S. Sharp

发表

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

X. Barril, M. Drysdale, P. Workman, 2004, Chemistry & biology.

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.

X. Barril, B. Davis, M. Drysdale, 2009, Journal of medicinal chemistry.

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

Mike Wood, Brian Dymock, Xavier Barril, 2007, Journal of medicinal chemistry.

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

L. Pearl, X. Barril, M. Drysdale, 2008, Cancer research.

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

L. Pearl, P. Workman, W. Aherne, 2011, ACS chemical biology.

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

G. Vassal, Chris Jones, P. Workman, 2009, Cancer research.

DT-Diaphorase expression and tumor cell sensitivity to 17-allylamino, 17-demethoxygeldanamycin, an inhibitor of heat shock protein 90.

T G Myers, T. Myers, P. Workman, 1999, Journal of the National Cancer Institute.

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

Paul Workman, Edward McDonald, Chrisostomos Prodromou, 2005, Bioorganic & medicinal chemistry letters.

Gene and protein expression profiling of human ovarian cancer cells treated with the heat shock protein 90 inhibitor 17-allylamino-17-demethoxygeldanamycin.

Paul Workman, Rainer Cramer, Marketa Zvelebil, 2007, Cancer research.

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

Nathan Brown, Julian Blagg, Paul Workman, 2018, Molecular oncology.

Cancer esearch apeutics , Targets , and Chemical Biology MT-Independent Temozolomide Resistance in Pediatric blastoma Cells Associated with a PI 3-Kinase – Mediated R / Stem Cell Gene Signature

D. Bax, G. Vassal, Chris Jones, 2010 .

/ Stem Cell Gene Signature HOX Mediated − Glioblastoma Cells Associated with a PI 3-Kinase MGMT-Independent Temozolomide Resistance in Pediatric

D. Bax, G. Vassal, Chris Jones, 2010 .

Mini-review: discovery and development of platinum complexes designed to circumvent cisplatin resistance.

P. Beale, I. Judson, C. O'Neill, 1999, Journal of inorganic biochemistry.

The association of CCND1 overexpression and cisplatin resistance in testicular germ cell tumors and other cancers.

D. Berney, Yong-jie Lu, T. Powles, 2010, The American journal of pathology.

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

P. Workman, I. Judson, M. Walton, 2008, Cancer Chemotherapy and Pharmacology.

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

P. Workman, K. Boxall, P. Clarke, 2005, Assay and drug development technologies.

Transport of cisplatin and bis-acetato-ammine-dichlorocyclohexylamine Platinum(IV) (JM216) in human ovarian carcinoma cell lines: identification of a plasma membrane protein associated with cisplatin resistance.

L. Kèlland, P. Rogers, S. Sharp, 1995, Clinical cancer research : an official journal of the American Association for Cancer Research.

Solution structure of the Hop TPR2A domain and investigation of target druggability by NMR, biochemical and in silico approaches

B. Al-Lazikani, L. Pearl, P. Simpson, 2020, Scientific Reports.

Lack of a role for MRP1 in platinum drug resistance in human ovarian cancer cell lines.

L. Kèlland, S. Sharp, S. Hobbs, 1998, British Journal of Cancer.

Synthetic ansamycins prepared by a ring-expanding Claisen rearrangement. Synthesis and biological evaluation of ring and conformational analogues of the Hsp90 molecular chaperone inhibitor geldanamycin.

A. Slawin, P. Workman, K. Boxall, 2007, Organic & biomolecular chemistry.

Molecular profiling and combinatorial activity of CCT068127

M. Noble, P. Workman, S. Whittaker, 2017 .

Retention of activity by the new generation platinum agent AMD0473 in four human tumour cell lines possessing acquired resistance to oxaliplatin.

C. O'Neill, L. Kèlland, P. Rogers, 2002, European Journal of Cancer.

Mechanisms of drug resistance to the platinum complex ZD0473 in ovarian cancer cell lines.

P. Beale, L. Kèlland, S. Sharp, 2000, European journal of cancer.

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

L. Pearl, P. Workman, W. Aherne, 2010, Chemistry.

Effects of a new antioestrogen, idoxifene, on cisplatin- and doxorubicin-sensitive and -resistant human ovarian carcinoma cell lines.

L. Kèlland, M. Rowlands, S. Sharp, 1994, British Journal of Cancer.

Selective potentiation of platinum drug cytotoxicity in cisplatin-sensitive and-resistant human ovarian carcinoma cell lines by amphotericin B

L. Kèlland, M. Valenti, S. Sharp, 2004, Cancer Chemotherapy and Pharmacology.

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

Paul Workman, Chrisostomos Prodromou, Laurence H Pearl, 2006, Chemistry & biology.

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.

P. Workman, M. Stevens, W. Lewis, 2016, Organic & biomolecular chemistry.

In vitro circumvention of cisplatin resistance by the novel sterically hindered platinum complex AMD473.

