7wit

Structure of SUR1 in complex with mitiglinideStructure of SUR1 in complex with mitiglinide

Structural highlights 7wit is a 1 chain structure with sequence from Bos taurus and Mesocricetus auratus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: , Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function A0A1U8CME7_MESAU A2VDS4_BOVIN Publication Abstract from PubMed Mitiglinide is a highly selective fast-acting anti-diabetic drug that induces insulin secretion by inhibiting pancreatic KATP channels. However, how mitiglinide binds KATP channels remains unknown. Here, we show the cryo-EM structure of the SUR1 subunit complexed with mitiglinide. The structure reveals that mitiglinide binds inside the common insulin secretagogue-binding site of SUR1, which is surrounded by TM7, TM8, TM16, and TM17. Mitiglinide locks SUR1 in the NBD-separated inward-facing conformation. The detailed structural analysis of the mitiglinide-binding site uncovers the molecular basis of its high selectivity. Structural Insights Into the High Selectivity of the Anti-Diabetic Drug Mitiglinide.,Wang M, Wu JX, Chen L Front Pharmacol. 2022 Jun 30;13:929684. doi: 10.3389/fphar.2022.929684., eCollection 2022. PMID:35847046 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

spinqualitylabelsall models 7wit, resolution 3.21Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image