The crystal structures of human α-thrombin complexed with active site-directed diamino benzo[b]thiophene derivatives: A binding mode for a structurally novel class of inhibitors

The crystal structures of four active site-directed thrombin inhibitors, 1–4, in a complex with human α-thrombin have been determined and refined at up to 2.0 Å resolution using X-ray crystallography. These compounds belong to a structurally novel family of inhibitors based on a 2,3-disubstituted be...

Ausführliche Beschreibung

Bibliographische Detailangaben

Veröffentlicht in:	Protein science 2000-01, Vol.9 (1), p.29-36
Hauptverfasser:	CHIRGADZE, N.Y., SALL, D.J., BRIGGS, S.L., CLAWSON, D.K., ZHANG, M., SMITH, G.F., SCHEVITZ, R.W.
Format:	Artikel
Sprache:	eng
Schlagworte:	benzo[b]thiophene Binding Sites Crystallography, X-Ray Enzyme Inhibitors - chemistry human α‐thrombin Humans Models, Molecular nonpeptidyl inhibitor Structure-Activity Relationship structure‐based drug design Thiophenes - chemistry Thrombin - antagonists & inhibitors Thrombin - chemistry X‐ray crystallography
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!