Structure-based Drug Design Enables Conversion of a DFG-in Binding CSF-1R Kinase Inhibitor to a DFG-out Binding Mode

Overview

Journal Bioorg Med Chem Lett

Specialty Biochemistry

Date 2010 Feb 9

PMID 20137931

Citations 10

Authors

Marvin J Meyers

Matthew Pelc

Satwik Kamtekar

Jacqueline Day

Gennadiy I Poda

Molly K Hall

Marshall L Michener

Beverly A Reitz

Karl J Mathis

Betsy S Pierce

Mihir D Parikh

Deborah A Mischke

Scott A Long

John J Parlow

David R Anderson

Atli Thorarensen

Affiliations

Soon will be listed here.

Abstract

The work described herein demonstrates the utility of structure-based drug design (SBDD) in shifting the binding mode of an HTS hit from a DFG-in to a DFG-out binding mode resulting in a class of novel potent CSF-1R kinase inhibitors suitable for lead development.

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