Structural highlights
Publication Abstract from PubMed
Sarafotoxins (SRTXs) are endothelin-like peptides extracted from snake venom. SRTXs stimulate the endothelin ETA and ETB receptors and enhance vasoconstriction, followed by left ventricular dysfunction and bronchoconstriction. SRTXs include four major isopeptides, S6a-d, with different subtype selectivities. Here, we report the crystal structure of the human ETB receptor in complex with the non-selective sarafotoxin S6b at 3.0 A resolution. This structure reveals the similarities and differences between the binding modes of the endothelins and S6b. Moreover, molecular dynamics simulations based on the S6b-bound receptor provides structural insight into the subtype selectivity of the sarafotoxins. Our study clarifies the recognition mechanism of the endothelin-like peptide families.
Crystal structure of human endothelin ETB receptor in complex with sarafotoxin S6b.,Izume T, Miyauchi H, Shihoya W, Nureki O Biochem Biophys Res Commun. 2020 Jan 28. pii: S0006-291X(20)30021-8. doi:, 10.1016/j.bbrc.2019.12.091. PMID:32001000[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Izume T, Miyauchi H, Shihoya W, Nureki O. Crystal structure of human endothelin ETB receptor in complex with sarafotoxin S6b. Biochem Biophys Res Commun. 2020 Jan 28. pii: S0006-291X(20)30021-8. doi:, 10.1016/j.bbrc.2019.12.091. PMID:32001000 doi:http://dx.doi.org/10.1016/j.bbrc.2019.12.091
