1nl4

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PDB ID 1nl4

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, resolution 2.7Å
Ligands: , ,
Gene: FNTA (Rattus norvegicus), FNTB (Rattus norvegicus)
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



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

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