1sl3

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{{STRUCTURE_1sl3| PDB=1sl3 | SCENE= }}
{{STRUCTURE_1sl3| PDB=1sl3 | SCENE= }}
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'''crystal structue of Thrombin in complex with a potent P1 heterocycle-Aryl based inhibitor'''
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===crystal structue of Thrombin in complex with a potent P1 heterocycle-Aryl based inhibitor===
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==Overview==
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In an effort to discover potent, clinically useful thrombin inhibitors, a rapid analogue synthetic approach was used to explore the P(1) region. Various benzylamines were coupled to a pyridine/pyrazinone P(2)-P(3) template. One compound with an o-thiadiazole benzylic substitution was found to have a thrombin K(i) of 0.84 nM. A study of ortho-substituted five-membered-ring heterocycles was undertaken and subsequently demonstrated that the o-triazole and tetrazole rings were optimal. Combination of these potent P(1) aryl heterocycles with a variety of P(2)-P(3) groups produced a compound with an extraordinary thrombin inhibitory activity of 1.4 pM. It is hoped that this potency enhancement in P(1) will allow for more diversification in the P(2)-P(3) region to ultimately address additional pharmacological concerns.
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The line below this paragraph, {{ABSTRACT_PUBMED_15163182}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15163182 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15163182}}
==About this Structure==
==About this Structure==
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[[Category: Young, M B.]]
[[Category: Young, M B.]]
[[Category: Thrombin inhibitor complex]]
[[Category: Thrombin inhibitor complex]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 08:50:20 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Tue Jul 29 16:09:16 2008''

Revision as of 13:09, 29 July 2008

Image:1sl3.png

Template:STRUCTURE 1sl3

crystal structue of Thrombin in complex with a potent P1 heterocycle-Aryl based inhibitor

Template:ABSTRACT PUBMED 15163182

About this Structure

1SL3 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors., Young MB, Barrow JC, Glass KL, Lundell GF, Newton CL, Pellicore JM, Rittle KE, Selnick HG, Stauffer KJ, Vacca JP, Williams PD, Bohn D, Clayton FC, Cook JJ, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, McMasters DR, Miller-Stein C, Pietrak BL, Wallace AA, White RB, Wong B, Yan Y, Nantermet PG, J Med Chem. 2004 Jun 3;47(12):2995-3008. PMID:15163182

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