1n95

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[[Image:1n95.gif|left|200px]]
[[Image:1n95.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1n95 |SIZE=350|CAPTION= <scene name='initialview01'>1n95</scene>, resolution 2.3&Aring;
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The line below this paragraph, containing "STRUCTURE_1n95", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=FTH:1-[2-(4-CYANO-BENZYLAMINO)-3-(3-METHYL-3H-IMIDAZOL-4-YL)-PROPIONYL]-5-NAPHTHALEN-1-YL-1,2,3,6-TETRAHYDRO-PYRIDINE-4-CARBONITRILE'>FTH</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_1n95| PDB=1n95 | SCENE= }}
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|RELATEDENTRY=[[1n94|1N94]], [[1n9a|1N9A]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1n95 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1n95 OCA], [http://www.ebi.ac.uk/pdbsum/1n95 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1n95 RCSB]</span>
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}}
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'''Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives'''
'''Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives'''
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[[Category: Sullivan, G M.]]
[[Category: Sullivan, G M.]]
[[Category: Wang, W.]]
[[Category: Wang, W.]]
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[[Category: farnesyltransferase]]
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[[Category: Farnesyltransferase]]
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[[Category: histidine tetrahydropyridine]]
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[[Category: Histidine tetrahydropyridine]]
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[[Category: prenyltransferase]]
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[[Category: Prenyltransferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:14:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:27:07 2008''
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Revision as of 23:14, 2 May 2008

Template:STRUCTURE 1n95

Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives


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

1N95 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 Page seeded by OCA on Sat May 3 02:14:56 2008

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