2acl: Difference between revisions

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

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

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

caption="2acl, resolution 2.8Å" />

'''Liver X-Receptor alpha Ligand Binding Domain with SB313987'''<br />

==Overview==

Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a, high throughput screen as inducers of human ATP binding cassette, transporter A1 expression. Mechanism of action studies led to the, identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid, receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40, nM, profiles as an LXR agonist in functional assays, and activates LXR, though a mechanism that is similar to first generation LXR agonists.

Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists.

==About this Structure==

2ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with L05 and REA as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=2ACL OCA].

2ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=L05:'>L05</scene> and <scene name='pdbligand=REA:'>REA</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ACL OCA].

==Reference==

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[[Category: Protein complex]]

[[Category: Campobasso, N.]]

[[Category: Jaye, M.C.]]

[[Category: Jaye, M C.]]

[[Category: Kerrigan, J.J.]]

[[Category: Kerrigan, J J.]]

[[Category: Krawiec, J.A.]]

[[Category: Krawiec, J A.]]

[[Category: Lu, Q.]]

[[Category: Qiu, C.]]

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[[Category: nuclear hormone receptor ligand binding domain transcription factor three layered a-helix fold]]

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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:07 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2acl.gif|left|200px]]<br />
+[[Image:2acl.gif|left|200px]]<br /><applet load="2acl" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2acl" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2acl, resolution 2.8&Aring;" />
 '''Liver X-Receptor alpha Ligand Binding Domain with SB313987'''<br />
 ==Overview==
-Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a, high throughput screen as inducers of human ATP binding cassette, transporter A1 expression. Mechanism of action studies led to the, identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid, receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40, nM, profiles as an LXR agonist in functional assays, and activates LXR, though a mechanism that is similar to first generation LXR agonists.
+Substituted 3-(phenylamino)-1H-pyrrole-2,5-diones were identified from a high throughput screen as inducers of human ATP binding cassette transporter A1 expression. Mechanism of action studies led to the identification of GSK3987 as an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM, profiles as an LXR agonist in functional assays, and activates LXR though a mechanism that is similar to first generation LXR agonists.
 ==About this Structure==
-ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with L05 and REA as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2ACL OCA].
+ACL is a [http://en.wikipedia.org/wiki/Protein_complex Protein complex] structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus] with <scene name='pdbligand=L05:'>L05</scene> and <scene name='pdbligand=REA:'>REA</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2ACL OCA].
 ==Reference==
@@ Line 16: / Line 15: @@
 [[Category: Protein complex]]
 [[Category: Campobasso, N.]]
-[[Category: Jaye, M.C.]]
+[[Category: Jaye, M C.]]
-[[Category: Kerrigan, J.J.]]
+[[Category: Kerrigan, J J.]]
-[[Category: Krawiec, J.A.]]
+[[Category: Krawiec, J A.]]
 [[Category: Lu, Q.]]
 [[Category: Qiu, C.]]
@@ Line 26: / Line 25: @@
 [[Category: nuclear hormone receptor ligand binding domain transcription factor three layered a-helix fold]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 20:48:50 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 16:26:07 2008''