High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.
Acta Crystallogr Sect F Struct Biol Cryst Commun
; 68(Pt 4): 404-8, 2012 Apr 01.
Article
in En
| MEDLINE
| ID: mdl-22505407
ABSTRACT
Factor XI (FXI) is a key enzyme in the coagulation pathway and an attractive target for the development of anticoagulant drugs. A small number of high-resolution crystal structures of FXIa in complex with small synthetic inhibitors have been published to date. All of these ligands have a basic P1 group and bind exclusively in the nonprime side of the active site of FXIa. Here, two structures of FXIa in complex with nonbasic inhibitors that occupy both the prime and nonprime sides of the active site are presented. These new structures could be valuable in the design and optimization of new FXIa synthethic inhibitors.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Factor XIa
/
Enzyme Inhibitors
/
Protein Interaction Domains and Motifs
Type of study:
Prognostic_studies
Limits:
Humans
Language:
En
Journal:
Acta Crystallogr Sect F Struct Biol Cryst Commun
Year:
2012
Type:
Article
Affiliation country:
United kingdom