L. Kèlland, M. Abrams, B. Murrer, 1998, British Journal of Cancer.

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

P. Workman, W. Aherne, M. Rowlands, 2010, Chemistry.

Discovery of a Chemical Probe Bisamide (CCT251236): An Orally Bioavailable Efficacious Pirin Ligand from a Heat Shock Transcription Factor 1 (HSF1) Phenotypic Screen

R. V. van Montfort, P. Workman, R. T. te Poele, 2016, Journal of medicinal chemistry.

Exploiting Cancer Dependence on Molecular Chaperones: HSP90 Inhibitors Past, Present, and Future

P. Workman, Keith Jones, S. Sharp, 2014 .

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

G. Morgan, P. Workman, F. Davies, 2007, Blood.

HSP90 inhibitors: targeting the cancer chaperone for combinatorial blockade of oncogenic pathways

P. Workman, S. Sharp, K. Jones, 2008 .

DRUGGING THE HSP90 MOLECULAR CHAPERONE MACHINE FOR CANCER TREATMENT

P. Workman, S. Sharp, J. Holmes, 2007 .

Second-Generation HSP90 Inhibitor Onalespib Blocks mRNA Splicing of Androgen Receptor Variant 7 in Prostate Cancer Cells.

S. Plymate, P. Workman, J. Lyons, 2016, Cancer research.

HSP90 inhibition: two-pronged exploitation of cancer dependencies.

Paul Workman, Jon Travers, P. Workman, 2012, Drug discovery today.

A molecular cytogenetic approach to studying platinum resistance.

B. Leyland-Jones, M. Seckl, L. Hiorns, 1999, Journal of inorganic biochemistry.

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

R. Reis, D. Bax, G. Vassal, 2010, Cancer research.

Inhibitors of the HSP90 molecular chaperone: current status.

Paul Workman, P. Workman, S. Sharp, 2006, Advances in cancer research.

EGFRvIII Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines

Paul Workman, Jorge S. Reis-Filho, Darren Hargrave, 2009, Clinical Cancer Research.

Targeting Hsp90: The Cancer Super-Chaperone

P. Workman, S. Sharp, 2007 .

In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors.

L. Pearl, P. Workman, R. Marais, 2007, Cancer research.

BCL-2 family protein expression and platinum drug resistance in ovarian carcinoma

P. Beale, L. Kèlland, P. Rogers, 2000, British Journal of Cancer.

Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines

J. Reis-Filho, S. Al-Sarraj, R. Reis, 2009 .

Targeting heat shock protein 72 enhances Hsp90 inhibitor-induced apoptosis in myeloma

G. Morgan, P. Workman, D. Gonzalez, 2010, Leukemia.

Mechanistic Evaluation of the Novel HSP90 Inhibitor NVP-AUY922 in Adult and Pediatric Glioblastoma

G. Vassal, Chris Jones, P. Workman, 2010, Molecular Cancer Therapeutics.

Establishment of an isogenic human colon tumor model for NQO1 gene expression: application to investigate the role of DT-diaphorase in bioreductive drug activation in vitro and in vivo.

P. Workman, L. Kèlland, M. Valenti, 2000, Molecular pharmacology.

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

P. Workman, P. Clarke, J. Caldwell, 2017, Journal of medicinal chemistry.

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

P. Workman, S. Sharp, S. Hobbs, 2008, Cancer research.

Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues

L. Pearl, X. Barril, M. Drysdale, 2007, Molecular Cancer Therapeutics.

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

M. Leach, P. Workman, S. Sharp, 2010, Oncotarget.

Effects of HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin (17-AAG) on NEU/HER2 overexpressing mammary tumours in MMTV-NEU-NT mice monitored by Magnetic Resonance Spectroscopy

J. Griffiths, M. Leach, P. Workman, 2012, BMC Research Notes.

Discovery and validation of biomarkers to support clinical development of NXP800: A first-in-class orally active, small-molecule HSF1 pathway inhibitor

P. Workman, P. Clarke, M. Valenti, 2022, European Journal of Cancer.

Abstract 2433:In vitroandin vivoantitumor activity of the next generation HSP90 inhibitor, AT13387, in both hormone-sensitive and castration-resistant prostate cancer models.

P. Workman, J. Lyons, S. Eccles, 2013 .

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

P. Workman, S. Roe, C. Prodromou, 2012, PloS one.

HSF1 Pathway Inhibitor Clinical Candidate (CCT361814/NXP800) Developed from a Phenotypic Screen as a Potential Treatment for Refractory Ovarian Cancer and Other Malignancies

P. Workman, P. Clarke, Alan T. Henley, 2023, Journal of medicinal chemistry.

The association of CCND1 overexpression and cisplatin resistance in testicular germ cell tumors and other cancers.

D. Berney, T. Powles, A. McIntyre, 2010, The American journal of pathology.

Discovery of 4,6-disubstituted pyrimidines as potent inhibitors of the heat shock factor 1 (HSF1) stress pathway and CDK9

Alan T. Henley, A. Hayes, S. Sharp, 2016, MedChemComm.

EGFRvIII Deletion Mutations in Pediatric High-Grade Glioma and Response to Targeted Therapy in Pediatric Glioma Cell Lines

J. Reis-Filho, S. Al-Sarraj, R. Reis, 2009, Clinical Cancer Research.

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

P. Workman, W. Aherne, F. Raynaud, 2011, ACS chemical biology.