Structure-Based Design of FXIIIa-Blockers: Addressing a Transient Hydrophobic Pocket in the Active Site of FXIIIa.

Blood coagulation factor XIII (FXIII, F13) is considered to be a promising target for anticoagulants with reduced bleeding risk because of its unique position in the coagulation cascade downstream of thrombin. However, until now, a potent drug addressing FXIII is not available and no compound even entered clinical trials yet. In 2013, we published the co-crystal structure of FXIII in the active state (FXIIIa degrees ), providing a detailed map of the active site for rational design of potent FXIIIa blockers.