1x81

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[[Image:1x81.gif|left|200px]]<br /><applet load="1x81" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1x81.gif|left|200px]]
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caption="1x81, resolution 3.5&Aring;" />
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'''Farnesyl transferase structure of Jansen compound'''<br />
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{{Structure
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|PDB= 1x81 |SIZE=350|CAPTION= <scene name='initialview01'>1x81</scene>, resolution 3.5&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> and <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>
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|ACTIVITY= [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]
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|GENE=
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}}
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'''Farnesyl transferase structure of Jansen compound'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1X81 is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=JAN:'>JAN</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [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] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1X81 OCA].
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1X81 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1X81 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=15454228 15454228]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/15454228 15454228]
[[Category: Protein complex]]
[[Category: Protein complex]]
[[Category: Protein farnesyltransferase]]
[[Category: Protein farnesyltransferase]]
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[[Category: fanesyltransferase]]
[[Category: fanesyltransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:51:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 15:06:16 2008''

Revision as of 13:06, 20 March 2008

Image:1x81.gif


PDB ID 1x81

Drag the structure with the mouse to rotate
, resolution 3.5Å
Ligands: and
Activity: Protein farnesyltransferase, with EC number 2.5.1.58
Coordinates: save as pdb, mmCIF, xml



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 Thu Mar 20 15:06:16 2008

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