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Review

Inhibitors of HSP90 and other chaperones for the treatment of cancer

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Pages 837-847 | Published online: 25 Feb 2005

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (4)

Tony Taldone, Hardik J Patel, Alexander Bolaender, Maulik R Patel & Gabriela Chiosis. (2014) Protein chaperones: a composition of matter review (2008 – 2013). Expert Opinion on Therapeutic Patents 24:5, pages 501-518.
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Ghassan Abu Sheikha, Mahmoud A. Al-Sha’er & Mutasem O. Taha. (2011) Some sulfonamide drugs inhibit ATPase activity of heat shock protein 90: investigation by docking simulation and experimental validation. Journal of Enzyme Inhibition and Medicinal Chemistry 26:5, pages 603-609.
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Jennifer S Isaacs. (2005) Heat-shock protein 90 inhibitors in antineoplastic therapy: is it all wrapped up?. Expert Opinion on Investigational Drugs 14:6, pages 569-589.
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P. Workman. (2004) Drug Discovery Strategies: Technologies to Accelerate Translation from Target to Drug. Journal of Chemotherapy 16:sup4, pages 13-15.
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Articles from other publishers (40)

Yiming Xu, Dewang Jing, Dong Zhao, Yongji Wu, Lu Xing, Haroon ur Rashid, Haodong Wang, Lisheng Wang & Huiling Cao. (2020) New modification strategy of matrine as Hsp90 inhibitors based on its specific L conformation for cancer treatment. Bioorganic & Medicinal Chemistry 28:4, pages 115305.
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Jianhua Liu, Yumei Wang, Hao Guo & Songjie Fan. (2019) DFT study of the solvation effect on an antiangiogenic deguelin analogue's structure and properties. Chemical Data Collections 20, pages 100185.
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Ludger A. Wessjohann, Richard Bartelt & Wolfgang Brandt. 2017. Practical Medicinal Chemistry with Macrocycles. Practical Medicinal Chemistry with Macrocycles 77 100 .
Xin Chen & Jian Jin. 2017. The Molecular Basis of Human Cancer. The Molecular Basis of Human Cancer 771 795 .
Shengquan Duan, Sripathy Venkatraman, Xuechuan Hong, Kenneth Huang, Luckner Ulysse, Bingidimi I. Mobele, Alexander Smith, Lawrence Lawless, Andrew Locke & Ravi Garigipati. (2012) Process Development and Scale-Up of an Hsp90 Inhibitor. Organic Process Research & Development 16:11, pages 1787-1793.
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Mahmoud A. Al-Sha’er & Mutasem O. Taha. (2012) Application of docking-based comparative intermolecular contacts analysis to validate Hsp90α docking studies and subsequent in silico screening for inhibitors. Journal of Molecular Modeling 18:11, pages 4843-4863.
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Kenneth H. Huang, Thomas E. Barta, John W. Rice, Emilie D. Smith, Andy J. Ommen, Wei Ma, James M. Veal, R. Patrick Fadden, Amy F. Barabasz, Briana E. Foley, Philip F. Hughes, Gunnar J. Hanson, Christopher J. Markworth, Melanie Silinski, Jeffrey M. Partridge, Paul M. Steed & Steven E. Hall. (2012) Discovery of novel aminoquinazolin-7-yl 6,7-dihydro-indol-4-ones as potent, selective inhibitors of heat shock protein 90. Bioorganic & Medicinal Chemistry Letters 22:7, pages 2550-2554.
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Marco A. Biamonte, Ryan Van de Water, Joseph W. Arndt, Robert H. Scannevin, Daniel Perret & Wen-Cherng Lee. (2009) Heat Shock Protein 90: Inhibitors in Clinical Trials. Journal of Medicinal Chemistry 53:1, pages 3-17.
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Paul A. BroughXavier BarrilJenifer BorgognoniPatrick Chene, Nicholas G. M. DaviesBen DavisMartin J. DrysdaleBrian DymockSuzanne A. EcclesCarlos Garcia-Echeverria, Christophe FromontAngela HayesRoderick E. HubbardAllan M. JordanMichael Rugaard Jensen, Andrew MasseyAngela MerrettAntony PadfieldRachel ParsonsThomas Radimerski, Florence I. RaynaudAlan RobertsonStephen D. RoughleyJoseph Schoepfer, Heather SimmoniteSwee Y. SharpAllan SurgenorMelanie ValentiSteven WallsPaul WebbMike WoodPaul WorkmanLisa Wright. (2009) 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 . Journal of Medicinal Chemistry 52:15, pages 4794-4809.
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Martin Spichty, Antoine Taly, Franz Hagn, Horst Kessler, Sofia Barluenga, Nicolas Winssinger & Martin Karplus. (2009) The HSP90 binding mode of a radicicol-like E-oxime determined by docking, binding free energy estimations, and NMR 15N chemical shifts. Biophysical Chemistry 143:3, pages 111-123.
