Molecular Targeting of Protein Kinases to Optimize Selectivity and Resistance Profiles of Kinase Inhibitors

Author: Jeffrey, Liao J.i.e-L.o.u.¹

Source: Current Topics in Medicinal Chemistry, Volume 7, Number 14, July 2007 , pp. 1332-1335(4)

Publisher: Bentham Science Publishers

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Abstract:

This article reviews several important observations in the field of protein kinase drug discovery, exemplified mainly by targeting c-Abl for the treatment of CML. Structure-based strategy and insight are provided for the optimization of the selectivity and resistant mutation profiles of protein kinase inhibitors.

Keywords: Protein kinase; protein kinase inhibitor; selectivity; imatinib; CML; drug-resistant mutation; systematic structural analysis

Document Type: Research article

DOI: 10.2174/156802607781696800

Affiliations: 1: TransTech Pharma Inc., 4170 Mendenhall Oaks Pkwy, High Point, NC 27265.

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