1n9a
From Proteopedia
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|PDB= 1n9a |SIZE=350|CAPTION= <scene name='initialview01'>1n9a</scene>, resolution 3.20Å | |PDB= 1n9a |SIZE=350|CAPTION= <scene name='initialview01'>1n9a</scene>, resolution 3.20Å | ||
|SITE= | |SITE= | ||
| - | |LIGAND= | + | |LIGAND= <scene name='pdbligand=FTI:1-{2-[3-(4-CYANO-BENZYL)-3H-IMIDAZOL-4-YL]-ACETYL}-5-NAPHTHALEN-1-YL-1,2,3,6-TETRAHYDRO-PYRIDINE-4-CARBONITRILE'>FTI</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene> |
|ACTIVITY= | |ACTIVITY= | ||
|GENE= | |GENE= | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1n94|1N94]], [[1n95|1N95]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1n9a FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n9a OCA], [http://www.ebi.ac.uk/pdbsum/1n9a PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1n9a RCSB]</span> | ||
}} | }} | ||
| Line 32: | Line 35: | ||
[[Category: Sullivan, G M.]] | [[Category: Sullivan, G M.]] | ||
[[Category: Wang, W.]] | [[Category: Wang, W.]] | ||
| - | [[Category: FTI]] | ||
| - | [[Category: HFP]] | ||
| - | [[Category: ZN]] | ||
[[Category: farnesyltransferase]] | [[Category: farnesyltransferase]] | ||
[[Category: prenyltransferase]] | [[Category: prenyltransferase]] | ||
[[Category: tetrahydropyridine]] | [[Category: tetrahydropyridine]] | ||
| - | ''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 22:27:09 2008'' |
Revision as of 19:27, 30 March 2008
| |||||||
| , resolution 3.20Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | , , | ||||||
| Related: | 1N94, 1N95
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Farnesyltransferase complex with tetrahydropyridine inhibitors
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 bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.
About this Structure
1N9A is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.
Reference
Aryl tetrahydropyridine inhibitors of farnesyltransferase: bioavailable analogues with improved cellular potency., 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):1363-6. PMID:12657283
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