1n95
From Proteopedia
(New page: 200px<br /><applet load="1n95" size="450" color="white" frame="true" align="right" spinBox="true" caption="1n95, resolution 2.3Å" /> '''Aryl Tetrahydrophyrid...) |
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| - | [[Image:1n95.gif|left|200px]]<br /><applet load="1n95" size=" | + | [[Image:1n95.gif|left|200px]]<br /><applet load="1n95" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1n95, resolution 2.3Å" /> | caption="1n95, resolution 2.3Å" /> | ||
'''Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives'''<br /> | '''Aryl Tetrahydrophyridine Inhbitors of Farnesyltranferase: Glycine, Phenylalanine and Histidine Derivatives'''<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 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== | ==About this Structure== | ||
| - | 1N95 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 FTH as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1N95 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=FTH:'>FTH</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1N95 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: FTH]] | [[Category: FTH]] | ||
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[[Category: prenyltransferase]] | [[Category: prenyltransferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:03:33 2008'' |
Revision as of 12:03, 21 February 2008
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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 with , and as ligands. 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 Thu Feb 21 14:03:33 2008
