Author: Scapin, Giovanna

Source: Current Drug Targets, Volume 7, Number 11, November 2006 , pp. 1443-1454(12)

Publisher: Bentham Science Publishers

Abstract:

Protein kinases represent a large family of enzymes involved in regulating complex molecular machineries that control many cellular functions, from survival and proliferation to apoptosis. Abnormal protein kinase activity has been involved in a variety of pathophysiologic states, including cancer, inflammatory and autoimmune disorders, and cardiac diseases, and protein kinases have become one of the major therapeutical targets of the past 10 years. The major problem associated with ATP-competitive kinase inhibition is target specificity, since many other enzymes, kinases and not-kinases alike, utilize ATP: less specific inhibitors would be expected to exhibit undesirable toxicities that would limit their potential utility as therapeutic agents. The purpose of this review is to offer the reader an idea of the evolution of the methodologies utilized in the quest for selective kinase inhibitors, from the more traditional, screening-based methods to the newer technology of chemogenomics, proteomics and chemical genetics.

Keywords: protein kinase inhibition; specificity; ATP-competitive; substrate-competitive; chemogenomics; focused library; structural biology

Document Type: Research article

Affiliations: 1: Department of Medicinal Chemistry, MRL, Merck & Co., Inc. PO BOX 2000, Rahway, NJ, 07065,USA.

Publication date: 2006-11-01

More about this publication?

• Current Drug Targets aims to cover the latest and most outstanding developments on the medicinal chemistry and pharmacology of molecular drug targets e.g. disease specific proteins, receptors, enzymes, genes. Each issue of the journal will be devoted to a single timely topic, with series of in-depth reviews, written by leaders in the field, covering a range of current topics on drug targets. These issues will be organized and led by a guest editor who is a recognized expert in the overall topic. As the discovery, identification, characterisation and validation of novel human drug targets for drug discovery continues to grow; this journal will be essential reading for all pharmaceutical scientists involved in drug discovery and development.

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