2j14

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Current revision (14:31, 13 December 2023) (edit) (undo)
 
(12 intermediate revisions not shown.)
Line 1: Line 1:
-
{{Seed}}
 
-
[[Image:2j14.png|left|200px]]
 
-
<!--
+
==3,4,5-Trisubstituted Isoxazoles as Novel PPARdelta Agonists: Part2==
-
The line below this paragraph, containing "STRUCTURE_2j14", creates the "Structure Box" on the page.
+
<StructureSection load='2j14' size='340' side='right'caption='[[2j14]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
-
You may change the PDB parameter (which sets the PDB file loaded into the applet)
+
== Structural highlights ==
-
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
+
<table><tr><td colspan='2'>[[2j14]] 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=2J14 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2J14 FirstGlance]. <br>
-
or leave the SCENE parameter empty for the default display.
+
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.8&#8491;</td></tr>
-
-->
+
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GNI:(3-{4-[2-(2,4-DICHLORO-PHENOXY)-ETHYLCARBAMOYL]-5-PHENYL-ISOXAZOL-3-YL}-PHENYL)-ACETIC+ACID'>GNI</scene></td></tr>
-
{{STRUCTURE_2j14| PDB=2j14 | SCENE= }}
+
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2j14 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2j14 OCA], [https://pdbe.org/2j14 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2j14 RCSB], [https://www.ebi.ac.uk/pdbsum/2j14 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2j14 ProSAT]</span></td></tr>
 +
</table>
 +
== Function ==
 +
[https://www.uniprot.org/uniprot/PPARD_HUMAN PPARD_HUMAN] Ligand-activated transcription factor. Receptor that binds peroxisome proliferators such as hypolipidemic drugs and fatty acids. Has a preference for poly-unsaturated fatty acids, such as gamma-linoleic acid and eicosapentanoic acid. Once activated by a ligand, the receptor binds to promoter elements of target genes. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the acyl-CoA oxidase gene. Decreases expression of NPC1L1 once activated by a ligand.<ref>PMID:1333051</ref> <ref>PMID:15604518</ref>
 +
== 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/j1/2j14_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=2j14 ConSurf].
 +
<div style="clear:both"></div>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
A series of PPARdelta-selective agonists was investigated and optimized for a favorable in vivo pharmacokinetic profile. Isoxazole LCI765 (17d) was found to be a potent and selective PPARdelta agonist with good in vivo PK properties in mouse (C(max)=5.1 microM, t(1/2)=3.1 h). LCI765 regulated expression of genes involved in energy homeostasis in relevant tissues when dosed orally in C57BL6 mice. A co-crystal structure of compound LCI765 and the LBD of PPARdelta is discussed.
-
===3,4,5-TRISUBSTITUTED ISOXAZOLES AS NOVEL PPARDELTA AGONISTS: PART2===
+
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.,Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. Epub 2006 Aug 22. PMID:16931011<ref>PMID:16931011</ref>
 +
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 +
</div>
 +
<div class="pdbe-citations 2j14" style="background-color:#fffaf0;"></div>
-
<!--
+
==See Also==
-
The line below this paragraph, {{ABSTRACT_PUBMED_16931011}}, adds the Publication Abstract to the page
+
*[[Peroxisome proliferator-activated receptor 3D structures|Peroxisome proliferator-activated receptor 3D structures]]
-
(as it appears on PubMed at http://www.pubmed.gov), where 16931011 is the PubMed ID number.
+
== References ==
-
-->
+
<references/>
-
{{ABSTRACT_PUBMED_16931011}}
+
__TOC__
-
 
+
</StructureSection>
-
==About this Structure==
+
-
2J14 is a [[Single protein]] structure of sequence 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=2J14 OCA].
+
-
 
+
-
==Reference==
+
-
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2., Epple R, Azimioara M, Russo R, Xie Y, Wang X, Cow C, Wityak J, Karanewsky D, Bursulaya B, Kreusch A, Tuntland T, Gerken A, Iskandar M, Saez E, Martin Seidel H, Tian SS, Bioorg Med Chem Lett. 2006 Nov 1;16(21):5488-92. Epub 2006 Aug 22. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/16931011 16931011]
+
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
-
[[Category: Single protein]]
+
[[Category: Large Structures]]
-
[[Category: Azimioara, M.]]
+
[[Category: Azimioara M]]
-
[[Category: Bursulaya, B.]]
+
[[Category: Bursulaya B]]
-
[[Category: Cow, C.]]
+
[[Category: Cow C]]
-
[[Category: Epple, R.]]
+
[[Category: Epple R]]
-
[[Category: Gerken, A.]]
+
[[Category: Gerken A]]
-
[[Category: Iskandar, M.]]
+
[[Category: Iskandar M]]
-
[[Category: Karanewsky, D.]]
+
[[Category: Karanewsky D]]
-
[[Category: Kreusch, A.]]
+
[[Category: Kreusch A]]
-
[[Category: Russo, R.]]
+
[[Category: Russo R]]
-
[[Category: Saez, E.]]
+
[[Category: Saez E]]
-
[[Category: Seidel, H M.]]
+
[[Category: Seidel HM]]
-
[[Category: Tian, S S.]]
+
[[Category: Tian SS]]
-
[[Category: Tuntland, T.]]
+
[[Category: Tuntland T]]
-
[[Category: Wang, X.]]
+
[[Category: Wang X]]
-
[[Category: Wityak, J.]]
+
[[Category: Wityak J]]
-
[[Category: Xie, Y.]]
+
[[Category: Xie Y]]
-
[[Category: Activator]]
+
-
[[Category: Alternative splicing]]
+
-
[[Category: Dna-binding]]
+
-
[[Category: Fatty acid]]
+
-
[[Category: Metal-binding]]
+
-
[[Category: Nuclear protein]]
+
-
[[Category: Nuclear receptor fold]]
+
-
[[Category: Ppar]]
+
-
[[Category: Receptor]]
+
-
[[Category: Transcription]]
+
-
[[Category: Transcription regulation]]
+
-
[[Category: Zinc]]
+
-
[[Category: Zinc-finger]]
+
-
 
+
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 02:34:05 2008''
+

Current revision

3,4,5-Trisubstituted Isoxazoles as Novel PPARdelta Agonists: Part2

PDB ID 2j14

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/2j14"
Personal tools