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List of works by Paul Workman

3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone

scientific article

4,5-diarylisoxazole Hsp90 chaperone inhibitors: potential therapeutic agents for the treatment of cancer

scientific article

4-Amino derivatives of the Hsp90 inhibitor CCT018159.

scientific article published on 9 February 2006

A HIF-regulated VHL-PTP1B-Src signaling axis identifies a therapeutic target in renal cell carcinoma

scientific article published on June 2011

A Phase II trial of 17-allylamino, 17-demethoxygeldanamycin (17-AAG, tanespimycin) in patients with metastatic melanoma

scientific article published on 5 August 2010

A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms.

scientific article

A liquid chromatographic-tandem mass spectrometric method for the determination of two selective thymidylate synthase inhibitors, BGC945 and BGC638, in mouse plasma

scientific article published in September 2005

A phase I study of SR-4554 via intravenous administration for noninvasive investigation of tumor hypoxia by magnetic resonance spectroscopy in patients with malignancy ⬇️

scientific article published on November 1, 2003

A phase I study of the heat shock protein 90 inhibitor alvespimycin (17-DMAG) given intravenously to patients with advanced solid tumors

scientific article

A public-private partnership to unlock the untargeted kinome

scientific article published in January 2013

A selective PIKfyve inhibitor blocks PtdIns(3,5)P(2) production and disrupts endomembrane transport and retroviral budding

scientific article

A stressful life (or death): Combinatorial proteotoxic approaches to cancer-selective therapeutic vulnerability ⬇️

scientific article published on April 1, 2011

A structural comparison of inhibitor binding to PKB, PKA and PKA-PKB chimera

scientific article

A useful approach to identify novel small-molecule inhibitors of Wnt-dependent transcription

scientific article published on 7 July 2010

AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity

scientific article

AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth

scientific article

ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

scientific article

Acquired resistance to 17-allylamino-17-demethoxygeldanamycin (17-AAG, tanespimycin) in glioblastoma cells

scientific article published on 24 February 2009

Activated B-RAF is an Hsp90 client protein that is targeted by the anticancer drug 17-allylamino-17-demethoxygeldanamycin

scientific article published on December 2005

Activation of the ATPase activity of hsp90 by the stress-regulated cochaperone aha1

scientific article

Altered states: selectively drugging the Hsp90 cancer chaperone

scientific article published on February 2004

An evaluation of the ability of pifithrin-alpha and -beta to inhibit p53 function in two wild-type p53 human tumor cell lines

scientific article published on September 2005

An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models

scientific article published on 10 January 2008

Application of meso scale technology for the measurement of phosphoproteins in human tumor xenografts

scientific article

Assays for HSP90 and inhibitors.

scientific article

Assays for the identification and evaluation of histone acetyltransferase inhibitors

scientific article

Assessing the mechanism and therapeutic potential of modulators of the human Mediator complex-associated protein kinases

scientific article (publication date: 9 December 2016)

Auditing the pharmacological accounts for Hsp90 molecular chaperone inhibitors: unfolding the relationship between pharmacokinetics and pharmacodynamics.

scientific article

Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells

scientific article

BRAF and NRAS mutations in melanoma: potential relationships to clinical response to HSP90 inhibitors

scientific article

Benzoquinone ansamycin heat shock protein 90 inhibitors modulate multiple functions required for tumor angiogenesis

scientific article published on March 2006

Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941

scientific article published on 07 July 2009

Biomarker-driven early clinical trials in oncology: a paradigm shift in drug development

scientific article published on September 2009

Biopsy-Derived Biomarkers in Phase I Trials: Building Confidence in Drug Development.

scientific article

Bioreductive prodrugs for cancer therapy

scientific article published on January 2004

Blocking the survival of the nastiest by HSP90 inhibition

scientific article

CHK1 inhibition is synthetically lethal with loss of B-family DNA polymerase function in human lung and colorectal cancer cells

scientific article published on 11 March 2020

Can molecular biomarker-based patient selection in Phase I trials accelerate anticancer drug development?

