Alternative approaches to Hsp90 modulation for the treatment of cancer

Cruentaren A Binds F1F0 ATP Synthase To Modulate the Hsp90 Protein Folding Machinery

(2014) Jessica A. Hall et al.   ACS Chemical Biology

Synthesis and biological evaluation of coumarin replacements of novobiocin as Hsp90 inhibitors

(2014) Bhaskar Reddy Kusuma et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Asymmetric Hsp90 N Domain SUMOylation Recruits Aha1 and ATP-Competitive Inhibitors

(2014) Mehdi Mollapour et al.   MOLECULAR CELL

Synthesis and biological evaluation of novobiocin analogues as potential heat shock protein 90 inhibitors

(2013) G.M. Kamal B. Gunaherath et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A heat shock protein 90 inhibitor that modulates the immunophilins and regulates hormone receptors without inducing the heat shock response

(2013) Jeanette R. McConnell et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Contributions of co-chaperones and post-translational modifications towards Hsp90 drug sensitivity

(2013) Annerleim Walton-Diaz et al.   Future Medicinal Chemistry

Cdc37 (Cell Division Cycle 37) Restricts Hsp90 (Heat Shock Protein 90) Motility by Interaction with N-terminal and Middle Domain Binding Sites

(2013) Julia M. Eckl et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Gedunin Inactivates the Co-chaperone p23 Protein Causing Cancer Cell Death by Apoptosis

(2013) Chaitanya A. Patwardhan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis and Structure–Activity Relationships of EGCG Analogues, a Recently Identified Hsp90 Inhibitor

(2013) Anuj Khandelwal et al.   JOURNAL OF ORGANIC CHEMISTRY

Learning from Nature: Advances in Geldanamycin- and Radicicol-Based Inhibitors of Hsp90

(2013) Russell R. A. Kitson et al.   JOURNAL OF ORGANIC CHEMISTRY

Inhibition of HSP90 molecular chaperones: moving into the clinic

(2013) Rocio Garcia-Carbonero et al.   LANCET ONCOLOGY

Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2

(2013) Pallav D Patel et al.   Nature Chemical Biology

Integration of the accelerator Aha1 in the Hsp90 co-chaperone cycle

(2013) Jing Li et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The chaperone Hsp90: changing partners for demanding clients

(2013) Alina Röhl et al.   TRENDS IN BIOCHEMICAL SCIENCES

Identification of a New Scaffold for Hsp90 C-Terminal Inhibition

(2013) Huiping Zhao et al.   ACS Medicinal Chemistry Letters

SGTA: A New Player in the Molecular Co-Chaperone Game

(2013) Lisa K. Philp et al.   Hormones & Cancer

Structure, Function and Regulation of the Hsp90 Machinery

(2013) Johannes Buchner et al.   Biomedical Journal

Novobiocin analogues with second-generation noviose surrogates

(2012) Huiping Zhao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet?

(2012) L. Neckers et al.   CLINICAL CANCER RESEARCH

The network interaction of the human cytosolic 90kDa heat shock protein Hsp90: A target for cancer therapeutics

(2012) Viviane C.H. da Silva et al.   Journal of Proteomics

Development of a Grp94 inhibitor

(2012) Adam S. Duerfeldt et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The hERG Channel Is Dependent upon the Hsp90α Isoform for Maturation and Trafficking

(2012) Laura B. Peterson et al.   MOLECULAR PHARMACEUTICS

3-Arylcoumarin Derivatives Manifest Anti-proliferative Activity through Hsp90 Inhibition

(2012) Huiping Zhao et al.   ACS Medicinal Chemistry Letters

Elucidation of the Hsp90 C-Terminal Inhibitor Binding Site

(2011) Robert L. Matts et al.   ACS Chemical Biology

Macrocycles That Inhibit the Binding between Heat Shock Protein 90 and TPR-Containing Proteins

(2011) Veronica C. Ardi et al.   ACS Chemical Biology

HSP90 as a platform for the assembly of more effective cancer chemotherapy

(2011) Luke Whitesell et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Advances in the clinical development of heat shock protein 90 (Hsp90) inhibitors in cancers

(2011) Komal Jhaveri et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

The ‘active life’ of Hsp90 complexes

(2011) Chrisostomos Prodromou   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

The Hsp90 chaperone machinery: Conformational dynamics and regulation by co-chaperones

(2011) Jing Li et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Post-translational modifications of Hsp90 and their contributions to chaperone regulation

(2011) Mehdi Mollapour et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors

(2011) Bhaskar Reddy Kusuma et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Development and characterization of a novel C-terminal inhibitor of Hsp90 in androgen dependent and independent prostate cancer cells

(2011) Jeffery D Eskew et al.   BMC CANCER

Engineering an Antibiotic to Fight Cancer: Optimization of the Novobiocin Scaffold to Produce Anti-proliferative Agents

(2011) Huiping Zhao et al.   JOURNAL OF MEDICINAL CHEMISTRY

Convergent Synthesis and Discovery of a Natural Product-Inspired Paralog-Selective Hsp90 Inhibitor

(2011) Valer Jeso et al.   ORGANIC LETTERS

Balance between Folding and Degradation for Hsp90-Dependent Client Proteins: A Key Role for CHIP

