UNIT 9.5 Screening in Constitutively Active Receptor Systems
Published Online: 1 MAY 2001
Copyright © 2003 by John Wiley and Sons, Inc.
Lab Protocol Title
Current Protocols in Pharmacology
How to Cite
Kenakin, T. 2001. Screening in Constitutively Active Receptor Systems. Current Protocols in Pharmacology. 9:9.5.
- Published Online: 1 MAY 2001
- Published Print: MAR 2001
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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