scientific article published on 02 December 2009

Cancer genome targets: RAF-ing up tumor cells to overcome oncogene addiction

scientific article

Cancer: drug-tolerant insurgents

scientific article published in April 2010

Cassette dosing pharmacokinetics of a library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 inhibitors prepared by parallel synthesis

scientific article published in March 2004

Chemical biology approaches to target validation in cancer

scientific article published on 28 August 2014

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

scientific article

Co-Crystalization and In Vitro Biological Characterization of 5-Aryl-4-(5-Substituted-2-4-Dihydroxyphenyl)-1,2,3-Thiadiazole Hsp90 Inhibitors

scientific article

Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone

scientific article published on April 2004

Combinatorial drug therapy for cancer in the post-genomic era.

scientific article

Combining hit identification strategies: fragment-based and in silico approaches to orally active 2-aminothieno[2,3-d]pyrimidine inhibitors of the Hsp90 molecular chaperone

scientific article

Combining trail with PI3 kinase or HSP90 inhibitors enhances apoptosis in colorectal cancer cells via suppression of survival signaling

scientific article published on August 2013

Correction: Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases

scientific article published on 24 February 2020

Correlation of overall survival with gene expression profiles in a prospective study of resectable esophageal cancer

scientific article published in March 2011

Critical parameters in targeted drug development: the pharmacological audit trail

scientific article

Death by chaperone: HSP90, HSP70 or both?

scientific article

Demonstrating In-Cell Target Engagement Using a Pirin Protein Degradation Probe (CCT367766).

scientific article

Design, synthesis and biological evaluation of 6-pyridylmethylaminopurines as CDK inhibitors

scientific article published on 31 August 2011

Determinants of response to epidermal growth factor receptor tyrosine kinase inhibition in squamous cell carcinoma of the head and neck

scientific article

Development and validation of a sensitive solid-phase-extraction and high-performance liquid chromatography assay for the bioreductive agent tirapazamine and its major metabolites in mouse and human plasma for pharmacokinetically guided dose escalati

scholarly article by Hernani Robin Jr. et al published 1 May 1995 in Cancer Chemotherapy and Pharmacology

Discovering and Developing PI3 Kinase Inhibitors for Cancer: Rapid Progress through Academic-Biotech-Pharma Interactions ⬇️

scientific article published on November 1, 2011

Discovery and development of pyrazole-scaffold Hsp90 inhibitors

scientific article published on January 2006

Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19

scientific article

Discovery of small molecule cancer drugs: Successes, challenges and opportunities ⬇️

scientific article published on 03 March 2012

Disruption of WT1 gene expression and exon 5 splicing following cytotoxic drug treatment: antisense down-regulation of exon 5 alters target gene expression and inhibits cell survival

scientific article

Distinctive Behaviors of Druggable Proteins in Cellular Networks

scientific article (publication date: December 2015)

Drug discovery in advanced prostate cancer: translating biology into therapy

scientific article published on 22 July 2016

Drugging PI3K in cancer: refining targets and therapeutic strategies

scientific article published on 25 June 2015

Drugging cancer genomes

scientific article published in December 2013

Drugging the PI3 kinome

scientific article published in July 2006

Drugging the cancer chaperone HSP90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress

scientific article

Drugging the heat shock factor 1 pathway: exploitation of the critical cancer cell dependence on the guardian of the proteome.

scientific article

Dual targeting of HSC70 and HSP72 inhibits HSP90 function and induces tumor-specific apoptosis

scientific article published on September 2008

E3 ubiquitin ligase Cullin-5 modulates multiple molecular and cellular responses to heat shock protein 90 inhibition in human cancer cells

scientific article

EGFRvIII deletion mutations in pediatric high-grade glioma and response to targeted therapy in pediatric glioma cell lines

scientific article published on 08 September 2009

EML4-ALK fusions: propelling cancer but creating exploitable chaperone dependence

scientific article published in June 2014

Envisioning the future of early anticancer drug development

scientific article published on 10 June 2010

ErbB2 overexpression in an ovarian cancer cell line confers sensitivity to the HSP90 inhibitor geldanamycin

scientific article published on July 2002

Erratum: Corrigendum: ATP-competitive inhibitors block protein kinase recruitment to the Hsp90-Cdc37 system

scholarly article published in Nature Chemical Biology

Erratum: Corrigendum: The promise and peril of chemical probes

scientific article published in November 2015

Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line.

scientific article

Exploiting Protein Conformational Change to Optimize Adenosine-Derived Inhibitors of HSP70.

