Unit

UNIT 9.5 Screening in Constitutively Active Receptor Systems

  1. Terry Kenakin

Published Online: 1 MAY 2001

DOI: 10.1002/0471141755.ph0905s12

Current Protocols in Pharmacology

Current Protocols in Pharmacology

How to Cite

Kenakin, T. 2001. Screening in Constitutively Active Receptor Systems. Current Protocols in Pharmacology. 9:9.5.

Author Information

  1. GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina

Publication History

  1. Published Online: 1 MAY 2001
  2. Published Print: MAR 2001

This is not the most recent version of the article. View current version (1 APR 2006)

Abstract

This unit discusses the use of constitutive G protein-coupled receptor (GPCR) activity for the screening of new drug entities. It begins with an introduction to constitutive GPCR activity and then centers on the three basic components of a constitutive screening system, namely the receptor, the receptor coupling components (G protein) and the response reporting system. Then, the influence of ligands and particular application of such systems to drug screening, with reference to optimal conditions, is discussed. Finally, the relative advantages and disadvantages of constitutive screening are considered. This unit discusses the use of constitutive G protein-coupled receptor (GPCR) activity for the screening of new drug entities