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Kenneth H. Huang, James M. Veal, R. Patrick Fadden, John W. Rice, Jeron Eaves, Jon-Paul Strachan, Amy F. Barabasz, Briana E. Foley, Thomas E. Barta, Wei Ma, Melanie A. Silinski, Mei Hu, Jeffrey M. Partridge, Anisa Scott, Laura G. DuBois, Tiffany Freed, Paul M. Steed, Andy J. Ommen, Emilie D. Smith, Philip F. Hughes, Angela R. Woodward, Gunnar J. Hanson, W. Stephen McCall, Christopher J. Markworth, Lindsay Hinkley, Matthew Jenks, Lifeng Geng, Meredith Lewis, James Otto, Bert Pronk, Katleen Verleysen & Steven E. Hall. (2009) Discovery of Novel 2-Aminobenzamide Inhibitors of Heat Shock Protein 90 as Potent, Selective and Orally Active Antitumor Agents. Journal of Medicinal Chemistry 52:14, pages 4288-4305.
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Antonino Lauria, Mario Ippolito & Anna Maria Almerico. (2009) Inside the Hsp90 inhibitors binding mode through induced fit docking. Journal of Molecular Graphics and Modelling 27:6, pages 712-722.
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Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene, Vilma Michailoviene, Jolanta Torresan, Jelena Jachno & Daumantas Matulis. (2009) 5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone. Bioorganic & Medicinal Chemistry Letters 19:4, pages 1089-1092.
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Massimiliano Meli & Giorgio Colombo. 2009. Peptide Microarrays. Peptide Microarrays 77 153 .
C Garcia-Echeverria & W R Sellers. (2008) Drug discovery approaches targeting the PI3K/Akt pathway in cancer. Oncogene 27:41, pages 5511-5526.
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Xiaoguang Lei & Samuel J. Danishefsky. (2008) Efficient Synthesis of a Novel Resorcyclide as Anticancer Agent Based on Hsp90 Inhibition. Advanced Synthesis & Catalysis 350:11-12, pages 1677-1681.
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Jeffrey S. Johnston, Mitch A. Phelps, Kristie A. Blum, William Blum, Michael R. Grever, Katherine L. Farley & James T. Dalton. (2008) Development and validation of a rapid and sensitive high-performance liquid chromatography–mass spectroscopy assay for determination of 17-(allylamino)-17-demethoxygeldanamycin and 17-(amino)-17-demethoxygeldanamycin in human plasma. Journal of Chromatography B 871:1, pages 15-21.
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Thomas Hesterkamp & Mark Whittaker. (2008) Fragment-based activity space: smaller is better. Current Opinion in Chemical Biology 12:3, pages 260-268.
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Miriam Sgobba, Gianluca Degliesposti, Anna Maria Ferrari & Giulio Rastelli. (2008) Structural Models and Binding Site Prediction of the C-terminal Domain of Human Hsp90: A New Target for Anticancer Drugs. Chemical Biology & Drug Design 71:5, pages 420-433.
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Paul A. BroughWynne AherneXavier BarrilJenifer BorgognoniKathy BoxallJulie E. CansfieldKwai-Ming J. CheungIan CollinsNicholas G. M. DaviesMartin J. DrysdaleBrian DymockSuzanne A. EcclesHarry FinchAlexandra FinkAngela HayesRobert HowesRoderick E. HubbardKaren JamesAllan M. JordanAndrea LockieVanessa MartinsAndrew MasseyThomas P. MatthewsEdward McDonaldChristopher J. NorthfieldLaurence H. PearlChrisostomos ProdromouStuart RayFlorence I. RaynaudStephen D. RoughleySwee Y. SharpAllan SurgenorD. Lee WalmsleyPaul WebbMike WoodPaul WorkmanLisa Wright. (2007) 4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer. Journal of Medicinal Chemistry 51:2, pages 196-218.
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Srinivas R. Kasibhatla, Kevin Hong, Marco A. Biamonte, David J. Busch, Patricia L. Karjian, John L. Sensintaffar, Adeela Kamal, Rachel E. Lough, John Brekken, Karen Lundgren, Roy Grecko, Gregg A. Timony, Yingqing Ran, Robert Mansfield, Lawrence C. Fritz, Edgar Ulm, Francis J. Burrows & Marcus F. Boehm. (2007) Rationally Designed High-Affinity 2-Amino-6-halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity. Journal of Medicinal Chemistry 50:12, pages 2767-2778.
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Nicola F. Smith, Florence I. Raynaud & Paul Workman. (2007) The application of cassette dosing for pharmacokinetic screening in small-molecule cancer drug discovery. Molecular Cancer Therapeutics 6:2, pages 428-440.
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Carlos Garcia-Echeverria. 2007. Cancer. Cancer 169 206 .
Steven E. Hall. (2006) Chemoproteomics-driven drug discovery: addressing high attrition rates. Drug Discovery Today 11:11-12, pages 495-502.