scientific article

Exploiting the Cancer Genome: Strategies for the Discovery and Clinical Development of Targeted Molecular Therapeutics ⬇️

scientific article published on January 1, 2012

Exploiting tumor metabolism for non-invasive imaging of the therapeutic activity of molecularly targeted anticancer agents ⬇️

scientific article published on September 1, 2011

Expression of kinase-defective mutants of c-Src in human metastatic colon cancer cells decreases Bcl-xL and increases oxaliplatin- and Fas-induced apoptosis

scientific article

Finding the needle in the haystack: why high-throughput screening is good for your health

scientific article

Fused imidazoles as potential chemical scaffolds for inhibition of heat shock protein 70 and induction of apoptosis. Synthesis and biological evaluation of phenanthro[9,10-d]imidazoles and imidazo[4,5-f][1,10]phenanthrolines

scientific article published on April 2016

Gene expression microarray technologies in the development of new therapeutic agents

scientific article

Gene expression profiling after radiation-induced DNA damage is strongly predictive of BRCA1 mutation carrier status

scientific article published on February 2004

Genes and Proteins Governing the Cellular Sensitivity to HSP90 Inhibitors: A Mechanistic Perspective ⬇️

scientific article published on October 1, 2003

Genome-based cancer therapeutics: targets, kinase drug resistance and future strategies for precision oncology

scientific article published on 28 June 2013

HER3 Is an Actionable Target in Advanced Prostate Cancer

scientific article published on 09 November 2021

HSF1 in Translation

scientific article published in August 2013

HSP90 as a new therapeutic target for cancer therapy: the story unfolds

scientific article

HSP90 inhibition: two-pronged exploitation of cancer dependencies ⬇️

scientific article published on December 30, 2011

Heat shock protein inhibition is associated with activation of the unfolded protein response pathway in myeloma plasma cells

scientific article published on 24 May 2007

High-throughput screening assay for identification of small molecule inhibitors of Aurora2/STK15 kinase

scientific article

High-throughput screening assay for inhibitors of heat-shock protein 90 ATPase activity

scientific article published in April 2004

High-throughput screening for the identification of small-molecule inhibitors of retinoblastoma protein phosphorylation in cells

scientific article published in September 2003

Histone Deacetylase Inhibition Increases Levels of Choline Kinase α and Phosphocholine Facilitating Noninvasive Imaging in Human Cancers ⬇️

scientific article published on December 22, 2011

Histone H3.3. mutations drive pediatric glioblastoma through upregulation of MYCN.

scientific article published on May 2013

Histone modification enzymes: novel targets for cancer drugs

scientific article

Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases

scientific article published on 22 October 2007

How Much Longer Will We Put Up With $100,000 Cancer Drugs?

scientific article published in February 2017

How much gets there and what does it do?: The need for better pharmacokinetic and pharmacodynamic endpoints in contemporary drug discovery and development

scientific article

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet? ⬇️

scientific article published on January 1, 2012

Identification by High-Throughput Screening of Viridin Analogs as Biochemical and Cell-Based Inhibitors of the Cell Cycle–Regulated Nek2 Kinase ⬇️

scientific article published on July 27, 2010

Identification of 4-(4-aminopiperidin-1-yl)-7H-pyrrolo[2,3-d]pyrimidines as selective inhibitors of protein kinase B through fragment elaboration

scientific article

Identification of Novel Keratinocyte Differentiation Modulating Compounds by High-Throughput Screening

Identification of inhibitors of the kinase activity of oncogenic V600E BRAF in an enzyme cascade high-throughput screen

scientific article published on 16 December 2005

Identification of magnetic resonance detectable metabolic changes associated with inhibition of phosphoinositide 3-kinase signaling in human breast cancer cells

scientific article published in January 2006

Identification of novel small molecule inhibitors of hypoxia-inducible factor-1 that differentially block hypoxia-inducible factor-1 activity and hypoxia-inducible factor-1alpha induction in response to hypoxic stress and growth factors

scientific article published on June 2005

Imaging biomarker roadmap for cancer studies ⬇️

scientific article

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate

scientific article

In vitro Biological Characterization of a Novel, Synthetic Diaryl Pyrazole Resorcinol Class of Heat Shock Protein 90 Inhibitors

