A small-molecule inhibitor of C5 complement protein.

Keith JendzaMitsunori KatoMichael SalciusHonnappa SrinivasAndrea De ErkenezAnh NguyenDoug McLaughlinCeline BeChristian WiesmannJason MurphyPhilippe BolducMuneto MogiJose DucaAbdel NamilMichael CapparelliVeronique DarsignyErik MeredithRitesh TichkuleLuciana FerraraJessica HeyderFang LiuPatricia A HortonMichael J RomanowskiMarkus SchirleNello MainolfiKaren AndersonGregory A Michaud

Published in: Nature chemical biology (2019)

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.

Keyphrases

small molecule
protein protein
endothelial cells
amino acid
blood pressure
obstructive sleep apnea
atrial fibrillation
emergency department
depressive symptoms
adverse drug
sleep apnea
catheter ablation