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

Fingerprint

Deconvolution
Phosphotransferases
Cell signaling
Lead compounds
Bacteriophage T7
Phosphorylation
Molecules
Bacteriophages
Drug Discovery
Genomics
Hybrid systems
Modulators
Assays
Technology
Proteins

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

Cite this

Chemical kinomics : A powerful strategy for target deconvolution. / Kim, Do Hee; Sim, Taebo.

In: BMB Reports, Vol. 43, No. 11, 01.11.2010, p. 711-719.

Research output: Contribution to journalArticle

Kim, Do Hee ; Sim, Taebo. / Chemical kinomics : A powerful strategy for target deconvolution. In: BMB Reports. 2010 ; Vol. 43, No. 11. pp. 711-719.
@article{40eb033972bc4cd5bdefaa6ce0dbeb69,
title = "Chemical kinomics: A powerful strategy for target deconvolution",
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.",
keywords = "Chemical kinomics, Kinase inhibitor, Protein kinase, Target identification",
author = "Kim, {Do Hee} and Taebo Sim",
year = "2010",
month = "11",
day = "1",
doi = "10.3858/BMBRep.2010.43.11.711",
language = "English",
volume = "43",
pages = "711--719",
journal = "BMB Reports",
issn = "1976-6696",
publisher = "The Biochemical Society of the Republic of Korea",
number = "11",

}

TY - JOUR

T1 - Chemical kinomics

T2 - A powerful strategy for target deconvolution

AU - Kim, Do Hee

AU - Sim, Taebo

PY - 2010/11/1

Y1 - 2010/11/1

N2 - 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.

AB - 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.

KW - Chemical kinomics

KW - Kinase inhibitor

KW - Protein kinase

KW - Target identification

UR - http://www.scopus.com/inward/record.url?scp=78649790001&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=78649790001&partnerID=8YFLogxK

U2 - 10.3858/BMBRep.2010.43.11.711

DO - 10.3858/BMBRep.2010.43.11.711

M3 - Article

C2 - 21110913

AN - SCOPUS:78649790001

VL - 43

SP - 711

EP - 719

JO - BMB Reports

JF - BMB Reports

SN - 1976-6696

IS - 11

ER -