Inhibitors of Molecular Chaperones as Therapeutic Agents

Cover
Timothy D Machajewski, Zhenhai Gao
Royal Society of Chemistry, 23.10.2013 - 352 Seiten

This book aims to provide a comprehensive examination of the field of molecular chaperone inhibition and its application to pharmaceutical research. With several small molecule inhibitors in oncology clinical development, there is clearly intense interest in the chaperones as a molecular target. Filling a significant gap in the market by providing a detailed comparison of discovery programs across the industry, this text will find broad interest among researchers in the field of molecular chaperone pharmaceutical research, oncology research, and medicinal chemistry.


Arranged into three main sections the book covers structure and function, small molecule inhibitors and concludes with a section discussing clinical perspectives. With specific chapters covering the discovery of key molecules such as, BIIB028, STA-9090, Serenex Hsp90 inhibitor, NVP-AUY922 and NVP-HSP990, this comprehensive text is an essential treatise for researchers working in academia and industry.

 

Ausgewählte Seiten

Inhalt

Chapter 1 Overview of Molecular Chaperones in Health and Disease
1
Chapter 2 Structural Basis of Hsp90 Function
37
Chapter 3 Structure and Function of Hsp70 Molecular Chaperones
65
Chapter 4 Exploiting the Dependency of Cancer Cells on Molecular Chaperones
126
Chapter 5 The Discovery of BIIB021 and BIIB028
158
Chapter 6 Discovery and Development of Ganetespib
180
Chapter 7 Discovery of the Serenex Hsp90 Inhibitor SNX5422
198
Chapter 8 Discovery of NVPAUY922
213
Chapter 10 Inhibitors of the Hsp90 Cterminus
259
Chapter 11 Hsp70 Inhibitors
302
Drug Targeting and Posttranslational Regulation
318
Chapter 13 Hsp90 Inhibitors in Clinic
336
Chapter 14 Heatshock Protein 90 as an Antimalarial Target
379
Chapter 15 Molecular Chaperones as Potential Therapeutic Targets for Neurological Disorders
392
Subject Index
414
Urheberrecht

Chapter 9 Discovery and Selection of NVPHSP990 as a Clinical Candidate
241

Andere Ausgaben - Alle anzeigen

Inhibitors of Molecular Chaperones as Therapeutic Agents
Timothy D. Machajewski,Zhenhai Gao,David P. Rotella
Eingeschränkte Leseprobe - 2014

Häufige Begriffe und Wortgruppen

affinity aggregation Aha1 analogues anti-proliferative activity apoptosis assay ATP binding ATP lid ATPase ATPase activity Biochem bortezomib breast cancer cancer cells Cancer Res Cell Biol cell lines cellular Chem Clin clinical co-chaperones complex compounds conformation coumarin cycle cytosolic degradation dimerization disease DnaK docetaxel domain of Hsp90 dose Drug Discovery drug target effects efficacy EGFR evaluated Figure folding function ganetespib geldanamycin gene grade HER2 Hsf1 Hsp90 inhibitors human hydrogen bond hydrophobic induce inhibition interaction kinase L. H. Pearl linker mg/kg middle domain misfolded mitochondrial modulate molecular chaperones molecules mouse mutations N-terminal N-terminal domain Natl Acad Neckers neurodegenerative novobiocin NSCLC nucleotide observed oncogenic Oncol over-expression pathway patients peptide Phase phosphorylation potency potential Prodromou proteasome radicicol receptor resorcinol shown side-chain structure substrate tanespimycin therapeutic toxicity trastuzumab treatment tumor ubiquitin vitro vivo Wang Workman xenograft yeast Zhang

Bibliografische Informationen

TitelInhibitors of Molecular Chaperones as Therapeutic Agents
HerausgeberTimothy D Machajewski, Zhenhai Gao
VerlagRoyal Society of Chemistry, 2013
ISBN1849739684, 9781849739689
Länge352 Seiten
  
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