Protein kinase profiling assays: a technology review

Yuren Wang; Haiching Ma

doi:10.1016/j.ddtec.2015.10.007

Protein kinase profiling assays: a technology review

Drug Discov Today Technol. 2015 Nov:18:1-8. doi: 10.1016/j.ddtec.2015.10.007. Epub 2015 Oct 31.

Authors

Yuren Wang¹, Haiching Ma²

Affiliations

¹ Reaction Biology Corp., One Great Valley Parkway, Suite 2, Malvern, PA 19355, USA. Electronic address: yuren.wang@reactionbiology.com.
² Reaction Biology Corp., One Great Valley Parkway, Suite 2, Malvern, PA 19355, USA.

PMID: 26723886
DOI: 10.1016/j.ddtec.2015.10.007

Abstract

Protein kinases have become one of the most intensively pursued classes of drug targets for many diseases such as cancers and inflammatory diseases. Kinase profiling work seeks to understand general selectivity trends of lead compounds across the kinome, which help with target selection, compound prioritization, and potential implications in toxicity. Under the current drug discovery process, screening of compounds against comprehensive panels of kinases and their mutants has become the standard approach. Many screening assays and technologies which are compatible for high-throughput screening (HTS) against kinases have been extensively pursued and developed.

Publication types

Review

MeSH terms

Drug Discovery / instrumentation
Drug Discovery / methods*
Protein Binding
Protein Kinase Inhibitors / chemistry
Protein Kinase Inhibitors / pharmacology*
Protein Kinases* / genetics
Protein Kinases* / metabolism
Technology, Pharmaceutical / instrumentation
Technology, Pharmaceutical / methods*

Substances

Protein Kinase Inhibitors
Protein Kinases