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Lista de obras de Paul Workman

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

artículo científico publicado en 2005

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

artículo científico publicado en 2008

4-Amino derivatives of the Hsp90 inhibitor CCT018159.

artículo científico publicado en 2006

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

artículo científico publicado en 2011

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

artículo científico publicado en 2010

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

artículo científico publicado en 2016

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

artículo científico publicado en 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 ⬇️

artículo científico publicado el 1 de noviembre de 2003

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

artículo científico publicado en 2011

A public-private partnership to unlock the untargeted kinome

artículo científico publicado en 2013

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

artículo científico publicado en 2008

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

artículo científico publicado el 1 de abril de 2011

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

artículo científico publicado en 2007

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

artículo científico publicado en 2010

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

artículo científico publicado en 2012

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

artículo científico publicado en 2010

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

artículo científico publicado en 2013

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

artículo científico publicado en 2005

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

artículo científico publicado en 2002

Altered states: selectively drugging the Hsp90 cancer chaperone

artículo científico publicado en 2004

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

artículo científico publicado en 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

artículo científico publicado en 2008

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

artículo científico publicado en 2007

Assays for HSP90 and inhibitors.

artículo científico publicado en 2003

Assays for the identification and evaluation of histone acetyltransferase inhibitors

artículo científico publicado en 2002

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

artículo científico publicado en 2016

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

artículo científico publicado en 2003

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

artículo científico publicado en 2013

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

artículo científico publicado en 2008

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

artículo científico publicado en 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

artículo científico publicado en 2009

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

artículo científico publicado en 2009

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

artículo científico publicado en 2016

Bioreductive prodrugs for cancer therapy

artículo científico publicado en 2004

Blocking the survival of the nastiest by HSP90 inhibition

artículo científico publicado en 2016

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

artículo científico publicado en 2020

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

artículo científico publicado en 2009

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

artículo científico publicado en 2002

Cancer: drug-tolerant insurgents

artículo científico publicado en 2010

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

artículo científico publicado en 2004

Chemical biology approaches to target validation in cancer

artículo científico

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

artículo científico publicado en 2017

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

artículo científico publicado en 2012

Combinatorial attack on multistep oncogenesis by inhibiting the Hsp90 molecular chaperone

artículo científico publicado en 2004

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

artículo científico publicado en 2012

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

artículo científico publicado en 2009

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

artículo científico publicado en 2013

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

artículo científico publicado en 2020

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

artículo científico publicado en 2011

Critical parameters in targeted drug development: the pharmacological audit trail

artículo científico publicado en 2016

Death by chaperone: HSP90, HSP70 or both?

artículo científico publicado en 2009

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

artículo científico publicado en 2017

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

artículo científico publicado en 2011

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

artículo científico publicado en 2009

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 ⬇️

artículo científico publicado el 1 de noviembre de 2011

Discovery and development of pyrazole-scaffold Hsp90 inhibitors

artículo científico publicado en 2006

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

artículo científico publicado en 2016

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

artículo científico publicado el 3 de marzo de 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

artículo científico publicado en 2004

Distinctive Behaviors of Druggable Proteins in Cellular Networks

artículo científico publicado en 2015

Drug discovery in advanced prostate cancer: translating biology into therapy

artículo científico publicado en 2016

Drugging PI3K in cancer: refining targets and therapeutic strategies

artículo científico

Drugging cancer genomes

artículo científico publicado en 2013

Drugging the PI3 kinome

artículo científico publicado en 2006

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

artículo científico publicado en 2007

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

artículo científico publicado en 2009

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

artículo científico publicado en 2008

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

artículo científico publicado en 2014

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

artículo científico

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

artículo científico publicado en 2014

Envisioning the future of early anticancer drug development

artículo científico publicado en 2010

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

artículo científico publicado en 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

artículo científico publicado en 2015

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

artículo científico publicado en 2002

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

artículo científico publicado en 2016

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

artículo científico publicado el 1 de enero de 2012

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

artículo científico publicado el 1 de septiembre de 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

artículo científico publicado en 2004

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

artículo científico publicado en 2002

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

artículo científico publicado en 2016

Gene expression microarray technologies in the development of new therapeutic agents

artículo científico publicado en 2004

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

artículo científico publicado en 2004

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

artículo científico publicado el 1 de octubre de 2003

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

artículo científico

HER3 Is an Actionable Target in Advanced Prostate Cancer

artículo científico publicado en 2021

HSF1 in Translation

artículo científico publicado en 2013

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

artículo científico publicado en 2002

HSP90 inhibition: two-pronged exploitation of cancer dependencies ⬇️

artículo científico publicado el 30 de diciembre de 2011

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

artículo científico publicado en 2007

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

artículo científico publicado en 2004

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

artículo científico publicado en 2004

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

artículo científico publicado en 2003

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

artículo científico publicado el 22 de diciembre de 2011

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

artículo científico publicado en 2013

Histone modification enzymes: novel targets for cancer drugs

artículo científico publicado en 2004

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

artículo científico publicado en 2007

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

artículo científico publicado en 2017

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

artículo científico publicado en 2003

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet? ⬇️

artículo científico publicado el 1 de enero de 2012

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

artículo científico publicado el 27 de julio de 2010

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

artículo científico publicado en 2008

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

artículo científico publicado en 2005

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

artículo científico publicado en 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

