2yly

From Proteopedia

(Difference between revisions)

Revision as of 12:57, 22 July 2020

Sulfonamides as selective Estrogen Receptor beta Agonists.

Structural highlights

2yly is a 2 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	1yy4, 1u3s, 1x78, 1qkm, 1u3r, 1l2j, 2fsz, 1x7j, 1x7b, 1u9e, 1x76, 1nde, 1yye, 2jj3, 1u3q
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[ESR2_HUMAN] Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner. Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by ESR1 and ESR2 is rapidly lost at 37 degrees Celsius in the absence of ligand while in the presence of 17 beta-estradiol and 4-hydroxy-tamoxifen loss in DNA-binding at elevated temperature is more gradual.

Publication Abstract from PubMed

A series of p-hydroxybenzenesulphonamides ERbeta receptor agonists were discovered and several compounds identified had excellent selectivity over the related ERalpha receptor. One of these, compound 11, had an interesting binding conformation determined by X-ray and represents an excellent starting point in the quest for further selective ERbeta agonists.

Sulfonamides as selective oestrogen receptor beta agonists.,Roberts LR, Armor D, Barker C, Bent A, Bess K, Brown A, Favor DA, Ellis D, Irving SL, MacKenny M, Phillips C, Pullen N, Stennett A, Strand L, Styles M Bioorg Med Chem Lett. 2011 Oct 1;21(19):5680-3. Epub 2011 Aug 16. PMID:21885279^[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Roberts LR, Armor D, Barker C, Bent A, Bess K, Brown A, Favor DA, Ellis D, Irving SL, MacKenny M, Phillips C, Pullen N, Stennett A, Strand L, Styles M. Sulfonamides as selective oestrogen receptor beta agonists. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5680-3. Epub 2011 Aug 16. PMID:21885279 doi:10.1016/j.bmcl.2011.08.041

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/2yly"

@@ Line 1: / Line 1: @@
 ==Sulfonamides as selective Estrogen Receptor beta Agonists.==
-<StructureSection load='2yly' size='340' side='right' caption='[[2yly]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
+<StructureSection load='2yly' size='340' side='right'caption='[[2yly]], [[Resolution|resolution]] 3.20&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[2yly]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YLY OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2YLY FirstGlance]. <br>
+<table><tr><td colspan='2'>[[2yly]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YLY OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2YLY FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=SU4:N-CYCLOPROPYL-4-OXIDANYL-N-[(2R)-2-OXIDANYL-2-PHENYL-PROPYL]BENZENESULFONAMIDE'>SU4</scene></td></tr>
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>, <scene name='pdbligand=SU4:N-CYCLOPROPYL-4-OXIDANYL-N-[(2R)-2-OXIDANYL-2-PHENYL-PROPYL]BENZENESULFONAMIDE'>SU4</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[1yy4|1yy4]], [[1u3s|1u3s]], [[1x78|1x78]], [[1qkm|1qkm]], [[1u3r|1u3r]], [[1l2j|1l2j]], [[2fsz|2fsz]], [[1x7j|1x7j]], [[1x7b|1x7b]], [[1u9e|1u9e]], [[1x76|1x76]], [[1nde|1nde]], [[1yye|1yye]], [[2jj3|2jj3]], [[1u3q|1u3q]]</td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2yly FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2yly OCA], [http://pdbe.org/2yly PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2yly RCSB], [http://www.ebi.ac.uk/pdbsum/2yly PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2yly ProSAT]</span></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2yly FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2yly OCA], [http://pdbe.org/2yly PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2yly RCSB], [http://www.ebi.ac.uk/pdbsum/2yly PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2yly ProSAT]</span></td></tr>
 </table>
 == Function ==
@@ Line 21: / Line 21: @@
 ==See Also==
-*[[Estrogen receptor|Estrogen receptor]]
+*[[Estrogen receptor 3D structures|Estrogen receptor 3D structures]]
 == References ==
 <references/>
@@ Line 27: / Line 27: @@
 </StructureSection>
 [[Category: Human]]
+[[Category: Large Structures]]
 [[Category: Armour, D]]
 [[Category: Barker, C]]

2yly

From Proteopedia

Revision as of 12:57, 22 July 2020

Sulfonamides as selective Estrogen Receptor beta Agonists.

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

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