8AYH

Structure of Complement C5 in Complex with small molecule inhibitor and CVF

「6I2X」から置き換えられました

8AYH の概要

• エントリーDOI: 10.2210/pdb8ayh/pdb
• EMDBエントリー: 15713
• 分子名称: Complement C5 beta chain, Complement C5 alpha chain, Cobra venom factor, ... (5 entities in total)
• 機能のキーワード: inhibitor, protease, complex, cryo-em, toxin, immune system
• 由来する生物種: Homo sapiens (human); 詳細
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 371446.33

構造登録者

Srinivas, H. (登録日: 2022-09-02, 公開日: 2022-12-21, 最終更新日: 2024-10-09)

主引用文献

Jendza, K.,Kato, M.,Salcius, M.,Srinivas, H.,De Erkenez, A.,Nguyen, A.,McLaughlin, D.,Be, C.,Wiesmann, C.,Murphy, J.,Bolduc, P.,Mogi, M.,Duca, J.,Namil, A.,Capparelli, M.,Darsigny, V.,Meredith, E.,Tichkule, R.,Ferrara, L.,Heyder, J.,Liu, F.,Horton, P.A.,Romanowski, M.J.,Schirle, M.,Mainolfi, N.,Anderson, K.,Michaud, G.A.
A small-molecule inhibitor of C5 complement protein.
Nat.Chem.Biol., 15:666-668, 2019

PubMed Abstract: The complement pathway is an important part of the immune system, and uncontrolled activation is implicated in many diseases. The human complement component 5 protein (C5) is a validated drug target within the complement pathway, as an anti-C5 antibody (Soliris) is an approved therapy for paroxysmal nocturnal hemoglobinuria. Here, we report the identification, optimization and mechanism of action for the first small-molecule inhibitor of C5 complement protein.

PubMed: 31209353
DOI: 10.1038/s41589-019-0303-9

実験手法

ELECTRON MICROSCOPY (3.35 Å)