artículo científico publicado en 2005

Imaging biomarker roadmap for cancer studies ⬇️

artículo científico publicado en 2016

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

artículo científico publicado en 2010

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

artículo científico

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

artículo científico publicado en 2006

Inhibiting the molecular evolution of cancer through HSP90 ⬇️

artículo científico publicado el 1 de octubre de 2012

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

artículo científico publicado en 2010

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

artículo científico publicado en 2006

Inhibitors of cyclin-dependent kinases as cancer therapeutics

artículo científico publicado en 2017

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

artículo científico publicado en 2006

Inhibitors of the HSP90 molecular chaperone: current status

artículo científico publicado en 2006

Inhibitors of the heat shock response: biology and pharmacology

artículo científico publicado en 2007

Isothiazolones as inhibitors of PCAF and p300 histone acetyltransferase activity

artículo científico publicado en 2005

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

artículo científico publicado en 2014

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

artículo científico publicado en 2013

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

artículo científico publicado en 2010

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

artículo científico publicado en 2003

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

artículo científico publicado en 2005

Maximizing the Therapeutic Potential of HSP90 Inhibitors

artículo científico publicado en 2015

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

artículo científico publicado en 2007

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

artículo científico publicado en 2012

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

artículo científico publicado en 2010

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

artículo científico publicado en 2005

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

artículo científico publicado en 2006

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

artículo científico publicado en 2016

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

artículo científico publicado en 2013

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

artículo científico publicado en 2017

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

artículo científico publicado en 2010

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

artículo científico publicado en 2009

Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma

artículo científico publicado en 2009

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

artículo científico publicado en 2018

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

artículo científico publicado en 2008

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

artículo científico publicado en 2015

New approaches to molecular cancer therapeutics

artículo científico publicado en 2006

New cancer drugs on the horizon

artículo científico publicado en 2005

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

artículo científico publicado en 2006

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

artículo científico publicado en 2008

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

artículo científico publicado en 2008

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

artículo científico publicado en 2006

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

artículo científico publicado en 2005

Objective assessment of cancer genes for drug discovery

article

Objective, Quantitative, Data-Driven Assessment of Chemical Probes

artículo científico publicado en 2017

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

artículo científico publicado en 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

artículo científico publicado en 2012

Overview: Translating Hsp90 Biology into Hsp90 Drugs ⬇️

artículo científico publicado el 1 de octubre de 2003

PI(3) kinases: revealing the delta lady.

artículo científico publicado en 2010

PI3 Kinase in Cancer: From Biology to Clinic

artículo científico publicado en 2012

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

artículo científico publicado en 2018

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

artículo científico publicado en 2003

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

artículo científico publicado en 2017

Personalized medicine: patient-predictive panel power

artículo científico publicado en 2012

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

artículo científico publicado en 2019

Pharmacodynamic biomarkers for molecular cancer therapeutics

artículo científico publicado en 2006

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

artículo científico publicado en 2005

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

artículo científico publicado en 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

artículo científico publicado en 2008

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

artículo científico publicado en 2009

Polypharmacology in Precision Oncology: Current Applications and Future Prospects

artículo científico publicado en 2016

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

artículo científico publicado en 2006

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

artículo científico publicado el 29 de diciembre de 2010

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

artículo científico publicado en 2010

Probing the probes: fitness factors for small molecule tools

artículo científico publicado en 2010

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 ⬇️

artículo científico publicado el 28 de marzo de 2013

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

artículo científico publicado en 2017

Role for amplification and expression of glypican-5 in rhabdomyosarcoma

artículo científico publicado en 2007

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

artículo científico

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

artículo científico publicado en 2018

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

artículo científico publicado en 2014

Shock about heat shock in cancer ⬇️

artículo científico publicado el 1 de agosto de 2012

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

artículo científico publicado en 2017

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

artículo científico publicado en 2008

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

artículo científico publicado el 5 de julio de 2012

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

artículo científico publicado en 2005

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

artículo científico publicado en 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

artículo científico publicado en 2009

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

artículo científico publicado en 2004

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

artículo científico publicado en 2005

Structure-based design of molecular cancer therapeutics

artículo científico publicado en 2009

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

artículo científico publicado en 2017

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

artículo científico publicado en 2006

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

artículo científico publicado en 2006

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

artículo científico publicado en 2007

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

artículo científico publicado en 2008

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

artículo científico publicado en 2009

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

artículo científico publicado en 2006

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

artículo científico publicado en 2010

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

artículo científico publicado en 2011

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

artículo científico publicado en 2016

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

artículo científico publicado el 1 de octubre de 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

artículo científico publicado en 2004

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

artículo científico publicado el 16 de abril de 2012

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

artículo científico publicado en 2008

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

artículo científico publicado en 2007

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

artículo científico publicado el 1 de enero de 2003

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

artículo científico publicado en 2007

The expanding proteome of the molecular chaperone HSP90.

artículo científico publicado en 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

artículo científico publicado en 2008

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

artículo científico publicado en 2009

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

artículo científico publicado en 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

artículo científico publicado en 2003

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

artículo científico

Transforming cancer drug discovery with Big Data and AI

scientific article published on 08 July 2019

Translating basic cancer research into new cancer therapeutics

artículo científico publicado en 2002

Unpicking the combination lock for mutant BRAF and RAS melanomas.

artículo científico publicado en 2013

Using biomarkers in drug development.

artículo científico publicado en 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

artículo científico publicado en 2003

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

artículo científico publicado en 2002

Wnt signalling modulates transcribed-ultraconserved regions in hepatobiliary cancers

artículo científico publicado en 2016

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

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