In vitro nuclear magnetic resonance spectroscopy metabolic biomarkers for the combination of temozolomide with PI3K inhibition in paediatric glioblastoma cells

scientific article published on 13 July 2017

In vivo biological activity of the histone deacetylase inhibitor LAQ824 is detectable with 3'-deoxy-3'-[18F]fluorothymidine positron emission tomography.

scientific article

Inhibiting the molecular evolution of cancer through HSP90 ⬇️

scientific article published on October 1, 2012

Inhibition of Hsp90 with resorcylic acid macrolactones: synthesis and binding studies

scientific article

Inhibition of Hsp90 with synthetic macrolactones: synthesis and structural and biological evaluation of ring and conformational analogs of radicicol

scientific article published on November 2006

Inhibitors of cyclin-dependent kinases as cancer therapeutics

scientific article published on 4 February 2017

Inhibitors of the HSP90 molecular chaperone: attacking the master regulator in cancer

scientific article published on January 2006

Inhibitors of the HSP90 molecular chaperone: current status

scientific article published on January 2006

Inhibitors of the heat shock response: biology and pharmacology

scientific article published on 25 May 2007

Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity

scientific article published on October 2005

Lactate and choline metabolites detected in vitro by nuclear magnetic resonance spectroscopy are potential metabolic biomarkers for PI3K inhibition in pediatric glioblastoma

scientific article

MEK1/2 inhibition decreases lactate in BRAF-driven human cancer cells

scientific article published on 2 May 2013

MGMT-independent temozolomide resistance in pediatric glioblastoma cells associated with a PI3-kinase-mediated HOX/stem cell gene signature

scientific article published on 8 October 2010

Magnetic resonance spectroscopic pharmacodynamic markers of the heat shock protein 90 inhibitor 17-allylamino,17-demethoxygeldanamycin (17AAG) in human colon cancer models

scientific article published in November 2003

Magnetic resonance spectroscopy monitoring of mitogen-activated protein kinase signaling inhibition

scientific article

Maximizing the Therapeutic Potential of HSP90 Inhibitors

scientific article (publication date: November 2015)

Mechanism of action of the Aurora kinase inhibitor CCT129202 and in vivo quantification of biological activity

scientific article published on December 2007

Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling

scientific article

Mechanistic evaluation of the novel HSP90 inhibitor NVP-AUY922 in adult and pediatric glioblastoma

scientific article

Metabolism and pharmacokinetics of the cyclin-dependent kinase inhibitor R-roscovitine in the mouse

scientific article published in January 2005

Minimally invasive pharmacokinetic and pharmacodynamic technologies in hypothesis-testing clinical trials of innovative therapies

scientific article

Minimizing bias in target selection by exploiting multidisciplinary Big Data and the protein interactome

scientific article

Mode of cell death induced by the HSP90 inhibitor 17-AAG (tanespimycin) is dependent on the expression of pro-apoptotic BAX.

scientific article published on November 2013

Modulation of Plasma Metabolite Biomarkers of the MAPK Pathway with MEK Inhibitor RO4987655: Pharmacodynamic and Predictive Potential in Metastatic Melanoma

scientific article published on 21 June 2017

Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition

scientific article

Molecular and phenotypic characterisation of paediatric glioma cell lines as models for preclinical drug development

scientific article

Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma

scientific article

Molecular profiling and combinatorial activity of CCT068127: a potent CDK2 and CDK9 inhibitor

scientific article

Multiparametric analysis of cell membrane permeability by two colour flow cytometry with complementary fluorescent probes

article

NVP-AUY922: a novel heat shock protein 90 inhibitor active against xenograft tumor growth, angiogenesis, and metastasis

scientific article

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

scientific article

New approaches to molecular cancer therapeutics

scientific article published on December 2006

New cancer drugs on the horizon

scientific article

Niacin induces PPARgamma expression and transcriptional activation in macrophages via HM74 and HM74a-mediated induction of prostaglandin synthesis pathways

scientific article (publication date: 28 February 2006)

Noninvasive imaging of cell proliferation following mitogenic extracellular kinase inhibition by PD0325901.

scientific article published on September 2008

Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of a novel histone deacetylase inhibitor, LAQ824, in human colon carcinoma cells and xenografts

scientific article published on April 2008

Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of the choline kinase inhibitor MN58b in human carcinoma models

scientific article published in January 2006

Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design

scientific article published in June 2005

Objective assessment of cancer genes for drug discovery

article

Objective, Quantitative, Data-Driven Assessment of Chemical Probes

scientific article

Opportunities and challenges in ovarian cancer research, a perspective from the 11th Ovarian cancer action/HHMT Forum, Lake Como, March 2007.

