1ni1
From Proteopedia
(Difference between revisions)
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<StructureSection load='1ni1' size='340' side='right'caption='[[1ni1]], [[Resolution|resolution]] 2.30Å' scene=''> | <StructureSection load='1ni1' size='340' side='right'caption='[[1ni1]], [[Resolution|resolution]] 2.30Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[1ni1]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[1ni1]] is a 2 chain structure with sequence from [https://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]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1NI1 FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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></td></tr> | |
| - | + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=1ni1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ni1 OCA], [https://pdbe.org/1ni1 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1ni1 RCSB], [https://www.ebi.ac.uk/pdbsum/1ni1 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1ni1 ProSAT]</span></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/FNTA_RAT FNTA_RAT] Catalyzes the transfer of a farnesyl or geranyl-geranyl moiety from farnesyl or geranyl-geranyl pyrophosphate to a cysteine at the fourth position from the C-terminus of several proteins having the C-terminal sequence Cys-aliphatic-aliphatic-X. The alpha subunit is thought to participate in a stable complex with the substrate. The beta subunit binds the peptide substrate. Through RAC1 prenylation and activation may positively regulate neuromuscular junction development downstream of MUSK (By similarity). |
== Evolutionary Conservation == | == Evolutionary Conservation == | ||
[[Image:Consurf_key_small.gif|200px|right]] | [[Image:Consurf_key_small.gif|200px|right]] | ||
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1ni1 ConSurf]. | </jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=1ni1 ConSurf]. | ||
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | 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. | ||
| - | |||
| - | 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<ref>PMID:12699757</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 1ni1" style="background-color:#fffaf0;"></div> | ||
==See Also== | ==See Also== | ||
*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]] | *[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]] | ||
| - | == References == | ||
| - | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: Buffalo rat]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Bauch | + | [[Category: Rattus norvegicus]] |
| - | [[Category: Cohen | + | [[Category: Bauch J]] |
| - | [[Category: Gu | + | [[Category: Cohen J]] |
| - | [[Category: Hasvold | + | [[Category: Gu WZ]] |
| - | [[Category: Leonard | + | [[Category: Hasvold L]] |
| - | [[Category: Li | + | [[Category: Leonard N]] |
| - | [[Category: Li | + | [[Category: Li Q]] |
| - | [[Category: Lin | + | [[Category: Li T]] |
| - | [[Category: Marsh | + | [[Category: Lin NH]] |
| - | [[Category: Rosenberg | + | [[Category: Marsh K]] |
| - | [[Category: Sham | + | [[Category: Rosenberg SH]] |
| - | [[Category: Stoll | + | [[Category: Sham HL]] |
| - | [[Category: Tong | + | [[Category: Stoll V]] |
| - | [[Category: Wang | + | [[Category: Tong Y]] |
| - | [[Category: Wang | + | [[Category: Wang L]] |
| - | [[Category: Zhang | + | [[Category: Wang W]] |
| - | + | [[Category: Zhang H]] | |
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Current revision
Imidazole and cyanophenyl farnesyl transferase inhibitors
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Categories: Large Structures | Rattus norvegicus | Bauch J | Cohen J | Gu WZ | Hasvold L | Leonard N | Li Q | Li T | Lin NH | Marsh K | Rosenberg SH | Sham HL | Stoll V | Tong Y | Wang L | Wang W | Zhang H
