks.

scientific article

Copper is required for oncogenic BRAF signalling and tumorigenesis

scientific article (publication date: 22 May 2014)

Coupling PAF Signaling to Dynein Regulation

Critical residues for structure and catalysis in short-chain dehydrogenases/reductases

scientific article

Crystal Structure and Inhibitor Identifications Reveal Targeting Opportunity for the Atypical MAPK Kinase ERK3

scientific article published on 26 October 2020

Crystal Structure of Human Aurora B in Complex with INCENP and VX-680

scientific article

Crystal Structure of Sphingosine Kinase 1 with PF-543

scientific article published on 27 October 2014

Crystal Structures of ABL-Related Gene (ABL2) in Complex with Imatinib, Tozasertib (VX-680), and a Type I Inhibitor of the Triazole Carbothioamide Class

scientific article

Crystal Structures of the p21-Activated Kinases PAK4, PAK5, and PAK6 Reveal Catalytic Domain Plasticity of Active Group II PAKs

scientific article

Crystal structure of human protein tyrosine phosphatase 14 (PTPN14) at 1.65-A resolution

scientific article

Crystal structure of the PIM2 kinase in complex with an organoruthenium inhibitor

scientific article

Crystal structure of the SOCS2-elongin C-elongin B complex defines a prototypical SOCS box ubiquitin ligase

scholarly article

Crystal structure of the tetrameric Mad1-Mad2 core complex: implications of a 'safety belt' binding mechanism for the spindle checkpoint

scientific article

Crystal structure of the tyrosine kinase domain of the hepatocyte growth factor receptor c-Met and its complex with the microbial alkaloid K-252a

scientific article

Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases

scientific article

DNA damage in oocytes induces a switch of the quality control factor TAp63α from dimer to tetramer

scientific article

Decoding the Papain Inhibitor from Streptomyces mobaraensis as Being Hydroxylated Chymostatin Derivatives: Purification, Structure Analysis, and Putative Biosynthetic Pathway

scientific article published on 30 September 2020

Defined PEG smears as an alternative approach to enhance the search for crystallization conditions and crystal-quality improvement in reduced screens

scientific article published on 28 July 2015

Design of a Chemical Probe for the Bromodomain and Plant Homeodomain Finger-Containing (BRPF) Family of Proteins.

scientific article published on 17 July 2017

Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer

scientific article published on 17 November 2020

Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders

Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity

scientific article published on 21 February 2019

Development of Selective CBP/P300 Benzoxazepine Bromodomain Inhibitors

scientific article

Development of a chemical probe against NUDT15

scientific article published on 20 July 2020

Development, Optimization, and Structure-Activity Relationships of Covalent-Reversible JAK3 Inhibitors Based on a Tricyclic Imidazo[5,4- d]pyrrolo[2,3- b]pyridine Scaffold

scientific article published on 13 June 2018

Differential Recognition Preferences of the Three Src Homology 3 (SH3) Domains from the Adaptor CD2-associated Protein (CD2AP) and Direct Association with Ras and Rab Interactor 3 (RIN3).

scientific article published on 20 August 2015

Discovery and Characterization of GSK2801, a Selective Chemical Probe for the Bromodomains BAZ2A and BAZ2B.

scientific article published on 23 March 2015

Discovery and Optimization of a Selective Ligand for the Switch/Sucrose Nonfermenting-Related Bromodomains of Polybromo Protein-1 by the Use of Virtual Screening and Hydration Analysis

scientific article

Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains

scientific article (publication date: 2 July 2014)

Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening

scientific article published on 20 September 2016

Discovery of Novel Small-Molecule Inhibitors of BRD4 Using Structure-Based Virtual Screening

scientific article

Discovery of a Chemical Tool Inhibitor Targeting the Bromodomains of TRIM24 and BRPF.

