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G-Protein–Coupled Receptors Signaling Pathways in New Antiplatelet Drug Development
| Content Provider | Scilit |
|---|---|
| Author | Gurbel, Paul A. Kuliopulos, Athan Tantry, Udaya S. |
| Copyright Year | 2015 |
| Description | Journal: Arteriosclerosis, thrombosis, and vascular biology Platelet G-protein–coupled receptors influence platelet function by mediating the response to various agonists, including ADP, thromboxane A$ _{2}$ , and thrombin. Blockade of the ADP receptor, P2Y$ _{12}$ , in combination with cyclooxygenase-1 inhibition by aspirin has been among the most widely used pharmacological strategies to reduce cardiovascular event occurrence in high-risk patients. The latter dual pathway blockade strategy is one of the greatest advances in the field of cardiovascular medicine. In addition to P2Y$ _{12}$ , the platelet thrombin receptor, protease activated receptor-1, has also been recently targeted for inhibition. Blockade of protease activated receptor-1 has been associated with reduced thrombotic event occurrence when added to a strategy using P2Y$ _{12}$ and cyclooxygenase-1 inhibition. At this time, the relative contributions of these G-protein–coupled receptor signaling pathways to in vivo thrombosis remain incompletely defined. The observation of treatment failure in ≈10% of high-risk patients treated with aspirin and potent P2Y$ _{12}$ inhibitors provides the rationale for targeting novel pathways mediating platelet function. Targeting intracellular signaling downstream from G-protein–coupled receptor receptors with phosphotidylionisitol 3-kinase and Gq inhibitors are among the novel strategies under investigation to prevent arterial ischemic event occurrence. Greater understanding of the mechanisms of G-protein–coupled receptor–mediated signaling may allow the tailoring of antiplatelet therapy. |
| Related Links | https://www.ahajournals.org/doi/pdf/10.1161/ATVBAHA.114.303412 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4836833/pdf https://www.ahajournals.org/doi/reader/10.1161/ATVBAHA.114.303412 |
| Ending Page | 512 |
| Page Count | 13 |
| Starting Page | 500 |
| ISSN | 10795642 |
| e-ISSN | 15244636 |
| DOI | 10.1161/atvbaha.114.303412 |
| Journal | Arteriosclerosis, thrombosis, and vascular biology |
| Issue Number | 3 |
| Volume Number | 35 |
| Language | English |
| Publisher | Ovid Technologies (Wolters Kluwer Health) |
| Publisher Date | 2015-03-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Arteriosclerosis, thrombosis, and vascular biology Peripheral Vascular Disease Purinerginc 2y12 Receptor Agoists Gtp-binding Proteins Blood Platelet Coronary Disease |
| Content Type | Text |
| Resource Type | Article |
| Subject | Cardiology and Cardiovascular Medicine |
