1x81

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[[Image:1x81.gif|left|200px]]
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{{Seed}}
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[[Image:1x81.png|left|200px]]
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{{STRUCTURE_1x81| PDB=1x81 | SCENE= }}
{{STRUCTURE_1x81| PDB=1x81 | SCENE= }}
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'''Farnesyl transferase structure of Jansen compound'''
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===Farnesyl transferase structure of Jansen compound===
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==Overview==
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As a part of our efforts to identify potent inhibitors of farnesyltransferase (FTase), modification of the structure of tipifarnib through structure-based design was undertaken by replacing the 2-quinolones with 4-quinolones and pyridones, and subsequent relocation of the D-ring to the N-methyl group on the imidazole ring. This study has yielded a novel series of potent and selective FTase inhibitors. The X-ray structure of tipifarnib (1) in complex with FTase was described.
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The line below this paragraph, {{ABSTRACT_PUBMED_15454228}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 15454228 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15454228}}
==About this Structure==
==About this Structure==
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[[Category: Stoll, V S.]]
[[Category: Stoll, V S.]]
[[Category: Fanesyltransferase]]
[[Category: Fanesyltransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 14:41:19 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 14:56:26 2008''

Revision as of 11:56, 27 July 2008

Image:1x81.png

Template:STRUCTURE 1x81

Farnesyl transferase structure of Jansen compound

Template:ABSTRACT PUBMED 15454228

About this Structure

1X81 is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Design, synthesis, and activity of 4-quinolone and pyridone compounds as nonthiol-containing farnesyltransferase inhibitors., Li Q, Claiborne A, Li T, Hasvold L, Stoll VS, Muchmore S, Jakob CG, Gu W, Cohen J, Hutchins C, Frost D, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2004 Nov 1;14(21):5367-70. PMID:15454228

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