1n94: Difference between revisions

Revision as of 02:14, 3 May 2008

Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates

OverviewOverview

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 StructureAbout this Structure

1N94 is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

ReferenceReference

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 02:14:50 2008

Proteopedia Page Contributors and Editors (what is this?)Proteopedia Page Contributors and Editors (what is this?)

OCA

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 [[Image:1n94.gif|left|200px]]
- {{Structure
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+The line below this paragraph, containing "STRUCTURE_1n94", creates the "Structure Box" on the page.
-|SITE=
+You may change the PDB parameter (which sets the PDB file loaded into the applet)
-|LIGAND= <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=TIN:2-{(5-{[BUTYL-(2-CYCLOHEXYL-ETHYL)-AMINO]-METHYL}-2&#39;-METHYL-BIPHENYL-2-CARBONYL)-AMINO]-4-METHYLSULFANYL-BUTYRIC+ACID'>TIN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
+or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-|ACTIVITY=
+or leave the SCENE parameter empty for the default display.
-|GENE=
+-->
-|DOMAIN=
+{{STRUCTURE_1n94|  PDB=1n94  |  SCENE=  }}
-|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>
-}}
 '''Aryl Tetrahydropyridine Inhbitors of Farnesyltransferase: Glycine, Phenylalanine and Histidine Derivates'''
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 [[Category: Sullivan, G M.]]
 [[Category: Wang, W.]]
-[[Category: farnesyltransferase]]
+[[Category: Farnesyltransferase]]
-[[Category: prenyltransferase]]
+[[Category: Prenyltransferase]]
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May  3 02:14:50 2008''
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:27:04 2008''