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G Protein-coupled Receptor Biased Agonism.

Publication ,  Journal Article
Hodavance, SY; Gareri, C; Torok, RD; Rockman, HA
Published in: J Cardiovasc Pharmacol
March 2016

G protein-coupled receptors are the largest family of targets for current therapeutics. The classic model of their activation was binary, where agonist binding induced an active conformation and subsequent downstream signaling. Subsequently, the revised concept of biased agonism emerged, where different ligands at the same G protein-coupled receptor selectively activate one downstream pathway versus another. Advances in understanding the mechanism of biased agonism have led to the development of novel ligands, which have the potential for improved therapeutic and safety profiles. In this review, we summarize the theory and most recent breakthroughs in understanding biased signaling, examine recent laboratory investigations concerning biased ligands across different organ systems, and discuss the promising clinical applications of biased agonism.

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Published In

J Cardiovasc Pharmacol

DOI

EISSN

1533-4023

Publication Date

March 2016

Volume

67

Issue

3

Start / End Page

193 / 202

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Conformation
  • Protein Binding
  • Molecular Targeted Therapy
  • Ligands
  • Humans
  • Drug Discovery
  • Cardiovascular System & Hematology
 

Citation

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Hodavance, S. Y., Gareri, C., Torok, R. D., & Rockman, H. A. (2016). G Protein-coupled Receptor Biased Agonism. J Cardiovasc Pharmacol, 67(3), 193–202. https://doi.org/10.1097/FJC.0000000000000356
Hodavance, Sima Y., Clarice Gareri, Rachel D. Torok, and Howard A. Rockman. “G Protein-coupled Receptor Biased Agonism.J Cardiovasc Pharmacol 67, no. 3 (March 2016): 193–202. https://doi.org/10.1097/FJC.0000000000000356.
Hodavance SY, Gareri C, Torok RD, Rockman HA. G Protein-coupled Receptor Biased Agonism. J Cardiovasc Pharmacol. 2016 Mar;67(3):193–202.
Hodavance, Sima Y., et al. “G Protein-coupled Receptor Biased Agonism.J Cardiovasc Pharmacol, vol. 67, no. 3, Mar. 2016, pp. 193–202. Pubmed, doi:10.1097/FJC.0000000000000356.
Hodavance SY, Gareri C, Torok RD, Rockman HA. G Protein-coupled Receptor Biased Agonism. J Cardiovasc Pharmacol. 2016 Mar;67(3):193–202.

Published In

J Cardiovasc Pharmacol

DOI

EISSN

1533-4023

Publication Date

March 2016

Volume

67

Issue

3

Start / End Page

193 / 202

Location

United States

Related Subject Headings

  • Structure-Activity Relationship
  • Signal Transduction
  • Receptors, G-Protein-Coupled
  • Protein Conformation
  • Protein Binding
  • Molecular Targeted Therapy
  • Ligands
  • Humans
  • Drug Discovery
  • Cardiovascular System & Hematology