2bed

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[[Image:2bed.gif|left|200px]]
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{{Seed}}
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[[Image:2bed.png|left|200px]]
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{{STRUCTURE_2bed| PDB=2bed | SCENE= }}
{{STRUCTURE_2bed| PDB=2bed | SCENE= }}
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'''Structure of FPT bound to inhibitor SCH207736'''
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===Structure of FPT bound to inhibitor SCH207736===
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==Overview==
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Benzocycloheptapyridine tricyclic compounds with piperazine or substituted piperidine moieties extending either from the 5- or 6-position of the tricyclic bridgehead exhibited enhanced FTase activity: this resulted from favorable binding of the ligand nitrogen with the catalytic zinc found in the FTase. A single isomer at C-11 with piperazine adduct extending from the 6-position, compound 24, exhibited excellent FTase activity with IC50 = 0.007 microM, soft agar IC50 = 72 nM, and Rat AUC(PO, 10 mpk) = 4.0 microM x h. X-ray of (-)-[8-chloro-6-(1-piperazinyl)-1H-benzo[5,6]]cyclohepta[1,2-b]pyridine-11 -yl]-1-(methylsulfonyl)piperidine 24 bound to Ftase revealed favorable interaction between piperazine nitrogen and catalytic zinc atom.
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The line below this paragraph, {{ABSTRACT_PUBMED_16298128}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 16298128 is the PubMed ID number.
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{{ABSTRACT_PUBMED_16298128}}
==About this Structure==
==About this Structure==
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[[Category: Fpt]]
[[Category: Fpt]]
[[Category: Ptase]]
[[Category: Ptase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:10:36 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 18:40:01 2008''

Revision as of 15:40, 28 July 2008

Image:2bed.png

Template:STRUCTURE 2bed

Structure of FPT bound to inhibitor SCH207736

Template:ABSTRACT PUBMED 16298128

About this Structure

2BED is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Enhanced FTase activity achieved via piperazine interaction with catalytic zinc., Njoroge FG, Vibulbhan B, Pinto P, Strickland C, Bishop WR, Nomeir A, Girijavallabhan V, Bioorg Med Chem Lett. 2006 Feb 15;16(4):984-8. Epub 2005 Nov 16. PMID:16298128

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