Assay design and development strategies for finding Hsp90 inhibitors and their role in human diseases

Discovery and Optimization of Small Molecules Targeting the Protein–Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer

(2020) Lei Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

From Bacteria to Cancer: A Benzothiazole-Based DNA Gyrase B Inhibitor Redesigned for Hsp90 C-Terminal Inhibition

(2020) Kyler W. Pugh et al.   ACS Medicinal Chemistry Letters

Structure, Function, and Regulation of the Hsp90 Machinery

(2019) Maximilian M. Biebl et al.   Cold Spring Harbor Perspectives in Biology

Mitochondrial-targeted Hsp90 C-terminal inhibitors manifest anti-proliferative activity

(2019) Zheng Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Small-molecule inhibitor targeting the Hsp90-Cdc37 protein-protein interaction in colorectal cancer

(2019) Lei Wang et al.   Science Advances

Development of a Cell-Based Ligand-Screening System for Identifying Hsp90 Inhibitors

(2019) Tsuyoshi Ueda et al.   BIOCHEMISTRY

C-terminal modulators of heat shock protein of 90 kDa (HSP90): State of development and modes of action

(2019) David Bickel et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Identification of Isoform-Selective Ligands for the Middle Domain of Heat Shock Protein 90 (Hsp90)

(2019) Oi Wei Mak et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Synthesis and evaluation of a ring-constrained Hsp90 C-terminal inhibitor that exhibits neuroprotective activity

(2018) Zheng Zhang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Methods to validate Hsp90 inhibitor specificity, to identify off-target effects, and to rethink approaches for further clinical development

(2018) Len Neckers et al.   CELL STRESS & CHAPERONES

Synthesis and Structure–Activity Relationships of Inhibitors That Target the C-Terminal MEEVD on Heat Shock Protein 90

(2018) Marwa N. Rahimi et al.   ACS Medicinal Chemistry Letters

Structure-guided design of an Hsp90β N-terminal isoform-selective inhibitor

(2018) Anuj Khandelwal et al.   Nature Communications

Triptolide, a HSP90 middle domain inhibitor, induces apoptosis in triple manner

(2018) Frederick Zhehao Zhang et al.   Oncotarget

Discovery of new molecular entities able to strongly interfere with Hsp90 C-terminal domain

(2018) Stefania Terracciano et al.   Scientific Reports

3D-QSAR, molecular docking, and molecular dynamic simulations for prediction of new Hsp90 inhibitors based on isoxazole scaffold

(2017) Maryam Abbasi et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

The HSP90 chaperone machinery

(2017) Florian H. Schopf et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Hsp90 activator Aha1 drives production of pathological tau aggregates

(2017) Lindsey B. Shelton et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Imbalances in the Hsp90 Chaperone Machinery: Implications for Tauopathies

(2017) Lindsey B. Shelton et al.   Frontiers in Neuroscience

Thioflavin T as an amyloid dye: fibril quantification, optimal concentration and effect on aggregation

(2017) Christine Xue et al.   Royal Society Open Science

Mechanisms of Hsp90 regulation

(2016) C. Prodromou   BIOCHEMICAL JOURNAL

Tryptophan fluorescence quenching as a binding assay to monitor protein conformation changes in the membrane of intact mitochondria

(2016) S. MD. Akbar et al.   JOURNAL OF BIOENERGETICS AND BIOMEMBRANES

Thermodynamic Analysis of the Geldanamycin–Hsp90 Interaction in a Whole Cell Lysate Using a Mass Spectrometry-Based Proteomics Approach

(2016) Yingrong Xu et al.   JOURNAL OF THE AMERICAN SOCIETY FOR MASS SPECTROMETRY

Biophysics in drug discovery: impact, challenges and opportunities

(2016) Jean-Paul Renaud et al.   NATURE REVIEWS DRUG DISCOVERY

Establish an automated flow injection ESI-MS method for the screening of fragment based libraries: Application to Hsp90

(2015) Federico Riccardi Sirtori et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Molecular docking study, synthesis and biological evaluation of Mannich bases as Hsp90 inhibitors

(2015) Sayan Dutta Gupta et al.   INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES

Development of a Mitochondria-Targeted Hsp90 Inhibitor Based on the Crystal Structures of Human TRAP1

(2015) Changwook Lee et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Hsp90: Breaking the Symmetry

(2015) Matthias P. Mayer et al.   MOLECULAR CELL

Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors

(2014) Elena Casale et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Comparison of the sensitivities of WaterLOGSY and saturation transfer difference NMR experiments

(2014) Aleksandar Antanasijevic et al.   JOURNAL OF BIOMOLECULAR NMR

Designed Hsp90 Heterodimers Reveal an Asymmetric ATPase-Driven Mechanism In Vivo

(2014) Parul Mishra et al.   MOLECULAR CELL

Heat Shock Protein 90 in Alzheimer’s Disease

(2014) Jiang-Rong Ou et al.   Biomed Research International

Development of a High-Throughput Screening Cancer Cell-Based Luciferase Refolding Assay for Identifying Hsp90 Inhibitors

(2013) Takrima Sadikot et al.   ASSAY AND DRUG DEVELOPMENT TECHNOLOGIES

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

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

Inhibition of HSP90 molecular chaperones: moving into the clinic

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

Association of heat-shock proteins in various neurodegenerative disorders: is it a master key to open the therapeutic door?

(2013) Subhankar Paul et al.   MOLECULAR AND CELLULAR BIOCHEMISTRY

The chaperone Hsp90: changing partners for demanding clients

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

Molecular Pathways: Targeting Hsp90--Who Benefits and Who Does Not

(2012) M. Scaltriti et al.   CLINICAL CANCER RESEARCH

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet?

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

Heat Shock Protein 90 Inhibitors as Broad Spectrum Anti-Infectives

(2012) Ankit K. Rochani et al.   CURRENT PHARMACEUTICAL DESIGN

From a Ratchet Mechanism to Random Fluctuations Evolution of Hsp90's Mechanochemical Cycle

(2012) Christoph Ratzke et al.   JOURNAL OF MOLECULAR BIOLOGY

The rapid and direct determination of ATPase activity by ion exchange chromatography and the application to the activity of heat shock protein-90

(2012) Manuela Bartolini et al.   JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS

Heat shock protein 90 in neurodegenerative diseases

(2012) Wenjie Luo et al.   Molecular Neurodegeneration

Thermodynamic analysis of protein-ligand binding interactions in complex biological mixtures using the stability of proteins from rates of oxidation

(2012) Erin C Strickland et al.   Nature Protocols

Discovery and validation of small-molecule heat-shock protein 90 inhibitors through multimodality molecular imaging in living subjects

(2012) C. T. Chan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Elucidation of the Hsp90 C-Terminal Inhibitor Binding Site

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

Design strategies to target crystallographic waters applied to the Hsp90 molecular chaperone

(2011) Pei-Pei Kung et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

How Well Can Fragments Explore Accessed Chemical Space? A Case Study from Heat Shock Protein 90

(2011) Stephen D. Roughley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural analysis of the interaction between Hsp90 and the tumor suppressor protein p53

(2011) Franz Hagn et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Heat shock response and insulin-associated neurodegeneration

(2011) Michael J. Urban et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Collective Roles of Molecular Chaperones in Protein Degradation Pathways Associated with Neurodegenerative Diseases

(2010) Guang Luo et al.   CURRENT PHARMACEUTICAL BIOTECHNOLOGY

Fluorescence polarization assays in small molecule screening

(2010) Wendy A Lea et al.   Expert Opinion on Drug Discovery

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

HSP90 at the hub of protein homeostasis: emerging mechanistic insights

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

Hsp90 and co-chaperones twist the functions of diverse client proteins

(2009) Abbey Zuehlke et al.   BIOPOLYMERS

Thermodynamic Analysis of Protein Stability and Ligand Binding Using a Chemical Modification- and Mass Spectrometry-Based Strategy

(2008) Graham M. West et al.   ANALYTICAL CHEMISTRY

Chaperone signalling complexes in Alzheimer's disease

(2008) John Koren et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Dynamics of conserved waters in human Hsp90: implications for drug design

(2008) A. Yan et al.   Journal of the Royal Society Interface