scientific article published on 21 December 2007

Optimization of Imidazo[4,5- b ]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

scientific article

Overview: Translating Hsp90 Biology into Hsp90 Drugs ⬇️

scientific article published on October 1, 2003

PI(3) kinases: revealing the delta lady.

scientific article published in February 2010

PI3 Kinase in Cancer: From Biology to Clinic

scientific article published on January 2012

Patient-derived organoids model treatment response of metastatic gastrointestinal cancers.

scientific article

Paul Workman on the challenges of cancer drug development. Interview by Katharine E. Pestell

scientific article published in September 2003

Pediatric and adult glioblastoma radiosensitization induced by PI3K/mTOR inhibition causes early metabolic alterations detected by nuclear magnetic resonance spectroscopy

scientific article published on 24 May 2017

Personalized medicine: patient-predictive panel power

scientific article

Pharmacodynamic and Clinical Results from a Phase I/II Study of the HSP90 Inhibitor Onalespib in Combination with Abiraterone Acetate in Prostate Cancer

scientific article published on 21 May 2019

Pharmacodynamic biomarkers for molecular cancer therapeutics

scientific article

Pharmacokinetic-pharmacodynamic relationships for the heat shock protein 90 molecular chaperone inhibitor 17-allylamino, 17-demethoxygeldanamycin in human ovarian cancer xenograft models

scientific article

Phase I pharmacokinetic and pharmacodynamic study of 17-allylamino, 17-demethoxygeldanamycin in patients with advanced malignancies

scientific article published in June 2005

Phase I pharmacokinetic and pharmacodynamic study of LAQ824, a hydroxamate histone deacetylase inhibitor with a heat shock protein-90 inhibitory profile, in patients with advanced solid tumors

scientific article published on October 2008

Phase I safety, pharmacokinetic, and pharmacogenomic trial of ES-285, a novel marine cytotoxic agent, administered to adult patients with advanced solid tumors

scientific article

Polypharmacology in Precision Oncology: Current Applications and Future Prospects

scientific article

Potentiation of paclitaxel activity by the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin in human ovarian carcinoma cell lines with high levels of activated AKT.

scientific article published on May 2006

Preclinical Pharmacology, Antitumor Activity, and Development of Pharmacodynamic Markers for the Novel, Potent AKT Inhibitor CCT128930 ⬇️

scientific article published on December 29, 2010

Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements

scientific article

Probing the probes: fitness factors for small molecule tools

scientific article

Public resources for chemical probes: the journey so far and the road ahead

scientific article published on 28 November 2019

Q&A: Paul Workman on Big Data and Large Biases ⬇️

scientific article published on March 28, 2013

RNAi screen reveals synthetic lethality between cyclin G-associated kinase and FBXW7 by inducing aberrant mitoses

scientific article

Role for amplification and expression of glypican-5 in rhabdomyosarcoma

scientific article

Sensitization of (colon) cancer cells to death receptor related therapies: a report from the FP6-ONCODEATH research consortium

scientific article published on May 2012

Sequencing of prostate cancers identifies new cancer genes, routes of progression and drug targets

scientific article published on 16 April 2018

Services provided by community pharmacies in Wayne County, Michigan: a comparison by ZIP code characteristics

scientific article published in November 2014

Shock about heat shock in cancer ⬇️

scientific article published on August 1, 2012

SiGNet: A signaling network data simulator to enable signaling network inference

scientific article

Signalling involving MET and FAK supports cell division independent of the activity of the cell cycle-regulating CDK4/6 kinases

scientific article published on 12 July 2019

Silencing of HSP90 cochaperone AHA1 expression decreases client protein activation and increases cellular sensitivity to the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin

scientific article published on February 2008

Small-Molecule Inhibitors of the Protein Methyltransferase SET7/9 Identified in a High-Throughput Screen ⬇️

scientific article published on July 5, 2012

Solid-phase immunoassays in mechanism-based drug discovery: their application in the development of inhibitors of the molecular chaperone heat-shock protein 90.

scientific article published in June 2005

Strategies for treating cancers caused by multiple genome abnormalities: from concepts to cures?

