1x81
From Proteopedia
(New page: 200px<br /><applet load="1x81" size="450" color="white" frame="true" align="right" spinBox="true" caption="1x81, resolution 3.5Å" /> '''Farnesyl transferase ...) |
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| - | [[Image:1x81.gif|left|200px]]<br /><applet load="1x81" size=" | + | [[Image:1x81.gif|left|200px]]<br /><applet load="1x81" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1x81, resolution 3.5Å" /> | caption="1x81, resolution 3.5Å" /> | ||
'''Farnesyl transferase structure of Jansen compound'''<br /> | '''Farnesyl transferase structure of Jansen compound'''<br /> | ||
==Overview== | ==Overview== | ||
| - | As a part of our efforts to identify potent inhibitors of | + | 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== | ==About this Structure== | ||
| - | 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 ZN and JAN 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:// | + | 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]. |
==Reference== | ==Reference== | ||
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[[Category: Hasvold, L.]] | [[Category: Hasvold, L.]] | ||
[[Category: Hutchins, C.]] | [[Category: Hutchins, C.]] | ||
| - | [[Category: Jakob, C | + | [[Category: Jakob, C G.]] |
[[Category: Li, Q.]] | [[Category: Li, Q.]] | ||
[[Category: Li, T.]] | [[Category: Li, T.]] | ||
[[Category: Muchmore, S.]] | [[Category: Muchmore, S.]] | ||
| - | [[Category: Rosenberg, S | + | [[Category: Rosenberg, S H.]] |
| - | [[Category: Sham, H | + | [[Category: Sham, H L.]] |
| - | [[Category: Stoll, V | + | [[Category: Stoll, V S.]] |
[[Category: JAN]] | [[Category: JAN]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
[[Category: fanesyltransferase]] | [[Category: fanesyltransferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:51:56 2008'' |
Revision as of 13:52, 21 February 2008
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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 with and as ligands. Active as Protein farnesyltransferase, with EC number 2.5.1.58 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 Feb 21 15:51:56 2008
Categories: Protein complex | Protein farnesyltransferase | Rattus norvegicus | Claiborne, A. | Cohen, J. | Frost, D. | Gu, W. | Hasvold, L. | Hutchins, C. | Jakob, C G. | Li, Q. | Li, T. | Muchmore, S. | Rosenberg, S H. | Sham, H L. | Stoll, V S. | JAN | ZN | Fanesyltransferase
