Natural Product Inspired N-Terminal Hsp90 Inhibitors: From Bench to Bedside?

Design, synthesis and biological evaluation of biphenylamide derivatives as Hsp90 C-terminal inhibitors

(2015) Huiping Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Development of radamide analogs as Grp94 inhibitors

(2014) Aaron Muth et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of Novel 17-Phenylethylaminegeldanamycin Derivatives as Potent Hsp90 Inhibitors

(2014) Zhenyu Li et al.   Chemical Biology & Drug Design

Design, synthesis and biological evaluation of 17-arylmethylamine-17-demethoxygeldanamycin derivatives as potent Hsp90 inhibitors

(2014) Zhenyu Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of diamine-linked 17-aroylamido-17-demethoxygeldanamycins as potent Hsp90 inhibitors

(2014) Zhenyu Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Alternative approaches to Hsp90 modulation for the treatment of cancer

(2014) Jessica A Hall et al.   Future Medicinal Chemistry

Exploiting the interaction between Grp94 and aggregated myocilin to treat glaucoma

(2014) Andrew R. Stothert et al.   HUMAN MOLECULAR GENETICS

Microarray-based screening of heat shock protein inhibitors

(2014) Emilia Schax et al.   JOURNAL OF BIOTECHNOLOGY

Progress in the Discovery and Development of Heat Shock Protein 90 (Hsp90) Inhibitors

(2014) Rohit Bhat et al.   JOURNAL OF MEDICINAL CHEMISTRY

Overcoming the resistance to Crizotinib in patients with Non-Small Cell Lung Cancer harboring EML4/ALK translocation

(2014) Cesar A. Perez et al.   LUNG CANCER

Selective targeting of the stress chaperome as a therapeutic strategy

(2014) Tony Taldone et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

An improved route to 19-substituted geldanamycins as novel Hsp90 inhibitors – potential therapeutics in cancer and neurodegeneration

(2013) Russell R. A. Kitson et al.   CHEMICAL COMMUNICATIONS

Phase I Study of BIIB028, a Selective Heat Shock Protein 90 Inhibitor, in Patients with Refractory Metastatic or Locally Advanced Solid Tumors

(2013) D. Hong et al.   CLINICAL CANCER RESEARCH

Molecular Chaperone gp96 Is a Novel Therapeutic Target of Multiple Myeloma

(2013) Y. Hua et al.   CLINICAL CANCER RESEARCH

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

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

Experimental and Structural Testing Module to Analyze Paralogue-Specificity and Affinity in the Hsp90 Inhibitors Series

(2013) Tony Taldone et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

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

Inhibition of HSP90 molecular chaperones: moving into the clinic

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

The HSP90 Inhibitor NVP-AUY922 Potently Inhibits Non-Small Cell Lung Cancer Growth

(2013) E. B. Garon et al.   MOLECULAR CANCER THERAPEUTICS

Targeting heat-shock-protein 90 (Hsp90) by natural products: geldanamycin, a show case in cancer therapy

(2013) Jana Franke et al.   NATURAL PRODUCT REPORTS

21st Century natural product research and drug development and traditional medicines

(2013) Linh T. Ngo et al.   NATURAL PRODUCT REPORTS

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

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

Essential roles of grp94 in gut homeostasis via chaperoning canonical Wnt pathway

(2013) B. Liu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The chaperone Hsp90: changing partners for demanding clients

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

Structure, Function and Regulation of the Hsp90 Machinery

(2013) Johannes Buchner et al.   Biomedical Journal

Phase II study of the HSP90-inhibitor BIIB021 in gastrointestinal stromal tumors

(2012) M. A. Dickson et al.   ANNALS OF ONCOLOGY

Targeting the molecular chaperone heat shock protein 90 (HSP90): Lessons learned and future directions

(2012) David S. Hong et al.   CANCER TREATMENT REVIEWS

Ganetespib (STA-9090), a Nongeldanamycin HSP90 Inhibitor, Has Potent Antitumor Activity in In Vitro and In Vivo Models of Non-Small Cell Lung Cancer

(2012) T. Shimamura et al.   CLINICAL CANCER RESEARCH

Hsp90 Molecular Chaperone Inhibitors: Are We There Yet?

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

The Therapeutic Target Hsp90 and Cancer Hallmarks

(2012) Yoshihiko Miyata et al.   CURRENT PHARMACEUTICAL DESIGN

Overexpression of GRP94 in breast cancer cells resistant to oxidative stress promotes high levels of cancer cell proliferation and migration: Implications for tumor recurrence

(2012) Nicolas Dejeans et al.   FREE RADICAL BIOLOGY AND MEDICINE

Glucose-regulated Protein 94 Triage of Mutant Myocilin through Endoplasmic Reticulum-associated Degradation Subverts a More Efficient Autophagic Clearance Mechanism

(2012) Amirthaa Suntharalingam et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Charting, Navigating, and Populating Natural Product Chemical Space for Drug Discovery

(2012) Hugo Lachance et al.   JOURNAL OF MEDICINAL CHEMISTRY

Proteomic Plasma Membrane Profiling Reveals an Essential Role for gp96 in the Cell Surface Expression of LDLR Family Members, Including the LDL Receptor and LRP6

(2012) Michael P. Weekes et al.   JOURNAL OF PROTEOME RESEARCH

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

Fluorine- and rhenium-containing geldanamycin derivatives as leads for the development of molecular probes for imaging Hsp90

(2012) Frank Wuest et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

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

Hallmarks of Cancer: The Next Generation

(2011) Douglas Hanahan et al.   CELL

Heat-shock protein 90 inhibitors as antitumor agents: a survey of the literature from 2005 to 2010

