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-Structure paper
タイトル | A small-molecule inhibitor of C5 complement protein. |
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ジャーナル・号・ページ | Nat Chem Biol, Vol. 15, Issue 7, Page 666-668, Year 2019 |
掲載日 | 2019年6月17日 |
著者 | Keith Jendza / Mitsunori Kato / Michael Salcius / Honnappa Srinivas / Andrea De Erkenez / Anh Nguyen / Doug McLaughlin / Celine Be / Christian Wiesmann / Jason Murphy / Philippe Bolduc / Muneto Mogi / Jose Duca / Abdel Namil / Michael Capparelli / Veronique Darsigny / Erik Meredith / Ritesh Tichkule / Luciana Ferrara / Jessica Heyder / Fang Liu / Patricia A Horton / Michael J Romanowski / Markus Schirle / Nello Mainolfi / Karen Anderson / Gregory A Michaud / |
PubMed 要旨 | 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 ...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. |
リンク | Nat Chem Biol / PubMed:31209353 |
手法 | EM (単粒子) |
解像度 | 3.35 Å |
構造データ | EMDB-15713, PDB-8ayh: |
化合物 | ChemComp-H1H: ChemComp-MG: |
由来 |
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キーワード | IMMUNE SYSTEM / Inhibitor / Protease / Complex / Cryo-EM / Toxin |