(2010) Lenka Kundrat et al.   BIOCHEMISTRY

Click chemistry to probe Hsp90: Synthesis and evaluation of a series of triazole-containing novobiocin analogues

(2010) Laura B. Peterson et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Identification and initial SAR of silybin: An Hsp90 inhibitor

(2010) Huiping Zhao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antitumor activity of efrapeptins, alone or in combination with 2-deoxyglucose, in breast cancer in vitro and in vivo

(2010) Adonia E. Papathanassiu et al.   CELL STRESS & CHAPERONES

Cdc37-Hsp90 Complexes Are Responsive to Nucleotide-induced Conformational Changes and Binding of Further Cofactors

(2010) Andreas M. Gaiser et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Pih1-Tah1 Cochaperone Complex Inhibits Hsp90 Molecular Chaperone ATPase Activity

(2010) Kelvin Eckert et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Structural Basis for Assembly of Hsp90-Sgt1-CHORD Protein Complexes: Implications for Chaperoning of NLR Innate Immunity Receptors

(2010) Minghao Zhang 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

Milk thistle in liver diseases: past, present, future

(2010) Ludovico Abenavoli et al.   PHYTOTHERAPY RESEARCH

Dynamics of heat shock protein 90 C-terminal dimerization is an important part of its conformational cycle

(2010) C. Ratzke et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Cytotoxic sugar analogues of an optimized novobiocin scaffold

(2010) Alison C. Donnelly et al.   MedChemComm

Mechanistic Studies of Sansalvamide A-Amide: An Allosteric Modulator of Hsp90

(2010) Robert C. Vasko et al.   ACS Medicinal Chemistry Letters

Hsp90: A Drug Target?

(2010) Jeffrey M. Holzbeierlein et al.   Current Oncology Reports

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

Curcumin inhibits nuclear localization of telomerase by dissociating the Hsp90 co-chaperone p23 from hTERT

(2009) Ji Hoon Lee et al.   CANCER LETTERS

Protein Kinase CK2 in Health and Disease

(2009) Y. Miyata   CELLULAR AND MOLECULAR LIFE SCIENCES

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

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

(2009) Marco Retzlaff et al.   EMBO REPORTS

Sgt1 Dimerization Is Negatively Regulated by Protein Kinase CK2-mediated Phosphorylation at Ser361

(2009) Parmil K. Bansal et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

HDAC6 Modulates Hsp90 Chaperone Activity and Regulates Activation of Aryl Hydrocarbon Receptor Signaling

(2009) Vikram D. Kekatpure et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Celastrol Inhibits Hsp90 Chaperoning of Steroid Receptors by Inducing Fibrillization of the Co-chaperone p23

(2009) Ahmed Chadli et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Characterization of Celastrol to Inhibit Hsp90 and Cdc37 Interaction

(2009) Tao Zhang et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Heat Shock Protein 90: Inhibitors in Clinical Trials

(2009) Marco A. Biamonte et al.   JOURNAL OF MEDICINAL CHEMISTRY

Silibinin Attenuates Amyloid  25-35 Peptide-Induced Memory Impairments: Implication of Inducible Nitric-Oxide Synthase and Tumor Necrosis Factor-  in Mice

(2009) P. Lu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Functional Proteomics Identifies Targets of Phosphorylation by B-Raf Signaling in Melanoma

(2009) William M. Old et al.   MOLECULAR CELL

KU135, a Novel Novobiocin-Derived C-Terminal Inhibitor of the 90-kDa Heat Shock Protein, Exerts Potent Antiproliferative Effects in Human Leukemic Cells

(2009) S. N. Shelton et al.   MOLECULAR PHARMACOLOGY

The regulatory mechanism of Hsp90α secretion and its function in tumor malignancy

(2009) Xiaofeng Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

(−)-Epigallocatechin-3-gallate Is a Novel Hsp90 Inhibitor†

(2008) Zhengyu Yin et al.   BIOCHEMISTRY

Synthesis and biological activity of simplified denoviose-coumarins related to novobiocin as potent inhibitors of heat-shock protein 90 (hsp90)

(2008) Christine Radanyi et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antiproliferative and apoptotic activities of tosylcyclonovobiocic acids as potent heat shock protein 90 inhibitors in human cancer cells

(2008) Christine Radanyi et al.   CANCER LETTERS

Intra- and Intermonomer Interactions Are Required to Synergistically Facilitate ATP Hydrolysis in Hsp90

(2008) Christian N. Cunningham et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Gedunin, a Novel Hsp90 Inhibitor: Semisynthesis of Derivatives and Preliminary Structure−Activity Relationships

(2008) Gary E. L. Brandt et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Design, Synthesis, and Evaluation of Coumarin Ring Derivatives of the Novobiocin Scaffold that Exhibit Antiproliferative Activity

(2008) Alison C. Donnelly et al.   JOURNAL OF ORGANIC CHEMISTRY

Development of Novobiocin Analogues That Manifest Anti-proliferative Activity against Several Cancer Cell Lines

(2008) Joseph A. Burlison et al.   JOURNAL OF ORGANIC CHEMISTRY

Inhibition of Apoptosome Formation by Suppression of Hsp90  Phosphorylation in Tyrosine Kinase-Induced Leukemias

(2008) M. Kurokawa et al.   MOLECULAR AND CELLULAR BIOLOGY

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

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