7c61
From Proteopedia
Crystal structure of 5-HT1B-BRIL and SRP2070_Fab complex
Structural highlights
FunctionC562_ECOLX Electron-transport protein of unknown function.5HT1B_HUMAN This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. The activity of this receptor is mediated by G proteins that inhibit adenylate cyclase activity. Publication Abstract from PubMedG-protein-coupled receptors (GPCRs)-the largest family of cell-surface membrane proteins-mediate the intracellular signal transduction of many external ligands. Thus, GPCRs have become important drug targets. X-ray crystal structures of GPCRs are very useful for structure-based drug design (SBDD). Herein, we produced a new antibody (SRP2070) targeting the thermostabilised apocytochrome b562 from Escherichia coli M7W/H102I/R106L (BRIL). We found that a fragment of this antibody (SRP2070Fab) facilitated the crystallisation of the BRIL-tagged, ligand bound GPCRs, 5HT(1B) and AT(2)R. Furthermore, the electron densities of the ligands were resolved, suggesting that SPR2070Fab is versatile and adaptable for GPCR SBDD. We anticipate that this new tool will significantly accelerate structure determination of other GPCRs and the design of small molecular drugs targeting them. The discovery of a new antibody for BRIL-fused GPCR structure determination.,Miyagi H, Asada H, Suzuki M, Takahashi Y, Yasunaga M, Suno C, Iwata S, Saito JI Sci Rep. 2020 Jul 15;10(1):11669. doi: 10.1038/s41598-020-68355-x. PMID:32669569[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. Loading citation details.. Citations No citations found See AlsoReferences
|
| |||||||||||||||||||
Categories: Escherichia coli | Homo sapiens | Large Structures | Mus musculus | Asada H | Iwata S | Miyagi H | Saito J | Suno C | Suzuki M | Takahashi Y | Yasunaga M