scientific article published on 14 May 2015

Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK

scientific article published on 04 December 2020

Discovery of a PCAF Bromodomain Chemical Probe

scientific article published on 14 December 2016

Discovery of a potent and selective inhibitor for human carbonyl reductase 1 from propionate scanning applied to the macrolide zearalenone

scientific article

Discovery of a selective allosteric inhibitor targeting macrodomain 2 of poly-adenosine-diphosphate-ribose polymerases 14.

scientific article published on 9 October 2017

Discovery of pyrido[3,4-g]quinazoline derivatives as CMGC family protein kinase inhibitors: Design, synthesis, inhibitory potency and X-ray co-crystal structure

scientific article

Discovery of the First in Vivo Active Inhibitors of the Soluble Epoxide Hydrolase Phosphatase Domain

scientific article published on 17 September 2019

Discovery of the sEH Inhibitor Epoxykynin as a Potent Kynurenine Pathway Modulator

scientific article published in 2024

Dissection of PIM serine/threonine kinases in FLT3-ITD-induced leukemogenesis reveals PIM1 as regulator of CXCL12-CXCR4-mediated homing and migration

scientific article

Diverse Levels of Sequence Selectivity and Catalytic Efficiency of Protein-Tyrosine Phosphatases

scientific article

Doing more than just the structure-structural genomics in kinase drug discovery.

scientific article

Druggability analysis and structural classification of bromodomain acetyl-lysine binding sites

scientific article published on 12 July 2012

Drugging the “Undruggable” MYCN Oncogenic Transcription Factor: Overcoming Previous Obstacles to Impact Childhood Cancers

scientific article published in 2021

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

scientific article

Effect of BET Missense Mutations on Bromodomain Function, Inhibitor Binding and Stability

scientific article

Effect of single amino acid substitution observed in cancer on Pim-1 kinase thermodynamic stability and structure

scientific article

Emerging Target Families: Intractable Targets

scientific article

Erratum: Corrigendum: The promise and peril of chemical probes

scientific article published in November 2015

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

scientific article

Exploring Selective Inhibition of the First Bromodomain of the Human Bromodomain and Extra-terminal Domain (BET) Proteins

scientific article

Extremely Tight Binding of a Ruthenium Complex to Glycogen Synthase Kinase 3

scientific article

Family-wide Structural Analysis of Human Numb-Associated Protein Kinases

scientific article published on 29 January 2016

Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors

scientific article published on 26 November 2019

Fragment screening of cyclin G-associated kinase by weak affinity chromatography

scientific article

Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy

scientific article

Girls homozygous for an IL-2-inducible T cell kinase mutation that leads to protein deficiency develop fatal EBV-associated lymphoproliferation

scientific article published on May 2009

HD-PTP is a catalytically inactive tyrosine phosphatase due to a conserved divergence in its phosphatase domain

scientific article

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.

scientific article

High-throughput NMR-based screening with competition binding experiments

scientific article published in July 2002

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

scientific article

High-throughput structural characterisation of therapeutic protein targets

Highly functionalized terpyridines as competitive inhibitors of AKAP-PKA interactions

scientific article published on 23 September 2013

Histone recognition and large-scale structural analysis of the human bromodomain family

scientific article

Hot spots in Tcf4 for the interaction with beta-catenin

scientific article published on 25 March 2003

How to Separate Kinase Inhibition from Undesired Monoamine Oxidase A Inhibition-The Development of the DYRK1A Inhibitor AnnH75 from the Alkaloid Harmine

scientific article published on 16 December 2020

Hyperactive locomotion in a Drosophila model is a functional readout for the synaptic abnormalities underlying fragile X syndrome.

scientific article published on 2 May 2017

Identification and Development of 2,3-Dihydropyrrolo[1,2-a]quinazolin-5(1H)-one Inhibitors Targeting Bromodomains within the Switch/Sucrose Nonfermenting Complex

scientific article published on 27 April 2016

Identification and characterization of a small-molecule inhibitor of death-associated protein kinase 1.

