6LRY

Crystal structure of human endothelin ETB receptor in complex with sarafotoxin S6b

Summary for 6LRY

• Entry DOI: 10.2210/pdb6lry/pdb
• Descriptor: Endothelin receptor type B,Endolysin,Endothelin receptor type B, Sarafotoxin-B (2 entities in total)
• Functional Keywords: alpha helical, signaling protein, membrane protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 59322.55

Authors

Izume, T.,Miyauchi, H.,Shihoya, W.,Nureki, O. (deposition date: 2020-01-16, release date: 2020-02-12, Last modification date: 2024-10-16)

Primary citation

Izume, T.,Miyauchi, H.,Shihoya, W.,Nureki, O.
Crystal structure of human endothelin ETBreceptor in complex with sarafotoxin S6b.
Biochem.Biophys.Res.Commun., 528:383-388, 2020

PubMed Abstract: Sarafotoxins (SRTXs) are endothelin-like peptides extracted from snake venom. SRTXs stimulate the endothelin ET and ET 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 ET receptor in complex with the non-selective sarafotoxin S6b at 3.0 Å 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.

PubMed: 32001000
DOI: 10.1016/j.bbrc.2019.12.091

Experimental method

X-RAY DIFFRACTION (3 Å)