1nl4

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(New page: 200px<br /><applet load="1nl4" size="450" color="white" frame="true" align="right" spinBox="true" caption="1nl4, resolution 2.7&Aring;" /> '''Crystal Structure of ...)
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Revision as of 20:14, 20 November 2007

Image:1nl4.jpg

1nl4, resolution 2.7Å

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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 ZN, HFP and FTL 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

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