scientific article published on 7 November 2014

Identification and structure-function analysis of subfamily selective G protein-coupled receptor kinase inhibitors

scientific article

Identification of CLK1 Inhibitors by a Fragment-linking Based Virtual Screening

scientific article

Identification of a Chemical Probe for Bromo and Extra C-Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit

scientific article

Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit

scientific article

Identification of a Major Determinant for Serine-Threonine Kinase Phosphoacceptor Specificity

scientific article

Inhibition of BET bromodomain targets genetically diverse glioblastoma

scientific article

Inhibition of protein-protein interactions: The discovery of druglike β-catenin inhibitors by combining virtual and biophysical screening

scholarly article by Jean-Yves Trosset published in March 2006

Inhibitor affinity chromatography: profiling the specific reactivity of the proteome with immobilized molecules.

scientific article published in July 2003

Insights for the development of specific kinase inhibitors by targeted structural genomics

scientific article published on 29 March 2007

Insights into protein kinase regulation and inhibition by large scale structural comparison

scientific article

Kinase Domain Insertions Define Distinct Roles of CLK Kinases in SR Protein Phosphorylation

scientific article

Kinase inhibitor selectivity profiling using differential scanning fluorimetry

scientific article

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

scientific article

LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

scientific article (publication date: 18 May 2015)

Large-scale structural analysis of the classical human protein tyrosine phosphatome

scientific article

Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing.

scientific article published on 26 May 2011

Linear Motif Atlas for Phosphorylation-Dependent Signaling

scientific article (publication date: 2 September 2008)

MAPK-specific tyrosine phosphatases: new targets for drug discovery?

scientific article published on 21 August 2006

Maintenance of muscle myosin levels in adult C. elegans requires both the double bromodomain protein BET-1 and sumoylation

scientific article

Mapping the chemical chromatin reactivation landscape identifies BRD4-TAF1 cross-talk

scientific article

Mechanism and consequence of the autoactivation of p38α mitogen-activated protein kinase promoted by TAB1

scientific article

Mechanism of TAp73 inhibition by ΔNp63 and structural basis of p63/p73 hetero-tetramerization

scientific article

Modulation of the Chromatin Phosphoproteome by the Haspin Protein Kinase

scientific article

Molecular basis of histone tail recognition by human TIP5 PHD finger and bromodomain of the chromatin remodeling complex NoRC.

scientific article published on 18 December 2014

Multiple copies of hemolysin genes and associated sequences in the chromosomes of uropathogenic Escherichia coli strains ⬇️

scientific article published on September 1, 1984

NMR-Based screening with competition water-ligand observed via gradient spectroscopy experiments: detection of high-affinity ligands

scientific article

Nanog requires BRD4 to maintain murine embryonic stem cell pluripotency and is suppressed by bromodomain inhibitor JQ1 together with Lefty1

scientific article published on 17 December 2014

New potent dual inhibitors of CK2 and Pim kinases: discovery and structural insights

scientific article

Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases

scientific article published on November 2012

Novel approaches for targeting kinases: allosteric inhibition, allosteric activation and pseudokinases

scientific article published on April 2014

Optimization of 3,5-Dimethylisoxazole Derivatives as Potent Bromodomain Ligands

scientific article

Out of the box binding determines specificity of SH2 domain interaction

scientific article published on August 2009

Overcoming ABCG2-mediated drug resistance with imidazo-[1,2-b]-pyridazine-based Pim1 kinase inhibitors

scientific article published on 9 September 2015

PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains

scientific article

PIM serine/threonine kinases in the pathogenesis and therapy of hematologic malignancies and solid cancers

scientific article

PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase

scientific article published on 28 September 2020

Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis

scientific article published on 20 November 2020

Perspective on computational and structural aspects of kinase discovery from IPK2014

scientific article

Pharmacological inhibition of LIM kinase stabilizes microtubules and inhibits neoplastic growth

scientific article

Photosensitization enables Pauson-Khand–type reactions with nitrenes

scientific article published on 01 February 2024

Pim Kinase Inhibitors Evaluated with a Single-Molecule Engineered Nanopore Sensor

scientific article published on 8 June 2015

Predictions of Ligand Selectivity from Absolute Binding Free Energy Calculations

scientific article (publication date: 18 January 2017)

