1ni1

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[[Image:1ni1.gif|left|200px]]<br /><applet load="1ni1" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1ni1.gif|left|200px]]
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caption="1ni1, resolution 2.30&Aring;" />
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'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''<br />
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{{Structure
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|PDB= 1ni1 |SIZE=350|CAPTION= <scene name='initialview01'>1ni1</scene>, resolution 2.30&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=2C5:2-CHLORO-5-(3-CHLORO-PHENYL)-6-[(4-CYANO-PHENYL)-(3-METHYL-3H-IMIDAZOL-4-YL)- METHOXYMETHYL]-NICOTINONITRILE'>2C5</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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'''Imidazole and cyanophenyl farnesyl transferase inhibitors'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1NI1 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=2C5:'>2C5</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1NI1 OCA].
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1NI1 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=1NI1 OCA].
==Reference==
==Reference==
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Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=12699757 12699757]
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Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/12699757 12699757]
[[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 14:06:18 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:57:09 2008''

Revision as of 10:57, 20 March 2008

Image:1ni1.gif


PDB ID 1ni1

Drag the structure with the mouse to rotate
, resolution 2.30Å
Ligands: , and
Gene: FNTA (Rattus norvegicus), FNTB (Rattus norvegicus)
Coordinates: save as pdb, mmCIF, xml



Imidazole and cyanophenyl farnesyl transferase inhibitors


Overview

A pyridyl moiety was introduced into a previously developed series of farnesyltransferase inhibitors containing imidazole and cyanophenyl (such as 4), resulting in potent inhibitors with improved pharmacokinetics.

About this Structure

1NI1 is a Protein complex structure of sequences from Rattus norvegicus. Full crystallographic information is available from OCA.

Reference

Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability., Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2003 May 5;13(9):1571-4. PMID:12699757

Page seeded by OCA on Thu Mar 20 12:57:09 2008

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