Design and Selection of Novel C1s Inhibitors by In Silico and In Vitro Approaches.

ABSTRACT: The complement system is associated with various diseases such as inflammation or auto-immune diseases. Complement-targeted drugs could provide novel therapeutic intervention against the above diseases. C1s, a serine protease, plays an important role in the CS and could be an attractive target since it blocks the system at an early stage of the complement cascade. Designing C1 inhibitors is particularly challenging since known inhibitors are restricted to a narrow bioactive chemical space in addition selectivity over other serine proteases is an important requirement. The typical architecture of a small molecule inhibitor of C1s contains an amidine (or guanidine) residue, however, the discovery of non-amidine inhibitors might have high value, particularly if novel chemotypes and/or compoun

SUBMITTER: Szilagyi K 

PROVIDER: S-EPMC6832932 | biostudies-literature | 2019 Oct

REPOSITORIES: biostudies-literature