1x81

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[[Image:1x81.gif|left|200px]]
[[Image:1x81.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1x81 |SIZE=350|CAPTION= <scene name='initialview01'>1x81</scene>, resolution 3.5&Aring;
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The line below this paragraph, containing "STRUCTURE_1x81", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=JAN:6-[(S)-AMINO(4-CHLOROPHENYL)(1-METHYL-1H-IMIDAZOL-5-YL)METHYL]-4-(3-CHLOROPHENYL)-1-METHYLQUINOLIN-2(1H)-ONE'>JAN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_farnesyltransferase Protein farnesyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.58 2.5.1.58] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1x81| PDB=1x81 | SCENE= }}
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|RELATEDENTRY=[[1ni1|1NI1]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1x81 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1x81 OCA], [http://www.ebi.ac.uk/pdbsum/1x81 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1x81 RCSB]</span>
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}}
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'''Farnesyl transferase structure of Jansen compound'''
'''Farnesyl transferase structure of Jansen compound'''
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[[Category: Sham, H L.]]
[[Category: Sham, H L.]]
[[Category: Stoll, V S.]]
[[Category: Stoll, V S.]]
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[[Category: fanesyltransferase]]
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[[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 Mon Mar 31 00:45:55 2008''
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Revision as of 11:41, 3 May 2008

Image:1x81.gif

Template:STRUCTURE 1x81

Farnesyl transferase structure of Jansen compound


Overview

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.

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 Page seeded by OCA on Sat May 3 14:41:19 2008

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OCA

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