Advances in the discovery and development of heat-shock protein 90 inhibitors for cancer treatment

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

(2011) Jennifer R. Smith et al.   CELL CYCLE

Camptothecin disrupts androgen receptor signaling and suppresses prostate cancer cell growth

(2010) Shicheng Liu et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Natural and semisynthetic azaphilones as a new scaffold for Hsp90 inhibitors

(2010) Loana Musso et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Application of Chemoproteomics to Drug Discovery: Identification of a Clinical Candidate Targeting Hsp90

(2010) Patrick Fadden et al.   CHEMISTRY & BIOLOGY

New Molecular and Biological Mechanism of Antitumor Activities of KW-2478, a Novel Nonansamycin Heat Shock Protein 90 Inhibitor, in Multiple Myeloma Cells

(2010) T. Nakashima et al.   CLINICAL CANCER RESEARCH

Discovery and development of Hsp90 inhibitors: a promising pathway for cancer therapy

(2010) James R Porter et al.   CURRENT OPINION IN CHEMICAL BIOLOGY

HSP90 is a therapeutic target in JAK2-dependent myeloproliferative neoplasms in mice and humans

(2010) Sachie Marubayashi et al.   JOURNAL OF CLINICAL INVESTIGATION

Discovery of (2,4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone Hsp90 by Fragment Based Drug Design

(2010) Andrew J. Woodhead et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Drug Discovery Applied to Hsp90. Discovery of Two Lead Series with High Ligand Efficiency

(2010) Christopher W. Murray et al.   JOURNAL OF MEDICINAL CHEMISTRY

Gymnastics of Molecular Chaperones

(2010) Matthias P. Mayer   MOLECULAR CELL

Asymmetric Activation of the Hsp90 Dimer by Its Cochaperone Aha1

(2010) Marco Retzlaff et al.   MOLECULAR CELL

Swe1Wee1-Dependent Tyrosine Phosphorylation of Hsp90 Regulates Distinct Facets of Chaperone Function

(2010) Mehdi Mollapour et al.   MOLECULAR CELL

HSP90 at the hub of protein homeostasis: emerging mechanistic insights

(2010) Mikko Taipale et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Measuring the Pharmacodynamic Effects of a Novel Hsp90 Inhibitor on HER2/neu Expression in Mice Using 89Zr-DFO-Trastuzumab

(2010) Jason P. Holland et al.   PLoS One

Molecular Mechanism of Inhibition of the Human Protein Complex Hsp90-Cdc37, a Kinome Chaperone-Cochaperone, by Triterpene Celastrol

(2009) Sridhar Sreeramulu et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Withaferin A targets heat shock protein 90 in pancreatic cancer cells

(2009) Yanke Yu et al.   BIOCHEMICAL PHARMACOLOGY

Identification of new Hsp90 inhibitors by structure-based virtual screening

(2009) Tae-Joon Hong et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Protein Kinase CK2 in Health and Disease

(2009) Y. Miyata   CELLULAR AND MOLECULAR LIFE SCIENCES

Potent Triazolothione Inhibitor of Heat-Shock Protein-90

(2009) Richard I. Feldman et al.   Chemical Biology & Drug Design

Fragment-based Identification of Hsp90 Inhibitors

(2009) John J. Barker et al.   ChemMedChem

CUDC-305, a Novel Synthetic HSP90 Inhibitor with Unique Pharmacologic Properties for Cancer Therapy

(2009) R. Bao et al.   CLINICAL CANCER RESEARCH

Alternate Strategies of Hsp90 Modulation for the Treatment of Cancer and Other Diseases

(2009) Gary Brandt et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Purine-Scaffold Hsp90 Inhibitors

(2009) Tony Taldone et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Update on Hsp90 Inhibitors in Clinical Trial

(2009) Y. Kim et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Hsp90 is regulated by a switch point in the C-terminal domain

(2009) Marco Retzlaff et al.   EMBO REPORTS

Targeting heat shock protein 90 with non-quinone inhibitors: A novel chemotherapeutic approach in human hepatocellular carcinoma

(2009) Marco Breinig et al.   HEPATOLOGY

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

(2009) Paul A. Brough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel 2-Aminobenzamide Inhibitors of Heat Shock Protein 90 as Potent, Selective and Orally Active Antitumor Agents

