1mzc

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (07:50, 14 February 2024) (edit) (undo)
 
(13 intermediate revisions not shown.)
Line 1: Line 1:
-
[[Image:1mzc.jpg|left|200px]]
 
-
{{Structure
+
==Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a==
-
|PDB= 1mzc |SIZE=350|CAPTION= <scene name='initialview01'>1mzc</scene>, resolution 2.00&Aring;
+
<StructureSection load='1mzc' size='340' side='right'caption='[[1mzc]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
-
|SITE=
+
== Structural highlights ==
-
|LIGAND= <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=SUC:SUCROSE'>SUC</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
+
<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>
-
|ACTIVITY=
+
</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&#8491;</td></tr>
-
|GENE=
+
<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>
-
|DOMAIN=
+
<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>
-
|RELATEDENTRY=[[1ld7|1LD7]], [[1ld8|1LD8]], [[1jcq|1JCQ]]
+
</table>
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1mzc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1mzc OCA], [http://www.ebi.ac.uk/pdbsum/1mzc PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1mzc RCSB]</span>
+
== 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 ==
 +
[[Image:Consurf_key_small.gif|200px|right]]
 +
Check<jmol>
 +
<jmolCheckbox>
 +
<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/mz/1mzc_consurf.spt"</scriptWhenChecked>
 +
<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
 +
<text>to colour the structure by Evolutionary Conservation</text>
 +
</jmolCheckbox>
 +
</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>
-
'''Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a'''
+
==See Also==
-
 
+
*[[Farnesyltransferase 3D structures|Farnesyltransferase 3D structures]]
-
 
+
__TOC__
-
==Overview==
+
</StructureSection>
-
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.
+
-
 
+
-
==About this Structure==
+
-
1MZC is a [[Protein complex]] structure of sequences from [http://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].
+
-
 
+
-
==Reference==
+
-
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:[http://www.ncbi.nlm.nih.gov/pubmed/12825937 12825937]
+
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Protein complex]]
+
[[Category: Large Structures]]
-
[[Category: Beese, L S.]]
+
[[Category: Beese LS]]
-
[[Category: Buser, C A.]]
+
[[Category: Buser CA]]
-
[[Category: Ciccarone, T M.]]
+
[[Category: Ciccarone TM]]
-
[[Category: Ellis-Hutchings, M.]]
+
[[Category: Ellis-Hutchings M]]
-
[[Category: Fernandes, C.]]
+
[[Category: Fernandes C]]
-
[[Category: Graham, S L.]]
+
[[Category: Graham SL]]
-
[[Category: Hamilton, K A.]]
+
[[Category: Hamilton KA]]
-
[[Category: Huber, H E.]]
+
[[Category: Huber HE]]
-
[[Category: Kohl, N E.]]
+
[[Category: Kohl NE]]
-
[[Category: Lobell, R B.]]
+
[[Category: Lobell RB]]
-
[[Category: MacTough, S C.]]
+
[[Category: MacTough SC]]
-
[[Category: Robinson, R G.]]
+
[[Category: Robinson RG]]
-
[[Category: Shaw, A W.]]
+
[[Category: Shaw AW]]
-
[[Category: Taylor, J S.]]
+
[[Category: Taylor JS]]
-
[[Category: Tsou, N N.]]
+
[[Category: Tsou NN]]
-
[[Category: Walsh, E S.]]
+
[[Category: Walsh ES]]
-
[[Category: deSolms, S J.]]
+
[[Category: DeSolms SJ]]
-
[[Category: alpha-alpha barrel]]
+
-
[[Category: caax]]
+
-
[[Category: fpp]]
+
-
[[Category: ftase]]
+
-
[[Category: inhibitor]]
+
-
[[Category: pftase]]
+
-
[[Category: ra]]
+
-
 
+
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 22:23:11 2008''
+

Current revision

Co-Crystal Structure Of Human Farnesyltransferase With Farnesyldiphosphate and Inhibitor Compound 33a

PDB ID 1mzc

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1mzc"
Personal tools