Generic placeholder image

Current Topics in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

Target-Related Affinity Profiling: Teliks Lead Discovery Technology

Author(s): Paul Beroza, Komath Damodaran and Robert T. Lum

Volume 5, Issue 4, 2005

Page: [371 - 381] Pages: 11

DOI: 10.2174/1568026053828394

Price: $65

Abstract

Target-Related Affinity Profiling (TRAP*) is a computational drug discovery technology that is based on ‘affinity fingerprints’, which are molecular descriptors derived from the protein binding preferences of small molecules. The underlying concepts of TRAP are reviewed. Affinity fingerprints are compared to molecular descriptors derived from chemical structures and shown to be a useful alternative for lead discovery. The TRAP screening process is described and two example applications are presented: I. the discovery of novel inhibitors of human intestinal carboxylesterase, and II. the discovery of novel inhibitors of cyclooxygenase-1 through the use of the affinity fingerprints of known cyclooxygenase-1 inhibitors. A summary of the complementary advantages of TRAP screening technology compared to traditional approaches to drug lead discovery concludes the review.


Rights & Permissions Print Cite
© 2024 Bentham Science Publishers | Privacy Policy