Assay Development for Protein Kinase Enzymes

J. Fraser Glickman  1 ,  Sarine Markossian  1 ,  Abigail Grossman  1 ,  Hannah Baskir  1 ,  Michelle Arkin  2 ,  Douglas Auld  3 ,  Christopher Austin  4 ,  Jonathan Baell  5 ,  Kyle Brimacombe  1 ,  Thomas D.Y. Chung  6 ,  Nathan P. Coussens  7 ,  Jayme L. Dahlin  8 ,  Viswanath Devanarayan  9 ,  Timothy L. Foley  10 ,  Marcie Glicksman  11 ,  Kirill Gorshkov  12 ,  Stefan Grotegut  13 ,  Matthew D. Hall  1 ,  Samuel Hoare  14 ,  James Inglese  1 ,  Philip W. Iversen  15 ,  Madhu Lal-Nag  16 ,  Zhuyin Li  12 ,  Jason R. Manro  13 ,  James McGee  17 ,  Allison Norvil  13 ,  Mackenzie Pearson  13 ,  Terry Riss  18 ,  Peter Saradjian  19 ,  G. Sitta Sittampalam  20 ,  Michael A. Tarselli  21 ,  O. Joseph Trask Jr.  22 ,  Jeffrey R. Weidner  23 ,  Mary Jo Wildey  24 ,  Kelli Wilson  1 ,  Menghang Xia  1 ,  Xin Xu  1
Affiliations
  • 1. The Rockefeller University, New York, NY, 10065
PMID: 22553863
Abstract

Kinases are important drug targets that control cell growth, proliferation, differentiation and metabolism. This process involves phosphorylation of multiple substrates in cellular signal transduction pathways. Here, the authors provide a synopsis on assay technologies, mechanistic considerations for assay design and development pertaining to kinase Enzymes. This chapter, along with some of the earlier chapters in this manual on basics of enzyme assays, mechanism of action and purity and identity considerations, serves as an excellent resource for beginners in HTS applications.