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Nivedita Sain, Bhavani Krishnan, Michael G. Ormerod, Assunta De Rienzo, Wai M. Liu, Stanley B. Kaye, Paul Workman & Ann L. Jackman. (2006) Potentiation of paclitaxel activity by the HSP90 inhibitor 17-allylamino-17-demethoxygeldanamycin in human ovarian carcinoma cell lines with high levels of activated AKT. Molecular Cancer Therapeutics 5:5, pages 1197-1208.
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Swee Sharp & Paul Workman. 2006. 323 348 .
S. Pacey, U. Banerj, I. Judson & P. Workman. 2006. Molecular Chaperones in Health and Disease. Molecular Chaperones in Health and Disease 331 358 .
Yves L. Janin. (2005) Heat Shock Protein 90 Inhibitors. A Text Book Example of Medicinal Chemistry?. Journal of Medicinal Chemistry 48:24, pages 7503-7512.
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Xavier Barril, Paul Brough, Martin Drysdale, Roderick E. Hubbard, Andrew Massey, Allan Surgenor & Lisa Wright. (2005) Structure-based discovery of a new class of Hsp90 inhibitors. Bioorganic & Medicinal Chemistry Letters 15:23, pages 5187-5191.
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Paul A. Brough, Xavier Barril, Mandy Beswick, Brian W. Dymock, Martin J. Drysdale, Lisa Wright, Kate Grant, Andrew Massey, Allan Surgenor & Paul Workman. (2005) 3-(5-chloro-2,4-dihydroxyphenyl)-Pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone. Bioorganic & Medicinal Chemistry Letters 15:23, pages 5197-5201.
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Luke Whitesell & Susan L. Lindquist. (2005) HSP90 and the chaperoning of cancer. Nature Reviews Cancer 5:10, pages 761-772.
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Kwai-Ming J. Cheung, Thomas P. Matthews, Karen James, Martin G. Rowlands, Katherine J. Boxall, Swee Y. Sharp, Alison Maloney, S. Mark Roe, Chrisostomos Prodromou, Laurence H. Pearl, G. Wynne Aherne, Edward McDonald & Paul Workman. (2005) The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors. Bioorganic & Medicinal Chemistry Letters 15:14, pages 3338-3343.
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Udai Banerji, Anne O'Donnell, Michelle Scurr, Simon Pacey, Sarah Stapleton, Yasmin Asad, Laura Simmons, Alison Maloney, Florence Raynaud, Maeli Campbell, Michael Walton, Sunil Lakhani, Stanley Kaye, Paul Workman & Ian Judson. (2005) Phase I Pharmacokinetic and Pharmacodynamic Study of 17-Allylamino, 17-Demethoxygeldanamycin in Patients With Advanced Malignancies. Journal of Clinical Oncology 23:18, pages 4152-4161.
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Anthea HardcastleKathy BoxallJuliet RichardsPeter TomlinSwee SharpPaul ClarkePaul WorkmanWynne Aherne. (2005) Solid-Phase Immunoassays in Mechanism-Based Drug Discovery: Their Application in the Development of Inhibitors of the Molecular Chaperone Heat-Shock Protein 90. ASSAY and Drug Development Technologies 3:3, pages 273-285.
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Brian W. DymockXavier BarrilPaul A. BroughJulie E. CansfieldAndrew MasseyEdward McDonaldRoderick E. HubbardAllan SurgenorStephen D. RoughleyPaul WebbPaul WorkmanLisa WrightMartin J. Drysdale. (2005) Novel, Potent Small-Molecule Inhibitors of the Molecular Chaperone Hsp90 Discovered through Structure-Based Design. Journal of Medicinal Chemistry 48:13, pages 4212-4215.
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Emilie Moulin, Vincent Zoete, Sofia Barluenga, Martin Karplus & Nicolas Winssinger. (2005) Design, Synthesis, and Biological Evaluation of HSP90 Inhibitors Based on Conformational Analysis of Radicicol and Its Analogues. Journal of the American Chemical Society 127:19, pages 6999-7004.
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P. WORKMAN. (2005) Drugging the Cancer Kinome: Progress and Challenges in Developing Personalized Molecular Cancer Therapeutics. Cold Spring Harbor Symposia on Quantitative Biology 70:0, pages 499-515.
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Paul Workman. (2005) Genomics and the second golden era of cancer drug development. Molecular BioSystems 1:1, pages 17.
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Marco A. Biamonte, Jiandong Shi, David Hurst, Kevin Hong, Marcus F. Boehm & Srinivas R. Kasibhatla. (2004) Preparation of 8-(Arylsulfanyl)adenines with Diazonium Salts under Mild, Aerobic Conditions. The Journal of Organic Chemistry 70:2, pages 717-720.
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Ann L. Jackman, Stanley Kaye & Paul Workman. (2004) The combination of cytotoxic and molecularly targeted therapies – can it be done?. Drug Discovery Today: Therapeutic Strategies 1:4, pages 445-454.
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