Chemical kinomics: A powerful strategy for target deconvolution

Do Hee Kim, Taebo Sim

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

Kinomics is an emerging and promising approach for deciphering kinomes. Chemical kinomics is a discipline of chemical genomics that is also referred to as "chemogenomics", which is derived from chemistry and biology. Chemical kinomics has become a powerful approach to decipher complicated phosphorylation-based cellular signaling networks with the aid of small molecules that modulate kinase functions. Moreover, chemical kinomics has played a pivotal role in the field of kinase drug discovery as it enables identification of new molecular targets of small molecule kinase modulators and/or exploitation of novel functions of known kinases and has also provided novel chemical entities as hit/lead compounds. In this short review, contemporary chemical kinomics technologies such as activity-based protein profiling, T7 kinasetagged phages, kinobeads, three-hybrid systems, fluorescenttagged kinase binding assays, and chemical genomic profiling are discussed along with a novel allosteric Bcr-Abl kinase inhibitor (GNF-2/GNF-5) as a successful application of chemical kinomics approaches.

Original languageEnglish
Pages (from-to)711-719
Number of pages9
JournalBMB Reports
Volume43
Issue number11
DOIs
Publication statusPublished - 2010 Nov 1

Keywords

  • Chemical kinomics
  • Kinase inhibitor
  • Protein kinase
  • Target identification

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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