192 pages

Date published 
October 2008

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GPCR Report Overview


Brochure CoverGPCRs: Dawn of a New Era?

Author: Ken Rubenstein, PhD





Current advances in functional screening methodologies, medicinal chemistry, and structure-based drug design have generated large increases in the number and diversity of GPCR drug targets. Furthermore, basic research advances have opened the way for still further exploitation of this target class. This report:

  • Explores current and likely consequences of recent advances concerning GPCR x-ray structures, allosteric interactions, multimerization, and functional selectivity;
  • Extensively tabulates marketed drugs and compounds in development arranged by receptor type and subtype;
  • Presents in-depth interviews with recognized experts in the field.

G protein-coupled receptors (GPCRs) are popular drug targets, accounting for about one-third of approved drugs and many hundreds of drugs currently in development. Yet one can easily argue that the pharmacologic potential of GPCRs is far from exhausted. Currently approved drugs address only a few GPCRs. Technologic and scientific advances have resulted in R&D pipelines that target a great many more GPCRs than are represented among currently marketed products. In this report, we examine newer technologies used in GPCR pharmacology.

Furthermore, the evolution of GPCR pharmacology is far from over. Basic researchers have made a number of exciting and relevant discoveries in the past decade, and these have already begun to make important contributions to drug discovery. GPCRs: Dawn of a New Era? examines the current state of basic research, featuring key developments with the potential to favorably impact future drug discovery.

We consider the exciting area of allosteric modulation, which has already yielded two marketed drugs and promises many more, some with capabilities heretofore inaccessible. We also examine two other areas in basic research that promise to have significant impact on the field: functional selectivity and the role of homo- and heterodimers in GPCR function.
Another basic research advance, described herein, has, arguably, the greatest potential for advancing GPCR pharmacology. Until this year, drug discovery scientists had available to them only a single high-resolution x-ray crystallographic structure of a GPCR. That was for rhodopsin, which is atypical from the drug discovery perspective. Two relevant structures have become available, thus energizing the GPCR structure-based drug design community.


GPCRs: Dawn of a New Era? then examines trends in applied GPCR research before turning to a thorough presentation and analysis of marketed GPCR-based drugs and of compounds currently in development or registration. We consider all GPCR types and subtypes that are the subject of approved drugs or pipeline candidates.
The report spotlights numerous small pharmaceutical companies, which tend to push the limits of GPCR pharmacology by attacking more targets and by attempting to apply cutting-edge concepts derived from basic research. In addition, we present a compendium of views on a variety of relevant findings and issues in the field based on our extensive discussions with GPCR experts.

About the author:Ken Rubenstein, PhD, a biochemist and molecular biologist, received his PhD at the University of Wisconsin and postdoctoral training at the University of Pennsylvania School of Medicine. He was a key innovator and research manager for Syva Company, the diagnostics branch of Syntex Corporation. During his 13 years with Syva, Dr. Rubenstein became vice president, scientific affairs, a function that included strategic planning. Since 1983, he has served as a technology and marketing consultant to biomedical companies and an industry analyst, with more than 40 published studies to his credit.