4flp
From Proteopedia
(Difference between revisions)
(One intermediate revision not shown.) | |||
Line 1: | Line 1: | ||
==Crystal Structure of the first bromodomain of human BRDT in complex with the inhibitor JQ1== | ==Crystal Structure of the first bromodomain of human BRDT in complex with the inhibitor JQ1== | ||
- | <StructureSection load='4flp' size='340' side='right' caption='[[4flp]], [[Resolution|resolution]] 2.23Å' scene=''> | + | <StructureSection load='4flp' size='340' side='right'caption='[[4flp]], [[Resolution|resolution]] 2.23Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
- | <table><tr><td colspan='2'>[[4flp]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[4flp]] 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=4FLP OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4FLP FirstGlance]. <br> |
- | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=JQ1:(6S)-6-(2-TERT-BUTOXY-2-OXOETHYL)-4-(4-CHLOROPHENYL)-2,3,9-TRIMETHYL-6,7-DIHYDROTHIENO[3,2-F][1,2,4]TRIAZOLO[4,3-A][1,4]DIAZEPIN-10-IUM'>JQ1</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</scene> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.23Å</td></tr> |
- | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=JQ1:(6S)-6-(2-TERT-BUTOXY-2-OXOETHYL)-4-(4-CHLOROPHENYL)-2,3,9-TRIMETHYL-6,7-DIHYDROTHIENO[3,2-F][1,2,4]TRIAZOLO[4,3-A][1,4]DIAZEPIN-10-IUM'>JQ1</scene>, <scene name='pdbligand=K:POTASSIUM+ION'>K</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=4flp FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4flp OCA], [https://pdbe.org/4flp PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4flp RCSB], [https://www.ebi.ac.uk/pdbsum/4flp PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4flp ProSAT]</span></td></tr> | |
- | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Function == | == Function == | ||
- | [ | + | [https://www.uniprot.org/uniprot/BRDT_HUMAN BRDT_HUMAN] Testis-specific chromatin protein that specifically binds histone H4 acetylated at 'Lys-5' and 'Lys-8' (H4K5ac and H4K8ac, respectively) and plays a key role in spermatogenesis. Required in late pachytene spermatocytes: plays a role in meiotic and post-meiotic cells by binding to acetylated histones at the promoter of specific meiotic and post-meiotic genes, facilitating their activation at the appropriate time. In the post-meiotic phase of spermatogenesis, binds to hyperacetylated histones and participates in their general removal from DNA. Also acts as a component of the splicing machinery in pachytene spermatocytes and round spermatids and participates in 3'-UTR truncation of specific mRNAs in post-meiotic spermatids. Required for chromocenter organization, a structure comprised of peri-centromeric heterochromatin.<ref>PMID:9367677</ref> <ref>PMID:15647849</ref> <ref>PMID:22901802</ref> |
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
- | [[Category: | + | [[Category: Homo sapiens]] |
- | [[Category: Arrowsmith | + | [[Category: Large Structures]] |
- | [[Category: Bountra | + | [[Category: Arrowsmith CH]] |
- | [[Category: Bradner | + | [[Category: Bountra C]] |
- | [[Category: Canning | + | [[Category: Bradner J]] |
- | + | [[Category: Canning P]] | |
- | [[Category: Edwards | + | [[Category: Edwards A]] |
- | [[Category: Felletar | + | [[Category: Felletar I]] |
- | [[Category: Filippakopoulos | + | [[Category: Filippakopoulos P]] |
- | [[Category: Knapp | + | [[Category: Knapp S]] |
- | [[Category: Muniz | + | [[Category: Muniz J]] |
- | [[Category: Picaud | + | [[Category: Picaud S]] |
- | [[Category: Qi | + | [[Category: Qi J]] |
- | [[Category: | + | [[Category: Von Delft F]] |
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + | ||
- | + |
Current revision
Crystal Structure of the first bromodomain of human BRDT in complex with the inhibitor JQ1
|
Categories: Homo sapiens | Large Structures | Arrowsmith CH | Bountra C | Bradner J | Canning P | Edwards A | Felletar I | Filippakopoulos P | Knapp S | Muniz J | Picaud S | Qi J | Von Delft F