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-Structure paper
Title | A small-molecule inhibitor of C5 complement protein. |
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Journal, issue, pages | Nat Chem Biol, Vol. 15, Issue 7, Page 666-668, Year 2019 |
Publish date | Jun 17, 2019 |
Authors | 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 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 ...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. |
External links | Nat Chem Biol / PubMed:31209353 |
Methods | EM (single particle) |
Resolution | 3.35 Å |
Structure data | EMDB-15713, PDB-8ayh: |
Chemicals | ChemComp-H1H: ChemComp-MG: |
Source |
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Keywords | IMMUNE SYSTEM / Inhibitor / Protease / Complex / Cryo-EM / Toxin |