1n9a: Difference between revisions
New page: left|200px<br /><applet load="1n9a" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n9a, resolution 3.20Å" /> '''Farnesyltransferase ... |
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[[Image:1n9a.gif|left|200px]]<br /><applet load="1n9a" size=" | [[Image:1n9a.gif|left|200px]]<br /><applet load="1n9a" size="350" color="white" frame="true" align="right" spinBox="true" | ||
caption="1n9a, resolution 3.20Å" /> | caption="1n9a, resolution 3.20Å" /> | ||
'''Farnesyltransferase complex with tetrahydropyridine inhibitors'''<br /> | '''Farnesyltransferase complex with tetrahydropyridine inhibitors'''<br /> | ||
==Overview== | ==Overview== | ||
Inhibitors of farnesyltransferase are effective against a variety of | 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== | ==About this Structure== | ||
1N9A is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with ZN, HFP and FTI as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | 1N9A is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=ZN:'>ZN</scene>, <scene name='pdbligand=HFP:'>HFP</scene> and <scene name='pdbligand=FTI:'>FTI</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1N9A OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
[[Category: Cohen, J.]] | [[Category: Cohen, J.]] | ||
[[Category: Conner, S | [[Category: Conner, S J.O.]] | ||
[[Category: Gu, W | [[Category: Gu, W Z.]] | ||
[[Category: Hasvold, L.]] | [[Category: Hasvold, L.]] | ||
[[Category: II, S | [[Category: II, S L.Gwaltney.]] | ||
[[Category: Imade, H.]] | [[Category: Imade, H.]] | ||
[[Category: Li, Q.]] | [[Category: Li, Q.]] | ||
[[Category: Nelson, L | [[Category: Nelson, L T.]] | ||
[[Category: Sullivan, G | [[Category: Sullivan, G M.]] | ||
[[Category: Wang, W.]] | [[Category: Wang, W.]] | ||
[[Category: FTI]] | [[Category: FTI]] | ||
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[[Category: tetrahydropyridine]] | [[Category: tetrahydropyridine]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:03:35 2008'' | ||
Revision as of 15:03, 21 February 2008
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Farnesyltransferase complex with tetrahydropyridine inhibitors
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 bioavailable aryl tetrahydropyridines that are potent in cell culture. The design, synthesis, SAR and biological properties of these compounds will be discussed.
About this StructureAbout this Structure
1N9A is a Protein complex structure of sequences from Rattus norvegicus with , and as ligands. Full crystallographic information is available from OCA.
ReferenceReference
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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