scientific article published on December 2003

Structural and functional characterisation of human RNA helicase DHX8 provides insights into the mechanism of RNA-stimulated ADP release

scientific article published on 13 September 2019

Structural basis of the radicicol resistance displayed by a fungal hsp90

scientific article

Structure-activity relationships in purine-based inhibitor binding to HSP90 isoforms

scientific article

Structure-based design of isoquinoline-5-sulfonamide inhibitors of protein kinase B.

scientific article published on 24 October 2005

Structure-based design of molecular cancer therapeutics

scientific article published on 30 March 2009

Structure-based drug design: aiming for a perfect fit.

scientific article published on 8 November 2017

Synthesis and biological evaluation of 4-morpholino-2-phenylquinazolines and related derivatives as novel PI3 kinase p110alpha inhibitors

scientific article published on 11 July 2006

Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors

scientific article

Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors

scientific article

Synthesis of isothiazol-3-one derivatives as inhibitors of histone acetyltransferases (HATs).

scientific article

Targeting CDC37: an alternative, kinase-directed strategy for disruption of oncogenic chaperoning

scientific article

Targeting of multiple signalling pathways by heat shock protein 90 molecular chaperone inhibitors

scientific article published on December 2006

Targeting the Hsp90 chaperone: synthesis of novel resorcylic acid macrolactone inhibitors of Hsp90.

scientific article published in March 2010

Targeting the Hsp90 molecular chaperone with novel macrolactams. Synthesis, structural, binding, and cellular studies

scientific article

Targeting the PI3K-AKT-mTOR pathway: progress, pitfalls, and promises

scientific article published on 27 August 2008

The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate-Lactate Exchange in BRAF-Mutant Human Melanoma Cells

scientific article published on 07 October 2016

The Clinical Applications of Heat Shock Protein Inhibitors in Cancer - Present and Future ⬇️

scientific article published on October 1, 2003

The Cyclin-dependent kinase inhibitor CYC202 (R-roscovitine) inhibits retinoblastoma protein phosphorylation, causes loss of Cyclin D1, and activates the mitogen-activated protein kinase pathway

scientific article published on January 2004

The HSP90 Inhibitor NVP-AUY922 Radiosensitizes by Abrogation of Homologous Recombination Resulting in Mitotic Entry with Unresolved DNA Damage ⬇️

scientific article published on April 16, 2012

The Hsp90 molecular chaperone: an open and shut case for treatment

scientific article

The application of cassette dosing for pharmacokinetic screening in small-molecule cancer drug discovery

scientific article published on February 2007

The contemporary drug development process: advances and challenges in preclinical and clinical development

scientific article published on January 1, 2003

The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis

scientific article published on 5 October 2007

The expanding proteome of the molecular chaperone HSP90.

scientific article published on April 2012

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer

scientific article

The identification of novel PLC-gamma inhibitors using virtual high throughput screening

scientific article published on 3 March 2009

The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors

scientific article published on July 2005

The kinase polypharmacology landscape of clinical PARP inhibitors

scientific article published on 17 February 2020

The off-target kinase landscape of clinical PARP inhibitors

The opportunities and challenges of personalized genome-based molecular therapies for cancer: targets, technologies, and molecular chaperones

scientific article

The role of high expectations of self and social desirability in emotional processing in individuals with irritable bowel syndrome: A qualitative study

scientific article published on September 2017

Transforming cancer drug discovery with Big Data and AI

scientific article published on 08 July 2019

Translating basic cancer research into new cancer therapeutics

scientific article

Unpicking the combination lock for mutant BRAF and RAS melanomas.

scientific article

Using biomarkers in drug development.

scientific article published on October 2006

Validation of liquid chromatography assay for the quantitation of (Z)-3-[2,4-dimethyl-5-(2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-1H-pyrrol-3-yl]propionic acid (SU006668) in human plasma and its application to a phase I clinical trial

scientific article published in February 2003

Validation of the fluorinated 2-nitroimidazole SR-4554 as a noninvasive hypoxia marker detected by magnetic resonance spectroscopy

scientific article

Wnt signalling modulates transcribed-ultraconserved regions in hepatobiliary cancers

scientific article published on 12 September 2016

canSAR: update to the cancer translational research and drug discovery knowledgebase

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