Recent developments in low molecular weight complement inhibitors.
As a key part of the innate immune system, complement plays an important role not only in defending against invading pathogens but also in many other biological processes. Inappropriate or excessive activation of complement has been linked to many autoimmune, inflammatory, and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer. A wide array of low molecular weight complement inhibitors has been developed to target various components of the complement cascade. Their efficacy has been demonstrated in numerous in vitro and in vivo experiments. Though none of these inhibitors has reached the market so far, some of them have entered clinical trials and displayed promising results. This review provides a brief overview of the currently developed low molecular weight complement inhibitors, including short peptides and synthetic small molecules, with an emphasis on those targeting components C1 and C3, and the anaphylatoxin receptors.
Department of Pathology and Laboratory Medicine, School of Medicine, University of Pennsylvania, 401 Stellar Chance, 422 Curie Blvd., Philadelphia, PA 19104, USA.
Hongchang
H
Qu
Daniel
D
Ricklin
John D
JD
Lambris
D000818:Animals; D003169:Complement Inactivator Proteins / Q000276:immunology*; D003165:Complement System Proteins / Q000276:immunology*; D006801:Humans; D008958:Models, Molecular; D011485:Protein Binding / Q000276:immunology; D011951:Receptors, Complement / Q000276:immunology; D057057:Serine Proteases / Q000276:immunology
D003169:Complement Inactivator Proteins; D011951:Receptors, Complement; C028751:low molecular weight inhibitor (complement); D003165:Complement System Proteins; D057057:Serine Proteases