Probing the epigenome

scientific article published in August 2015

Progress in the development and application of small molecule inhibitors of bromodomain-acetyl-lysine interactions

scientific article published on 27 September 2012

Promiscuous targeting of bromodomains by bromosporine identifies BET proteins as master regulators of primary transcription response in leukemia.

scientific article published on 12 October 2016

Propionate analogues of zearalenone bind to Hsp90.

scientific article

Protein production and purification

scientific article

Protein stabilisation by compatible solutes: effect of mannosylglycerate on unfolding thermodynamics and activity of ribonuclease A.

scientific article published in August 2003

Protein-Protein Interaction Inhibition (2P2I)-Oriented Chemical Library Accelerates Hit Discovery

scientific article

Protein–protein interaction site mapping using NMR-detected mutational scanning

article

Quality control in oocytes by p63 is based on a spring-loaded activation mechanism on the molecular and cellular level.

scientific article published on 29 March 2016

RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain

scientific article

Rapid determination of multiple linear kinase substrate motifs by mass spectrometry

scientific article

Recently targeted kinases and their inhibitors-the path to clinical trials

scientific article

Regulation of the wild-type and Y1235D mutant Met kinase activation

scientific article published in November 2005

Restoring p53 Function in Human Melanoma Cells by Inhibiting MDM2 and Cyclin B1/CDK1-Phosphorylated Nuclear iASPP.

scientific article

Restoring p53 function in human melanoma cells by inhibiting MDM2 and cyclin B1/CDK1-phosphorylated nuclear iASPP

scientific article

Ruthenium half-sandwich complexes bound to protein kinase Pim-1

scientific article

SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK)

scientific article published on 26 February 2019

SH2 domains: modulators of nonreceptor tyrosine kinase activity

scientific article

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

scientific journal article

Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents

scientific article

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

scientific article published on 7 November 2016

Selective bisubstrate inhibitors with sub-nanomolar affinity for protein kinase Pim-1.

scientific article published on 24 April 2013

Selective inhibition of BET bromodomains

scientific article

Selective targeting of Bromodomains of the Bromodomain-PHD Fingers family impairs osteoclast differentiation

scientific article published on 29 August 2017

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.

scientific article published on 13 November 2015

Selectivity, cocrystal structures, and neuroprotective properties of leucettines, a family of protein kinase inhibitors derived from the marine sponge alkaloid leucettamine B

scientific article

Similar Biological Activities of Two Isostructural Ruthenium and Osmium Complexes

scientific article

Single-Molecule Protein Phosphorylation and Dephosphorylation by Nanopore Enzymology

scientific article published on 04 January 2019

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

scientific article

Small-molecule inhibition of BRDT for male contraception

scientific article

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

scientific article

Small-molecule modulators for epigenetics targets

scientific article

Specific CLK Inhibitors from a Novel Chemotype for Regulation of Alternative Splicing

scientific article

Specificity profiling of Pak kinases allows identification of novel phosphorylation sites

scientific article

Spontaneous deletions and flanking regions of the chromosomally inherited hemolysin determinant of an Escherichia coli O6 strain ⬇️

scientific article published on June 1, 1983

Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy

scientific article

Stimulation of Hepatic Apolipoprotein A-I Production by Novel Thieno-Triazolodiazepines: Roles of the Classical Benzodiazepine Receptor, PAF Receptor, and Bromodomain Binding

scientific article published on 22 December 2013

Stochastic detection of Pim protein kinases reveals electrostatically enhanced association of a peptide substrate

