2c93

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{{STRUCTURE_2c93| PDB=2c93 | SCENE= }}
{{STRUCTURE_2c93| PDB=2c93 | SCENE= }}
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'''THROMBIN INHIBITORS'''
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===THROMBIN INHIBITORS===
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==Overview==
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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.
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(as it appears on PubMed at http://www.pubmed.gov), where 16480269 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16480269}}
==About this Structure==
==About this Structure==
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[[Category: Serine protease]]
[[Category: Serine protease]]
[[Category: Thrombin]]
[[Category: Thrombin]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 15:19:45 2008''

Revision as of 12:19, 29 July 2008

Image:2c93.png

Template:STRUCTURE 2c93

THROMBIN INHIBITORS

Template:ABSTRACT PUBMED 16480269

About this Structure

2C93 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 Tue Jul 29 15:19:45 2008

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