International Union of Basic and Clinical Pharmacology. LXXXIII: classification of prostanoid receptors, updating 15 years of progress

• Published in: Pharmacological reviews Vol. 63; no. 3; pp. 471 - 538
• Main Authors: Woodward, D F, Jones, R L, Narumiya, S
• Format: Journal Article
• Language: English
• Published: United States 01-09-2011
• Subjects: Animals; Humans; International Agencies; Molecular Targeted Therapy; Prostaglandin Antagonists - therapeutic use; Prostaglandins - agonists; Prostaglandins - metabolism; Protein Isoforms - chemistry; Protein Isoforms - classification; Protein Isoforms - genetics; Protein Isoforms - metabolism; Receptors, Prostaglandin - chemistry; Receptors, Prostaglandin - classification; Receptors, Prostaglandin - genetics; Receptors, Prostaglandin - metabolism; Receptors, Thromboxane - chemistry; Receptors, Thromboxane - classification; Receptors, Thromboxane - genetics; Receptors, Thromboxane - metabolism; Second Messenger Systems - drug effects; Terminology as Topic; Thromboxanes - agonists; Thromboxanes - antagonists & inhibitors; Thromboxanes - metabolism
• ISSN: 0031-6997; 1521-0081
• DOI: 10.1124/pr.110.003517

It is now more than 15 years since the molecular structures of the major prostanoid receptors were elucidated. Since then, substantial progress has been achieved with respect to distribution and function, signal transduction mechanisms, and the design of agonists and antagonists (http://www.iuphar-db.org/DATABASE/FamilyIntroductionForward?familyId=58). This review systematically details these advances. More recent developments in prostanoid receptor research are included. The DP(2) receptor, also termed CRTH2, has little structural resemblance to DP(1) and other receptors described in the original prostanoid receptor classification. DP(2) receptors are more closely related to chemoattractant receptors. Prostanoid receptors have also been found to heterodimerize with other prostanoid receptor subtypes and nonprostanoids. This may extend signal transduction pathways and create new ligand recognition sites: prostacyclin/thromboxane A(2) heterodimeric receptors for 8-epi-prostaglandin E(2), wild-type/alternative (alt4) heterodimers for the prostaglandin FP receptor for bimatoprost and the prostamides. It is anticipated that the 15 years of research progress described herein will lead to novel therapeutic entities.