1mzc
From Proteopedia
(Difference between revisions)
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<StructureSection load='1mzc' size='340' side='right'caption='[[1mzc]], [[Resolution|resolution]] 2.00Å' scene=''> | <StructureSection load='1mzc' size='340' side='right'caption='[[1mzc]], [[Resolution|resolution]] 2.00Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[1mzc]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/ | + | <table><tr><td colspan='2'>[[1mzc]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MZC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=1MZC FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BNE:2-[3-(3-ETHYL-1-METHYL-2-OXO-AZEPAN-3-YL)-PHENOXY]-4-[1-AMINO-1-(1-METHYL-1H-IMIDIZOL-5-YL)-ETHYL]-BENZONITRILE'>BNE</scene>, <scene name='pdbligand=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand= | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2Å</td></tr> |
| - | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BNE:2-[3-(3-ETHYL-1-METHYL-2-OXO-AZEPAN-3-YL)-PHENOXY]-4-[1-AMINO-1-(1-METHYL-1H-IMIDIZOL-5-YL)-ETHYL]-BENZONITRILE'>BNE</scene>, <scene name='pdbligand=FPP:FARNESYL+DIPHOSPHATE'>FPP</scene>, <scene name='pdbligand=FRU:FRUCTOSE'>FRU</scene>, <scene name='pdbligand=GLC:ALPHA-D-GLUCOSE'>GLC</scene>, <scene name='pdbligand=PRD_900003:sucrose'>PRD_900003</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=1mzc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mzc OCA], [https://pdbe.org/1mzc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mzc RCSB], [https://www.ebi.ac.uk/pdbsum/1mzc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mzc ProSAT]</span></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=1mzc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mzc OCA], [https://pdbe.org/1mzc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=1mzc RCSB], [https://www.ebi.ac.uk/pdbsum/1mzc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=1mzc ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| - | + | [https://www.uniprot.org/uniprot/FNTA_HUMAN FNTA_HUMAN] 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=1mzc 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=1mzc ConSurf]. | ||
<div style="clear:both"></div> | <div style="clear:both"></div> | ||
| - | <div style="background-color:#fffaf0;"> | ||
| - | == Publication Abstract from PubMed == | ||
| - | A series of novel diaryl ether lactams have been identified as very potent dual inhibitors of protein farnesyltransferase (FTase) and protein geranylgeranyltransferase I (GGTase-I), enzymes involved in the prenylation of Ras. The structure of the complex formed between one of these compounds and FTase has been determined by X-ray crystallography. These compounds are the first reported to inhibit the prenylation of the important oncogene Ki-Ras4B in vivo. Unfortunately, doses sufficient to achieve this endpoint were rapidly lethal. | ||
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| - | Dual protein farnesyltransferase-geranylgeranyltransferase-I inhibitors as potential cancer chemotherapeutic agents.,deSolms SJ, Ciccarone TM, MacTough SC, Shaw AW, Buser CA, Ellis-Hutchings M, Fernandes C, Hamilton KA, Huber HE, Kohl NE, Lobell RB, Robinson RG, Tsou NN, Walsh ES, Graham SL, Beese LS, Taylor JS J Med Chem. 2003 Jul 3;46(14):2973-84. PMID:12825937<ref>PMID:12825937</ref> | ||
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| - | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| - | </div> | ||
| - | <div class="pdbe-citations 1mzc" 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: | + | [[Category: Homo sapiens]] |
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Beese | + | [[Category: Beese LS]] |
| - | [[Category: Buser | + | [[Category: Buser CA]] |
| - | [[Category: Ciccarone | + | [[Category: Ciccarone TM]] |
| - | [[Category: Ellis-Hutchings | + | [[Category: Ellis-Hutchings M]] |
| - | [[Category: Fernandes | + | [[Category: Fernandes C]] |
| - | [[Category: Graham | + | [[Category: Graham SL]] |
| - | [[Category: Hamilton | + | [[Category: Hamilton KA]] |
| - | [[Category: Huber | + | [[Category: Huber HE]] |
| - | [[Category: Kohl | + | [[Category: Kohl NE]] |
| - | [[Category: Lobell | + | [[Category: Lobell RB]] |
| - | [[Category: MacTough | + | [[Category: MacTough SC]] |
| - | [[Category: Robinson | + | [[Category: Robinson RG]] |
| - | [[Category: Shaw | + | [[Category: Shaw AW]] |
| - | [[Category: Taylor | + | [[Category: Taylor JS]] |
| - | [[Category: Tsou | + | [[Category: Tsou NN]] |
| - | [[Category: Walsh | + | [[Category: Walsh ES]] |
| - | [[Category: DeSolms | + | [[Category: DeSolms SJ]] |
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Current revision
Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a
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Categories: Homo sapiens | Large Structures | Beese LS | Buser CA | Ciccarone TM | Ellis-Hutchings M | Fernandes C | Graham SL | Hamilton KA | Huber HE | Kohl NE | Lobell RB | MacTough SC | Robinson RG | Shaw AW | Taylor JS | Tsou NN | Walsh ES | DeSolms SJ
