2bed: Difference between revisions

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{{STRUCTURE_2bed|  PDB=2bed  |  SCENE=  }}  
{{STRUCTURE_2bed|  PDB=2bed  |  SCENE=  }}  


'''Structure of FPT bound to inhibitor SCH207736'''
===Structure of FPT bound to inhibitor SCH207736===




==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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{{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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