Structural and dynamic insights into agonist recognition and function of the thromboxane A2 receptor - PubMed
3 hours ago
- #Structural Biology
- #Thromboxane A2 Receptor
- #GPCR
- The thromboxane A2 receptor (TP) is crucial for blood clotting and muscle contraction.
- TP's natural ligand, thromboxane A2 (TXA2), is short-lived, making structural studies challenging.
- Structures of TP with synthetic agonists U46619 and I-BOP were determined in complex with Gq.
- The study reveals a unique activation switch in TP, differing from typical class A GPCRs.
- Functional studies, mutational analysis, and MD simulations explore agonist vs. antagonist binding.
- A molecular gate formed by two transmembrane helices facilitates ligand entry from the membrane.
- Findings aid in designing TP-targeting compounds and understanding TP-related inherited disorders.