Structure-function studies with G protein-coupled receptors as a paradigm for improving drug discovery and therapeutic development

Details

• Alternative Title:
  Biotechnol J
• Personal Author:
  McNeely, Patrick M. ; Naranjo, Andrea N. ; Robinson, Anne Skaja
• Description:
  There are a great variety of human membrane proteins, and these currently form the largest group of targets for marketed drugs. Despite the advances in drug design, however, promiscuity between drug molecules and targets often leads to undesired signaling effects, which result in unintended side effects. In this review, one family of membrane proteins - the G protein-coupled receptors (GPCRs) - is used as a model to review experimental techniques that may be used to examine the activity of membrane proteins. As these receptors are highly relevant to healthy human physiology and represent the largest family of drug targets, they represent an excellent model for membrane proteins in general. We also review experimental evidence that suggests there may be multiple ways to target a GPCR - and by extension, membrane proteins - to more effectively target unhealthy phenotypes while reducing the occurrence and severity of side effects.
• Subjects:
  • Article
  • Animals
  • Biopharmaceutics
  • Drug Discovery
  • Humans
  • Membrane Proteins
  • Models, Biological
  • Molecular Targeted Therapy
  • Receptors, G-Protein-Coupled
  • Structure-Activity Relationship
  More +
• Source:
  Biotechnol J. 7(12):1451-1461
• Pubmed ID:
  23213015
• Pubmed Central ID:
  PMC3739047
• Document Type:
  Journal Article
• Funding:
  T32 GM008550/GM/NIGMS NIH HHSUnited States/ ; T32 GH08550/GH/CGH CDC HHSUnited States/
• Volume:
  7
• Issue:
  12
• Download URL:
  https://stacks.cdc.gov/view/cdc/33610/cdc_33610_DS1.pdf
• File Type:
  [PDF - 732.22 KB]
• Collection(s):
  CDC Public Access
• Main Document Checksum:
  urn:sha256:d86f37746e0c477f4cc96b53b6e1050b002e1737e37faec05d8fb8d262125456