We apologize for Proteopedia being slow to respond. For the past two years, a new implementation of Proteopedia has been being built. Soon, it will replace this 18-year old system. All existing content will be moved to the new system at a date that will be announced here.

1fax

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 27: Line 27:
[[Category: serine protease]]
[[Category: serine protease]]
-
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 12:02:35 2007''
+
''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 15:11:52 2007''

Revision as of 13:07, 30 October 2007

Image:1fax.gif

1fax, resolution 3.0Å

Drag the structure with the mouse to rotate

COAGULATION FACTOR XA INHIBITOR COMPLEX

Overview

The 3.0-A resolution x-ray structure of human des-Gla-coagulation factor, Xa (fXa) has been determined in complex with the synthetic inhibitor, DX-9065a. The binding geometry is characterized primarily by two, interaction sites: the naphthamidine group is fixed in the S1 pocket by a, typical salt bridge to Asp-189, while the pyrrolidine ring binds in the, unique aryl-binding site (S4) of fXa. Unlike the large majority of, inhibitor complexes with serine proteinases, Gly-216 (S3) does not, contribute to hydrogen bond formation. In contrast to typical thrombin, binding modes, the S2 site of fXa cannot be used by DX-9065a since it is, blocked by Tyr-99, and the aryl-binding site (S4) of fXa is lined by, carbonyl oxygen atoms that can accommodate positive charges. This has, implications for ... [(full description)]

About this Structure

1FAX is a [Protein complex] structure of sequences from [Homo sapiens] with CA and DX9 as [ligands]. Active as [Coagulation factor Xa], with EC number [3.4.21.6]. Structure known Active Site: CAT. Full crystallographic information is available from [OCA].

Reference

X-ray structure of active site-inhibited clotting factor Xa. Implications for drug design and substrate recognition., Brandstetter H, Kuhne A, Bode W, Huber R, von der Saal W, Wirthensohn K, Engh RA, J Biol Chem. 1996 Nov 22;271(47):29988-92. PMID:8939944

Page seeded by OCA on Tue Oct 30 15:11:52 2007

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1fax"
Personal tools