1nl4
From Proteopedia
| Line 4: | Line 4: | ||
|PDB= 1nl4 |SIZE=350|CAPTION= <scene name='initialview01'>1nl4</scene>, resolution 2.7Å | |PDB= 1nl4 |SIZE=350|CAPTION= <scene name='initialview01'>1nl4</scene>, resolution 2.7Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=FTL:4-[(3-CYANO-BENZYL)-(3-METHYL-3H-IMIDAZOL-4-YLMETHYL)-AMINO]-2-NAPHTHALEN-1-YL-BENZONITRILE'>FTL</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
|ACTIVITY= | |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]) | |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]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY= | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1nl4 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1nl4 OCA], [http://www.ebi.ac.uk/pdbsum/1nl4 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1nl4 RCSB]</span> | ||
}} | }} | ||
| Line 29: | Line 32: | ||
[[Category: Muchmore, S W.]] | [[Category: Muchmore, S W.]] | ||
[[Category: Sham, H L.]] | [[Category: Sham, H L.]] | ||
| - | [[Category: FTL]] | ||
| - | [[Category: HFP]] | ||
| - | [[Category: ZN]] | ||
[[Category: prenyltransferase]] | [[Category: prenyltransferase]] | ||
[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:31:54 2008'' |
Revision as of 19:31, 30 March 2008
| |||||||
| , resolution 2.7Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Gene: | FNTA (Rattus norvegicus), FNTB (Rattus norvegicus) | ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| 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 Sun Mar 30 22:31:54 2008
