1nl4

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[[Image:1nl4.jpg|left|200px]]<br /><applet load="1nl4" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1nl4.jpg|left|200px]]
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caption="1nl4, resolution 2.7&Aring;" />
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'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''<br />
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{{Structure
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|PDB= 1nl4 |SIZE=350|CAPTION= <scene name='initialview01'>1nl4</scene>, resolution 2.7&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene> and <scene name='pdbligand=FTL:4-[(3-CYANO-BENZYL)-(3-METHYL-3H-IMIDAZOL-4-YLMETHYL)-AMINO]-2-NAPHTHALEN-1-YL-BENZONITRILE'>FTL</scene>
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|ACTIVITY=
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|GENE= FNTA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus]), FNTB ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Rattus norvegicus])
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}}
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'''Crystal Structure of Rat Farnesyl Transferase in Complex With A Potent Biphenyl Inhibitor'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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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].
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1NL4 is a [[Protein complex]] structure of sequences from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NL4 OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12657284 12657284]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/12657284 12657284]
[[Category: Protein complex]]
[[Category: Protein complex]]
[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:07:14 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:58:15 2008''

Revision as of 10:58, 20 March 2008

Image:1nl4.jpg


PDB ID 1nl4

Drag the structure with the mouse to rotate
, resolution 2.7Å
Ligands: , and
Gene: FNTA (Rattus norvegicus), FNTB (Rattus norvegicus)
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

Page seeded by OCA on Thu Mar 20 12:58:15 2008

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