1nl4
From Proteopedia
(New page: 200px<br /><applet load="1nl4" size="450" color="white" frame="true" align="right" spinBox="true" caption="1nl4, resolution 2.7Å" /> '''Crystal Structure of ...) |
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| - | [[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size=" | + | [[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1nl4, resolution 2.7Å" /> | caption="1nl4, resolution 2.7Å" /> | ||
'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br /> | '''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br /> | ||
==Overview== | ==Overview== | ||
| - | A series of imidazole-containing biphenyls was prepared and evaluated in | + | A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (<1nM), FTase/GGTase selective (>300-fold) and cellularly active (<or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented. |
==About this Structure== | ==About this Structure== | ||
| - | 1NL4 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 FTL as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1NL4 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=FTL:'>FTL</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Rattus norvegicus]] | [[Category: Rattus norvegicus]] | ||
[[Category: Cohen, J.]] | [[Category: Cohen, J.]] | ||
| - | [[Category: Curtin, M | + | [[Category: Curtin, M L.]] |
| - | [[Category: Florjancic, A | + | [[Category: Florjancic, A S.]] |
| - | [[Category: Frost, D | + | [[Category: Frost, D J.]] |
| - | [[Category: Gu, W | + | [[Category: Gu, W J.]] |
| - | [[Category: Muchmore, S | + | [[Category: Muchmore, S W.]] |
| - | [[Category: Sham, H | + | [[Category: Sham, H L.]] |
[[Category: FTL]] | [[Category: FTL]] | ||
[[Category: HFP]] | [[Category: HFP]] | ||
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[[Category: transferase]] | [[Category: transferase]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:07:14 2008'' |
Revision as of 12:07, 21 February 2008
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Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor
Overview
A series of imidazole-containing biphenyls was prepared and evaluated in vitro for inhibition of FTase and cellular Ras processing. Several of these analogues, such as 21, are potent inhibitors of FTase (<1nM), FTase/GGTase selective (>300-fold) and cellularly active (<or=80nM). An X-ray crystal structure of inhibitor 21 bound to rat farnesyltransferase is also presented.
About this Structure
1NL4 is a Protein complex structure of sequences from Rattus norvegicus with , and as ligands. Full crystallographic information is available from OCA.
Reference
Novel and selective imidazole-containing biphenyl inhibitors of protein farnesyltransferase., Curtin ML, Florjancic AS, Cohen J, Gu WZ, Frost DJ, Muchmore SW, Sham HL, Bioorg Med Chem Lett. 2003 Apr 7;13(7):1367-71. PMID:12657284
Page seeded by OCA on Thu Feb 21 14:07:14 2008
Categories: Protein complex | Rattus norvegicus | Cohen, J. | Curtin, M L. | Florjancic, A S. | Frost, D J. | Gu, W J. | Muchmore, S W. | Sham, H L. | FTL | HFP | ZN | Prenyltransferase | Transferase