(2011) Samir Messaoudi et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Targeting the Heat Shock Protein 90 Dimer with Dimeric Inhibitors

(2011) Bhaskar Reddy Kusuma et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

Broad Substrate Specificity of the Amide Synthase in S. hygroscopicus—New 20-Membered Macrolactones Derived from Geldanamycin

(2011) Simone Eichner et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Learning from Falling: Retention of Fall-Resisting Behavior Derived from One Episode of Laboratory-Induced Slip Training

(2011) Tanvi Bhatt et al.   JOURNAL OF THE AMERICAN GERIATRICS SOCIETY

A phase 1 study of IPI-504 (retaspimycin hydrochloride) in patients with relapsed or relapsed and refractory multiple myeloma

(2011) David Siegel et al.   LEUKEMIA & LYMPHOMA

Strong anti-tumor effect of NVP-AUY922, a novel Hsp90 inhibitor, on non-small cell lung cancer

(2011) Tsuyoshi Ueno et al.   LUNG CANCER

The Heat Shock Protein 90 Inhibitor IPI-504 Induces KIT Degradation, Tumor Shrinkage, and Cell Proliferation Arrest in Xenograft Models of Gastrointestinal Stromal Tumors

(2011) G. Floris et al.   MOLECULAR CANCER THERAPEUTICS

Ganetespib, a Unique Triazolone-Containing Hsp90 Inhibitor, Exhibits Potent Antitumor Activity and a Superior Safety Profile for Cancer Therapy

(2011) W. Ying et al.   MOLECULAR CANCER THERAPEUTICS

Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90

(2011) Kamalika Moulick et al.   Nature Chemical 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 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

Synthesis of Reblastatin, Autolytimycin, and Non-Benzoquinone Analogues: Potent Inhibitors of Heat Shock Protein 90

(2010) Iwona E. Wrona et al.   JOURNAL OF ORGANIC CHEMISTRY

HSP90 at the hub of protein homeostasis: emerging mechanistic insights

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

GRP94 in ER quality control and stress responses

(2010) Davide Eletto et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

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

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

New, Highly Active Nonbenzoquinone Geldanamycin Derivatives by Using Mutasynthesis

(2009) Simone Eichner et al.   CHEMBIOCHEM

Rational Biosynthetic Engineering for Optimization of Geldanamycin Analogues

(2009) Woncheol Kim et al.   CHEMBIOCHEM

Preparation, Modification, and Evaluation of Cruentaren A and Analogues

(2009) Martin Bindl et al.   CHEMISTRY-A EUROPEAN JOURNAL

Structure-Based and in silico Design of Hsp90 Inhibitors

(2009) Miriam Sgobba et al.   ChemMedChem

17 AAG for HSP90 Inhibition in Cancer – From Bench to Bedside

(2009) Saad Usmani et al.   CURRENT MOLECULAR MEDICINE

Ansamycin Inhibitors of Hsp90: Natures Prototype for Anti-Chaperone Therapy

(2009) James Porter et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

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

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

Characterization of Celastrol to Inhibit Hsp90 and Cdc37 Interaction

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

Different Poses for Ligand and Chaperone in Inhibitor-Bound Hsp90 and GRP94: Implications for Paralog-Specific Drug Design

(2009) Robert M. Immormino et al.   JOURNAL OF MOLECULAR BIOLOGY

Natural Product Inhibitors of Hsp90: Potential Leads for Drug Discovery

(2009) M. Amolins et al.   MINI-REVIEWS IN 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

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

Design, Synthesis, and Biological Evaluation of Conformationally Constrainedcis-Amide Hsp90 Inhibitors

(2009) Adam S. Duerfeldt et al.   ORGANIC LETTERS

Drug Discovery and Natural Products: End of an Era or an Endless Frontier?

(2009) J. W.-H. Li et al.   SCIENCE

Synthesis and evaluation of 8,9-amido analogs of geldanamycin

(2009) Merritt B. Andrus et al.   TETRAHEDRON LETTERS

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

(2008) Zhengyu Yin et al.   BIOCHEMISTRY

Synthesis and evaluation of electron-rich curcumin analogues

(2008) Michael W. Amolins et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Cruentaren A Analogues

(2008) Viktor V. Vintonyak et al.   CHEMISTRY-A EUROPEAN JOURNAL

Natural products in drug discovery

(2008) A HARVEY   DRUG DISCOVERY TODAY

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

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

Optimizing Natural Products by Biosynthetic Engineering: Discovery of Nonquinone Hsp90 Inhibitors†

(2008) Ming-Qiang Zhang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Molecular Characterization of Macbecin as an Hsp90 Inhibitor#

(2008) Christine J. Martin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Natural Products as Leads to Potential Drugs: An Old Process or the New Hope for Drug Discovery?

(2008) David J. Newman   JOURNAL OF MEDICINAL CHEMISTRY

Signalling profile and antitumour activity of the novel Hsp90 inhibitor NVP-AUY922 in multiple myeloma

(2008) T Stühmer et al.   LEUKEMIA

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

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

Total Synthesis of the Hsp90 Inhibitor Geldanamycin

(2008) Hua-Li Qin et al.   ORGANIC LETTERS

4,5-Diarylisoxazole Hsp90 Chaperone Inhibitors: Potential Therapeutic Agents for the Treatment of Cancer

(2007) Paul A. Brough et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and anticancer activity of geldanamycin derivatives derived from biosynthetically generated metabolites

(2007) Kyeong Lee et al.   ORGANIC & BIOMOLECULAR CHEMISTRY