1nl4
From Proteopedia
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'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor''' | '''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor''' | ||
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[[Category: Muchmore, S W.]] | [[Category: Muchmore, S W.]] | ||
[[Category: Sham, H L.]] | [[Category: Sham, H L.]] | ||
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- | [[Category: | + | [[Category: Transferase]] |
- | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 02:39:47 2008'' | |
- | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + |
Revision as of 23:39, 2 May 2008
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. 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 Sat May 3 02:39:47 2008