2ewp: Difference between revisions

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[[Image:2ewp.gif|left|200px]]<br />

[[Image:2ewp.gif|left|200px]]<br /><applet load="2ewp" size="350" color="white" frame="true" align="right" spinBox="true"

<applet load="2ewp" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

caption="2ewp, resolution 2.30Å" />

'''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''<br />

==Overview==

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are, described. The binding affinities of these compounds toward the orphan, estrogen-related receptor gamma and the classical estrogen receptor alpha, demonstrate that analogs bearing hydroxyalkyl groups display improved, binding selectivity profiles compared with that of 4-OHT. An X-ray crystal, structure of one of the designed compounds bound to ERRgamma LBD confirms, the molecular basis of the selectivity.

The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.

==About this Structure==

2EWP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with TXF as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=2EWP OCA].

2EWP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=TXF:'>TXF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2EWP OCA].

==Reference==

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[[Category: Homo sapiens]]

[[Category: Single protein]]

[[Category: Nolte, R.T.]]

[[Category: Nolte, R T.]]

[[Category: TXF]]

[[Category: err]]

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[[Category: tamoxifen]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Mon Nov 12~~ 21:56:~~42 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:15:19 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2ewp.gif|left|200px]]<br />
+[[Image:2ewp.gif|left|200px]]<br /><applet load="2ewp" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2ewp" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2ewp, resolution 2.30&Aring;" />
 '''Crystal structure of Estrogen Related Reecptor-3 (ERR-gamma) ligand binding domaind with tamoxifen analog GSK5182'''<br />
 ==Overview==
-The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are, described. The binding affinities of these compounds toward the orphan, estrogen-related receptor gamma and the classical estrogen receptor alpha, demonstrate that analogs bearing hydroxyalkyl groups display improved, binding selectivity profiles compared with that of 4-OHT. An X-ray crystal, structure of one of the designed compounds bound to ERRgamma LBD confirms, the molecular basis of the selectivity.
+The design and synthesis of 4-hydroxytamoxifen (4-OHT) derivatives are described. The binding affinities of these compounds toward the orphan estrogen-related receptor gamma and the classical estrogen receptor alpha demonstrate that analogs bearing hydroxyalkyl groups display improved binding selectivity profiles compared with that of 4-OHT. An X-ray crystal structure of one of the designed compounds bound to ERRgamma LBD confirms the molecular basis of the selectivity.
 ==About this Structure==
-EWP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with TXF as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2EWP OCA].
+EWP is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=TXF:'>TXF</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2EWP OCA].
 ==Reference==
@@ Line 14: / Line 13: @@
 [[Category: Homo sapiens]]
 [[Category: Single protein]]
-[[Category: Nolte, R.T.]]
+[[Category: Nolte, R T.]]
 [[Category: TXF]]
 [[Category: err]]
@@ Line 21: / Line 20: @@
 [[Category: tamoxifen]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 21:56:42 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:15:19 2008''