8ywu: Difference between revisions

Latest revision as of 07:45, 9 April 2025

Human PPAR alpha ligand binding domain in complex with a 1H-pyrazolo[3,4-b]pyridine-derived compound

Structural highlights

8ywu is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 1.77Å
Ligands:	A1LZ9
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

PPARA_HUMAN Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety (By similarity). Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.^[1] ^[2] ^[3] ^[4]

References

↑ Sher T, Yi HF, McBride OW, Gonzalez FJ. cDNA cloning, chromosomal mapping, and functional characterization of the human peroxisome proliferator activated receptor. Biochemistry. 1993 Jun 1;32(21):5598-604. PMID:7684926
↑ Juge-Aubry CE, Gorla-Bajszczak A, Pernin A, Lemberger T, Wahli W, Burger AG, Meier CA. Peroxisome proliferator-activated receptor mediates cross-talk with thyroid hormone receptor by competition for retinoid X receptor. Possible role of a leucine zipper-like heptad repeat. J Biol Chem. 1995 Jul 28;270(30):18117-22. PMID:7629123
↑ Yan ZH, Karam WG, Staudinger JL, Medvedev A, Ghanayem BI, Jetten AM. Regulation of peroxisome proliferator-activated receptor alpha-induced transactivation by the nuclear orphan receptor TAK1/TR4. J Biol Chem. 1998 May 1;273(18):10948-57. PMID:9556573
↑ Gorla-Bajszczak A, Juge-Aubry C, Pernin A, Burger AG, Meier CA. Conserved amino acids in the ligand-binding and tau(i) domains of the peroxisome proliferator-activated receptor alpha are necessary for heterodimerization with RXR. Mol Cell Endocrinol. 1999 Jan 25;147(1-2):37-47. PMID:10195690

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OCA

[1] Sher T, Yi HF, McBride OW, Gonzalez FJ. cDNA cloning, chromosomal mapping, and functional characterization of the human peroxisome proliferator activated receptor. Biochemistry. 1993 Jun 1;32(21):5598-604. PMID:7684926

[2] Juge-Aubry CE, Gorla-Bajszczak A, Pernin A, Lemberger T, Wahli W, Burger AG, Meier CA. Peroxisome proliferator-activated receptor mediates cross-talk with thyroid hormone receptor by competition for retinoid X receptor. Possible role of a leucine zipper-like heptad repeat. J Biol Chem. 1995 Jul 28;270(30):18117-22. PMID:7629123

[3] Yan ZH, Karam WG, Staudinger JL, Medvedev A, Ghanayem BI, Jetten AM. Regulation of peroxisome proliferator-activated receptor alpha-induced transactivation by the nuclear orphan receptor TAK1/TR4. J Biol Chem. 1998 May 1;273(18):10948-57. PMID:9556573

[4] Gorla-Bajszczak A, Juge-Aubry C, Pernin A, Burger AG, Meier CA. Conserved amino acids in the ligand-binding and tau(i) domains of the peroxisome proliferator-activated receptor alpha are necessary for heterodimerization with RXR. Mol Cell Endocrinol. 1999 Jan 25;147(1-2):37-47. PMID:10195690

[1]

[2]

[3]

[4]

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 8ywu is ON HOLD  until Paper Publication
+==Human PPAR alpha ligand binding domain in complex with a 1H-pyrazolo[3,4-b]pyridine-derived compound==
+<StructureSection load='8ywu' size='340' side='right'caption='[[8ywu]], [[Resolution|resolution]] 1.77&Aring;' scene=''>
-Authors: Tachibana, K., Morie, T., Fukuda, S., Yuzuriha, T., Ishimoto, K., Nunomura, K., Lin, B., Miyachi, H., Oki, H., Kawahara, K., Meguro, K., Nakagawa, S., Tsujikawa, K., Akai, S., Doi, T., Yoshida, T.
+== Structural highlights ==
+<table><tr><td colspan='2'>[[8ywu]] 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=8YWU OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8YWU FirstGlance]. <br>
-Description: Human PPAR alpha ligand binding domain in complex with a 1H-pyrazolo[3,4-b]pyridine-derived compound
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.77&#8491;</td></tr>
-[[Category: Unreleased Structures]]
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1LZ9:1-(4-fluorophenyl)-6-[2-[(5-methyl-2-phenyl-1,3-oxazol-4-yl)methoxy]ethyl]-3-pentan-3-yl-pyrazolo[3,4-b]pyridine-4-carboxylic+acid'>A1LZ9</scene></td></tr>
-[[Category: Morie, T]]
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8ywu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8ywu OCA], [https://pdbe.org/8ywu PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8ywu RCSB], [https://www.ebi.ac.uk/pdbsum/8ywu PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8ywu ProSAT]</span></td></tr>
-[[Category: Nakagawa, S]]
+</table>
-[[Category: Kawahara, K]]
+== Function ==
-[[Category: Doi, T]]
+[https://www.uniprot.org/uniprot/PPARA_HUMAN PPARA_HUMAN] Ligand-activated transcription factor. Key regulator of lipid metabolism. Activated by the endogenous ligand 1-palmitoyl-2-oleoyl-sn-glycerol-3-phosphocholine (16:0/18:1-GPC). Activated by oleylethanolamide, a naturally occurring lipid that regulates satiety (By similarity). Receptor for peroxisome proliferators such as hypolipidemic drugs and fatty acids. Regulates the peroxisomal beta-oxidation pathway of fatty acids. Functions as transcription activator for the ACOX1 and P450 genes. Transactivation activity requires heterodimerization with RXRA and is antagonized by NR2C2.<ref>PMID:7684926</ref> <ref>PMID:7629123</ref> <ref>PMID:9556573</ref> <ref>PMID:10195690</ref>
-[[Category: Tsujikawa, K]]
+== References ==
-[[Category: Ishimoto, K]]
+<references/>
-[[Category: Lin, B]]
+__TOC__
-[[Category: Fukuda, S]]
+</StructureSection>
-[[Category: Yoshida, T]]
+[[Category: Homo sapiens]]
-[[Category: Yuzuriha, T]]
+[[Category: Large Structures]]
-[[Category: Tachibana, K]]
+[[Category: Akai S]]
-[[Category: Akai, S]]
+[[Category: Doi T]]
-[[Category: Oki, H]]
+[[Category: Fukuda S]]
-[[Category: Nunomura, K]]
+[[Category: Ishimoto K]]
-[[Category: Miyachi, H]]
+[[Category: Kawahara K]]
-[[Category: Meguro, K]]
+[[Category: Lin B]]
+[[Category: Meguro K]]
+[[Category: Miyachi H]]
+[[Category: Morie T]]
+[[Category: Nakagawa S]]
+[[Category: Nunomura K]]
+[[Category: Oki H]]
+[[Category: Tachibana K]]
+[[Category: Tsujikawa K]]
+[[Category: Yoshida T]]
+[[Category: Yuzuriha T]]

8ywu: Difference between revisions

Latest revision as of 07:45, 9 April 2025

Human PPAR alpha ligand binding domain in complex with a 1H-pyrazolo[3,4-b]pyridine-derived compound

Structural highlights

Function

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