1ni1

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|PDB= 1ni1 |SIZE=350|CAPTION= <scene name='initialview01'>1ni1</scene>, resolution 2.30&Aring;
|PDB= 1ni1 |SIZE=350|CAPTION= <scene name='initialview01'>1ni1</scene>, resolution 2.30&Aring;
|SITE=
|SITE=
-
|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>
+
|LIGAND= <scene name='pdbligand=2C5:2-CHLORO-5-(3-CHLORO-PHENYL)-6-[(4-CYANO-PHENYL)-(3-METHYL-3H-IMIDAZOL-4-YL)-+METHOXYMETHYL]-NICOTINONITRILE'>2C5</scene>, <scene name='pdbligand=HFP:ALPHA-HYDROXYFARNESYLPHOSPHONIC+ACID'>HFP</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
|ACTIVITY=
|ACTIVITY=
|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])
|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])
 +
|DOMAIN=
 +
|RELATEDENTRY=[[1n9a|1N9A]], [[1n95|1N95]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ni1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ni1 OCA], [http://www.ebi.ac.uk/pdbsum/1ni1 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ni1 RCSB]</span>
}}
}}
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[[Category: Wang, W.]]
[[Category: Wang, W.]]
[[Category: Zhang, H.]]
[[Category: Zhang, H.]]
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[[Category: 2C5]]
 
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[[Category: HFP]]
 
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[[Category: ZN]]
 
[[Category: cyanophenyl]]
[[Category: cyanophenyl]]
[[Category: ftase]]
[[Category: ftase]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 12:57:09 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:30:39 2008''

Revision as of 19:30, 30 March 2008


PDB ID 1ni1

Drag the structure with the mouse to rotate
, resolution 2.30Å
Ligands: , ,
Gene: FNTA (Rattus norvegicus), FNTB (Rattus norvegicus)
Related: 1N9A, 1N95


Resources: FirstGlance, OCA, PDBsum, RCSB
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

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