1n94
From Proteopedia
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|PDB= 1n94 |SIZE=350|CAPTION= <scene name='initialview01'>1n94</scene>, resolution 3.50Å | |PDB= 1n94 |SIZE=350|CAPTION= <scene name='initialview01'>1n94</scene>, resolution 3.50Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=TIN:2-{(5-{[BUTYL-(2-CYCLOHEXYL-ETHYL)-AMINO]-METHYL}-2'-METHYL-BIPHENYL-2-CARBONYL)-AMINO]-4-METHYLSULFANYL-BUTYRIC+ACID'>TIN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1n95|1N95]], [[1n9a|1N9A]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1n94 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n94 OCA], [http://www.ebi.ac.uk/pdbsum/1n94 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1n94 RCSB]</span> | ||
}} | }} | ||
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[[Category: Sullivan, G M.]] | [[Category: Sullivan, G M.]] | ||
[[Category: Wang, W.]] | [[Category: Wang, W.]] | ||
| - | [[Category: HFP]] | ||
| - | [[Category: TIN]] | ||
| - | [[Category: ZN]] | ||
[[Category: farnesyltransferase]] | [[Category: farnesyltransferase]] | ||
[[Category: prenyltransferase]] | [[Category: prenyltransferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:27:04 2008'' |
Revision as of 19:27, 30 March 2008
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| , resolution 3.50Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Related: | 1N95, 1N9A
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates
Overview
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
About this Structure
1N94 is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.
Reference
Aryl tetrahydropyridine inhibitors of farnesyltransferase: glycine, phenylalanine and histidine derivatives., Gwaltney SL 2nd, O'Connor SJ, Nelson LT, Sullivan GM, Imade H, Wang W, Hasvold L, Li Q, Cohen J, Gu WZ, Tahir SK, Bauch J, Marsh K, Ng SC, Frost DJ, Zhang H, Muchmore S, Jakob CG, Stoll V, Hutchins C, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1359-62. PMID:12657282
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