scientific article

Structural Basis for Cul3 Protein Assembly with the BTB-Kelch Family of E3 Ubiquitin Ligases

scientific article

Structural Basis for c-KIT Inhibition by the Suppressor of Cytokine Signaling 6 (SOCS6) Ubiquitin Ligase

scientific article

Structural Comparison of Human Mammalian Ste20-Like Kinases

scientific article published on 6 August 2010

Structural Determinants of G-protein   Subunit Selectivity by Regulator of G-protein Signaling 2 (RGS2)

scientific article

Structural Insights into Interaction Mechanisms of Alternative Piperazine-urea YEATS Domain Binders in MLLT1

scientific article published on 25 November 2019

Structural Insights into Pseudokinase Domains of Receptor Tyrosine Kinases

scientific article published on 24 June 2020

Structural analysis identifies imidazo[1,2-b]pyridazines as PIM kinase inhibitors with in vitro antileukemic activity

scientific article

Structural and Functional Characterization of the Human Protein Kinase ASK1

scientific article

Structural basis for Cul3 protein assembly with the BTB-Kelch family of E3 ubiquitin ligases

scientific article published on 27 September 2013

Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase

scientific article published in December 2005

Structural coupling of SH2-kinase domains links Fes and Abl substrate recognition and kinase activation

scientific article

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

Structural genomics of histone tail recognition

scientific article

Structural insights into the activation of MST3 by MO25

scientific article

Structural stability of human protein tyrosine phosphatase ρ catalytic domain: effect of point mutations

scientific article

Structurally Sophisticated Octahedral Metal Complexes as Highly Selective Protein Kinase Inhibitors

scientific article

Structure and functional characterization of the atypical human kinase haspin

scientific article

Structure and regulation of the human Nek2 centrosomal kinase

scientific article

Structure and substrate specificity of the Pim-1 kinase

scientific article published on 13 October 2005

Structure enabled design of BAZ2-ICR, a chemical probe targeting the bromodomains of BAZ2A and BAZ2B.

scientific article published on 26 February 2015

Structure of cyclin G-associated kinase (GAK) trapped in different conformations using nanobodies

scientific article

Structure of dystrophia myotonica protein kinase

scientific article

Structure of the CaMKIIdelta/calmodulin complex reveals the molecular mechanism of CaMKII kinase activation

scientific article

Structure of the Human Protein Kinase ZAK in Complex with Vemurafenib

scientific article

Structure of the Pseudokinase VRK3 Reveals a Degraded Catalytic Site, a Highly Conserved Kinase Fold, and a Putative Regulatory Binding Site

scientific article

Structure of the SOCS4-ElonginB/C Complex Reveals a Distinct SOCS Box Interface and the Molecular Basis for SOCS-Dependent EGFR Degradation

scientific article

Structure of the bone morphogenetic protein receptor ALK2 and implications for fibrodysplasia ossificans progressiva

scientific article

Structure of the human protein kinase MPSK1 reveals an atypical activation loop architecture

scientific article published in January 2008

Structure, function, and regulation of the plasmid-encoded hemolysin determinant of Escherichia coli

scientific article published on 01 January 1985

Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor

scientific article

Structure-Based Identification of Inhibitory Fragments Targeting the p300/CBP-Associated Factor Bromodomain

scientific article published on 5 January 2016

Structures of Down Syndrome Kinases, DYRKs, Reveal Mechanisms of Kinase Activation and Substrate Recognition

scientific article

Structures of the human eIF4E homologous protein, h4EHP, in its m7GTP-bound and unliganded forms

scientific article

Synthesis and structure-activity relationships of 3,5-disubstituted-pyrrolo[2,3- b]pyridines as inhibitors of adaptor associated kinase 1 (AAK1) with antiviral activity

scientific article published on 12 June 2019

Synthesis, kinase inhibitory potencies, and in vitro antiproliferative evaluation of new Pim kinase inhibitors

scientific article

Targeting Low-Druggability Bromodomains: Fragment Based Screening and Inhibitor Design against the BAZ2B Bromodomain

scientific article

Targeting bromodomains: epigenetic readers of lysine acetylation

scientific article (publication date: May 2014)

