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.
Inhaltsverzeichnis
Section I Structure and Function: Conformational Dynamics, Structure and Functional Interactions of Hsp90 Chaperones;
Structural Basis of Hsp90 Function;
Structure and Function of Hsp70 – TBD;
Exploiting the Dependency of Cancer Cells on Molecular Chaperones;
Section II Small Molecule Inhibitors;
Discovery of BIIB028;
Discovery of STA-9090;
Discovery of Serenex Hsp90 Inhibitor;
Discovery of NVP-AUY922;
Discovery of NVP-HSP990;
Inhibitors of Hsp90 C-Terminal Domain;
Hsp70 Inhibitors;
Section III Clinical Perspectives;
Clinical Development of Hsp90 Inhibitors as Anti-Cancer Agents;
Hsp90 as a Potential Anti-Malarial Agent;
Biomarker Development and Indication Selection;
Other Disease Indications
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