Methods in enzymology

by Shokat, Kevan M.

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Title Statements

Full title :Methods in enzymology. / edited by Kevan M. Shokat.

Edition Statements

Publication Date:2014.
Edition:First edition

Publication Statements

Publisher(s):Academic Press
Place of Publication:Waltham, Massachusetts
Language:eng
Publication Date:2014.

Notes

VERSEMENT EN LOT.

The Physical Object

Description:1 ressource en ligne.

Edition Identifiers

ISBN:9780123984623, 0123984629
oclc:on1044955388
LC Classification:QP606.P76
Dewey Decimal:572.792

Front Cover; Protein Kinase Inhibitors in Research and Medicine ; Copyright; Contents; Contributors; Preface; Chapter One: Catalytic Mechanisms and Regulation of Protein Kinases; 1. Introduction; 2. Kinetic Mechanism; 3. Chemical Mechanism of Kinase Phosphoryl Transfer; 4. Applications of Mechanistic Studies in Understanding Kinase Function and Regulation; 4.1. Bisubstrate analogs; 4.2. Oncogenic kinase mutants; 4.3. Chemical rescue of tyrosine kinases; 5. Summary and Outlook; References; Chapter Two: A Structural Atlas of Kinases Inhibited by Clinically Approved Drugs; 1. Introduction.

2. Kinase Structure and Catalytic Mechanism3. Staurosporine: A Promiscuous ATP-Competitive Inhibitor; 4. BCR-Abl Inhibitors; 4.1. Imatinib binds to a ``DFG-out ́ ́ Abl conformation; 4.2. Nilotinib (Tasigna): An imatinib analog effective against several imatinib-resistant Abl variants; 4.3. Ponatinib (Iclusig) overcomes an Abl gatekeeper resistance mutation; 4.4. Bosutinib (Bosulif) inhibits BCR-Abl; 4.5. Dasatinib (Sprycel) binds to a ``DFG-in ́ ́ conformation of Abl; 5. Tofacitinib (Xeljanz) Binds to a ``DFG-in ́ ́ Conformation of Janus Kinase; 6. Inhibition of Receptor Tyrosine Kinases.

6.1. Imatinib…