Targeting group II PAKs in cancer and metastasis

scientific article published on June 2009

Targeting kinases for the treatment of inflammatory diseases

scientific article published on 15 July 2010

Targeting the Protein Kinases Cysteinome.

scientific article published on 10 October 2017

Testis specific gene expression drives disease progression and Rituximab resistance in lymphoma ⬇️

scientific article published on August 1, 2013

The (un)targeted cancer kinome

scientific article published in March 2010

The BET inhibitor JQ1 selectively impairs tumour response to hypoxia and downregulates CA9 and angiogenesis in triple negative breast cancer

scientific article published on 13 June 2016

The Global Cancer Genomics Consortium's Second Annual Symposium: Genomics Medicine in Cancer Research

scientific article published on 17 April 2013

The Intersection of Structural and Chemical Biology - An Essential Synergy

scientific article

The Long Acidic Tail of High Mobility Group Box 1 (HMGB1) Protein Forms an Extended and Flexible Structure That Interacts with Specific Residues within and between the HMG Boxes†

scientific article published in September 2004

The MAPK Pathway Regulates Intrinsic Resistance to BET Inhibitors in Colorectal Cancer

scientific article published on 27 September 2016

The Structure of the Full-Length Tetrameric PKA Regulatory RII Complex Reveals the Mechanism of Allosteric PKA Activation

scientific article published on 8 May 2012

The bromodomain interaction module ⬇️

scientific article published on 03 May 2012

The crystal structure of human receptor protein tyrosine phosphatase kappa phosphatase domain 1

scientific article

The crystal structure of the RhoA-AKAP-Lbc DH-PH domain complex

scientific journal article

The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains

scientific article published on January 2013

The global cancer genomics consortium's symposium: new era of molecular medicine and epigenetic cancer medicine - cross section of genomics and epigenetics

scientific article published in January 2015

The global cancer genomics consortium's third annual symposium: from oncogenomics to cancer care

scientific article

The ins and outs of selective kinase inhibitor development

scientific article published on October 2015

The molecular mechanism of nitrogen-containing bisphosphonates as antiosteoporosis drugs

scholarly article

The p53 cofactor Strap exhibits an unexpected TPR motif and oligonucleotide-binding (OB)-fold structure

scientific article

The promise and peril of chemical probes

scientific article

The scientific impact of the Structural Genomics Consortium: a protein family and ligand-centered approach to medically-relevant human proteins

scientific article published on September 2007

The structural basis of PI3K cancer mutations: from mechanism to therapy

scientific article published on 23 January 2014

The structure of P-TEFb (CDK9/cyclin T1), its complex with flavopiridol and regulation by phosphorylation

scientific article

Thermal unfolding of the archaeal DNA and RNA binding protein Ssh10.

scientific article published on 20 June 2008

Thermodynamic properties of leukotriene A4 hydrolase inhibitors

scientific article

Topical antiangiogenic SRPK1 inhibitors reduce choroidal neovascularization in rodent models of exudative AMD

scientific article published on 05 September 2013

Type II Inhibitors Targeting CDK2

scientific article

UnPAKing the class differences among p21-activated kinases

scientific article published on 17 July 2008

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

scientific article

[1,2,4]triazolo[4,3-a]phthalazines: inhibitors of diverse bromodomains

scientific article

[b]-Annulated Halogen-Substituted Indoles as Potential DYRK1A Inhibitors

scientific article published on 13 November 2019

p63 uses a switch-like mechanism to set the threshold for induction of apoptosis

scientific article published on 27 July 2020

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