Targeting Cancer Using Fragment Based Drug Discovery

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)


Volume 16, 12 Issues, 2016


Download PDF Flyer




Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

Aims & ScopeAbstracted/Indexed in

Ranking and Category:
  • 27th of 59 in Chemistry, Medicinal

Submit Abstracts Online Submit Manuscripts Online

Editor-in-Chief:
Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex
France


View Full Editorial Board

Subscribe Purchase Articles Order Reprints

Current: 2.722
5 - Year: 2.849

Targeting Cancer Using Fragment Based Drug Discovery



Anti-Cancer Agents in Medicinal Chemistry, 12(1): 40-48.

Author(s): Andrew P. Turnbull and Susan M Boyd.

Affiliation: CRT Discovery Laboratories, Department of Crystallography, Birkbeck College, University of London, Malet Street, London, WC1E 7HX.

Abstract

Over the past decade, fragment-based drug discovery has developed significantly and has gained increasing popularity in the pharmaceutical industry as a powerful alternative and complement to traditional high-throughput screening approaches for hit identification. Fragment-based methods are capable of rapidly identifying starting points for structure-based drug design from relatively small libraries of low molecular weight compounds. The main constraints are the need for sensitive methods that can reliably detect the typically weak interactions between fragments and the target protein, and strategies for transforming fragments into higher molecular weight drug candidates. This approach has recently been validated as series of compounds from various programs have entered clinical trials.

Keywords:

Fragment screening, Ligand efficiency, Drug discovery, Cancer, high-throughput screening (HTS), Crystallography, fluorimetry, Phosphoinositide-Dependent Kinase-1 (PDK1), Anti-cancer, Cyclindependent kinase (CDK).



Download Free Order Reprints Order Eprints Rights and Permissions




Article Details

Volume: 12
Issue Number: 1
First Page: 40
Last Page: 48
Page Count: 9
DOI: 10.2174/187152012798764660
Advertisement

Related Journals




Webmaster Contact: urooj@benthamscience.org Copyright © 2016 Bentham Science