(2009) Kenneth H. Huang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Dihydroxyphenylisoindoline Amides as Orally Bioavailable Inhibitors of the Heat Shock Protein 90 (Hsp90) Molecular Chaperone

(2009) Pei-Pei Kung et al.   JOURNAL OF MEDICINAL CHEMISTRY

BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90

(2009) K. Lundgren et al.   MOLECULAR CANCER THERAPEUTICS

Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib

(2009) C. C. Leow et al.   MOLECULAR CANCER THERAPEUTICS

A purine scaffold Hsp90 inhibitor destabilizes BCL-6 and has specific antitumor activity in BCL-6–dependent B cell lymphomas

(2009) Leandro C Cerchietti et al.   NATURE MEDICINE

The large conformational changes of Hsp90 are only weakly coupled to ATP hydrolysis

(2009) Moritz Mickler et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Dissection of the ATP-induced conformational cycle of the molecular chaperone Hsp90

(2009) Martin Hessling et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models

(2009) E. Caldas-Lopes et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Modeling Signal Propagation Mechanisms and Ligand-Based Conformational Dynamics of the Hsp90 Molecular Chaperone Full-Length Dimer

(2009) Giulia Morra et al.   PLoS Computational Biology

A Novel Class of Small Molecule Inhibitors of Hsp90

(2008) Fang Yi et al.   ACS Chemical Biology

Designed TPR Modules as Novel Anticancer Agents

(2008) Aitziber L. Cortajarena et al.   ACS Chemical Biology

Apo-Hsp90 coexists in two open conformational states in solution

(2008) Patrick Bron et al.   BIOLOGY OF THE CELL

Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modeling

(2008) Thota Ganesh et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery and development of heat shock protein 90 inhibitors

(2008) Tony Taldone et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone

(2008) Pei-Pei Kung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

HDAC6 inhibition enhances 17-AAG-mediated abrogation of hsp90 chaperone function in human leukemia cells

(2008) R. Rao et al.   BLOOD

P-Glycoprotein-Mediated Resistance to Hsp90-Directed Therapy Is Eclipsed by the Heat Shock Response

(2008) A. K. McCollum et al.   CANCER RESEARCH

Role of Acetylation and Extracellular Location of Heat Shock Protein 90  in Tumor Cell Invasion

(2008) Y. Yang et al.   CANCER RESEARCH

SNX2112, a Synthetic Heat Shock Protein 90 Inhibitor, Has Potent Antitumor Activity against HER Kinase Dependent Cancers

(2008) S. Chandarlapaty et al.   CLINICAL CANCER RESEARCH

Novobiocin and Additional Inhibitors of the Hsp90 C-Terminal Nucleotide- binding Pocket

(2008) Alison Donnelly et al.   CURRENT MEDICINAL CHEMISTRY

Medicinal Chemistry of Hsp90 Inhibitors

(2008) Martin Drysdale et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Conserved Conformational Changes in the ATPase Cycle of Human Hsp90

(2008) Klaus Richter et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Discovery of Benzisoxazoles as Potent Inhibitors of Chaperone Heat Shock Protein 90

(2008) Ariamala Gopalsamy et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Studies on the Co-chaperone Hop and Its Complexes with Hsp90

(2008) S.C. Onuoha et al.   JOURNAL OF MOLECULAR BIOLOGY

MS-275, a novel histone deacetylase inhibitor with selectivity against HDAC1, induces degradation of FLT3 via inhibition of chaperone function of heat shock protein 90 in AML cells

(2008) Chie Nishioka et al.   LEUKEMIA RESEARCH

A novel Hsp90 inhibitor to disrupt Hsp90/Cdc37 complex against pancreatic cancer cells

(2008) T. Zhang et al.   MOLECULAR CANCER THERAPEUTICS

Silencing the cochaperone CDC37 destabilizes kinase clients and sensitizes cancer cells to HSP90 inhibitors

(2008) J R Smith et al.   ONCOGENE

Inhibition of Hsp90 activates osteoclast c-Src signaling and promotes growth of prostate carcinoma cells in bone

(2008) A. Yano et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Multiple Conformations of E. coli Hsp90 in Solution: Insights into the Conformational Dynamics of Hsp90

(2008) Kristin A. Krukenberg et al.   STRUCTURE