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.

2c90

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:2c90.gif|left|200px]]
+
{{Seed}}
 +
[[Image:2c90.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_2c90| PDB=2c90 | SCENE= }}
{{STRUCTURE_2c90| PDB=2c90 | SCENE= }}
-
'''THROMBIN INHIBITORS'''
+
===THROMBIN INHIBITORS===
-
==Overview==
+
<!--
-
The screening of fragments is an alternative approach to high-throughput screening for the identification of leads for therapeutic targets. Fragment hits have been discovered using X-ray crystallographic screening of protein crystals of the serine protease enzyme thrombin. The fragment library was designed to avoid any well-precedented, strongly basic functionality. Screening hits included a novel ligand (3), which binds exclusively to the S2-S4 pocket, in addition to smaller fragments which bind to the S1 pocket. The structure of these protein-ligand complexes are presented. A chemistry strategy to link two such fragments together and to synthesize larger drug-sized compounds resulted in the efficient identification of hybrid inhibitors with nanomolar potency (e.g., 7, IC50 = 3.7 nM). These potent ligands occupy the same area of the active site as previously described peptidic inhibitors, while having very different chemical architecture.
+
The line below this paragraph, {{ABSTRACT_PUBMED_16480269}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 16480269 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_16480269}}
==About this Structure==
==About this Structure==
Line 49: Line 53:
[[Category: Thrombin]]
[[Category: Thrombin]]
[[Category: Zymogen]]
[[Category: Zymogen]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 21:28:33 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 14:15:54 2008''

Revision as of 11:15, 27 July 2008

Image:2c90.png

Template:STRUCTURE 2c90

THROMBIN INHIBITORS

Template:ABSTRACT PUBMED 16480269

About this Structure

2C90 is a Protein complex structure of sequences from Hirudo medicinalis and Homo sapiens. Full crystallographic information is available from OCA.

Reference

Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors., Howard N, Abell C, Blakemore W, Chessari G, Congreve M, Howard S, Jhoti H, Murray CW, Seavers LC, van Montfort RL, J Med Chem. 2006 Feb 23;49(4):1346-55. PMID:16480269

Page seeded by OCA on Sun Jul 27 14:15:54 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2c90"
Personal tools