3l0e
From Proteopedia
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{{STRUCTURE_3l0e| PDB=3l0e | SCENE= }} | {{STRUCTURE_3l0e| PDB=3l0e | SCENE= }} | ||
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===X-ray crystal structure of a Potent Liver X Receptor Modulator=== | ===X-ray crystal structure of a Potent Liver X Receptor Modulator=== | ||
| + | {{ABSTRACT_PUBMED_20345102}} | ||
| + | ==Disease== | ||
| + | [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation. | ||
| - | + | ==Function== | |
| - | + | [[http://www.uniprot.org/uniprot/NR1H2_HUMAN NR1H2_HUMAN]] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity). [[http://www.uniprot.org/uniprot/NCOA2_HUMAN NCOA2_HUMAN]] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.<ref>PMID:9430642</ref> | |
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==About this Structure== | ==About this Structure== | ||
| - | + | [[3l0e]] is a 2 chain structure with 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=3L0E OCA]. | |
==Reference== | ==Reference== | ||
| - | <ref group="xtra">PMID: | + | <ref group="xtra">PMID:020345102</ref><references group="xtra"/><references/> |
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
| - | [[Category: | + | [[Category: Gampe, R T.]] |
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[[Category: Activator]] | [[Category: Activator]] | ||
[[Category: Dna-binding]] | [[Category: Dna-binding]] | ||
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[[Category: Nucleus]] | [[Category: Nucleus]] | ||
[[Category: Phosphoprotein]] | [[Category: Phosphoprotein]] | ||
| - | [[Category: Polymorphism]] | ||
[[Category: Receptor]] | [[Category: Receptor]] | ||
[[Category: Sulfonamide modulator]] | [[Category: Sulfonamide modulator]] | ||
[[Category: Transcription]] | [[Category: Transcription]] | ||
[[Category: Transcription regulation]] | [[Category: Transcription regulation]] | ||
| - | [[Category: Zinc]] | ||
[[Category: Zinc-finger]] | [[Category: Zinc-finger]] | ||
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| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu May 20 09:02:20 2010'' | ||
Revision as of 19:38, 24 March 2013
Contents |
X-ray crystal structure of a Potent Liver X Receptor Modulator
Template:ABSTRACT PUBMED 20345102
Disease
[NCOA2_HUMAN] Note=Chromosomal aberrations involving NCOA2 may be a cause of acute myeloid leukemias. Inversion inv(8)(p11;q13) generates the KAT6A-NCOA2 oncogene, which consists of the N-terminal part of KAT6A and the C-terminal part of NCOA2/TIF2. KAT6A-NCOA2 binds to CREBBP and disrupts its function in transcription activation.
Function
[NR1H2_HUMAN] Orphan receptor. Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (By similarity). [NCOA2_HUMAN] Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to control energy balance between white and brown adipose tissues.[1]
About this Structure
3l0e is a 2 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Zuercher WJ, Buckholz RG, Campobasso N, Collins JL, Galardi CM, Gampe RT, Hyatt SM, Merrihew SL, Moore JT, Oplinger JA, Reid PR, Spearing PK, Stanley TB, Stewart EL, Willson TM. Discovery of Tertiary Sulfonamides as Potent Liver X Receptor Antagonists. J Med Chem. 2010 Mar 26. PMID:20345102 doi:10.1021/jm901797p
- ↑ Voegel JJ, Heine MJ, Tini M, Vivat V, Chambon P, Gronemeyer H. The coactivator TIF2 contains three nuclear receptor-binding motifs and mediates transactivation through CBP binding-dependent and -independent pathways. EMBO J. 1998 Jan 15;17(2):507-19. PMID:9430642 doi:10.1093/emboj/17.2.507
