1nl4: Difference between revisions
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[[Image:1nl4.jpg|left|200px]] | [[Image:1nl4.jpg|left|200px]] | ||
'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor''' | {{Structure | ||
|PDB= 1nl4 |SIZE=350|CAPTION= <scene name='initialview01'>1nl4</scene>, resolution 2.7Å | |||
|SITE= | |||
|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene> and <scene name='pdbligand=FTL:4-[(3-CYANO-BENZYL)-(3-METHYL-3H-IMIDAZOL-4-YLMETHYL)-AMINO]-2-NAPHTHALEN-1-YL-BENZONITRILE'>FTL</scene> | |||
|ACTIVITY= | |||
|GENE= FNTA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus]), FNTB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus]) | |||
}} | |||
'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor''' | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
1NL4 is a [ | 1NL4 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=1NL4 OCA]. | ||
==Reference== | ==Reference== | ||
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase., Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1367-71. PMID:[http:// | Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase., Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1367-71. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12657284 12657284] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:58:15 2008'' | ||
Revision as of 10:58, 20 March 2008
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| 1nl4, resolution 2.7Å | |||||||||||||
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| Ligands: | ZN, HFP and FTL | ||||||||||||
| Gene: | FNTA (Rattus norvegicus), FNTB (Rattus norvegicus) | ||||||||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||||||||
Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor
Overview
A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (<1nM), FTase/GGTase selective (>300-fold) and cellularly active (<or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
About this Structure
1NL4 is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.
Reference
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase., Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1367-71. PMID:12657284
Page seeded by OCA on Thu Mar 20 12:58:15 2008
