3cs4: Difference between revisions

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[[Image:3cs4.~~jpg~~|left|200px]]

[[Image:3cs4.png|left|200px]]

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~~'''~~Structure-based design of a superagonist ligand for the vitamin D nuclear receptor~~'''~~

===Structure-based design of a superagonist ligand for the vitamin D nuclear receptor===

~~==Overview==~~

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~~Vitamin D nuclear receptor (VDR)~~, a ligand-dependent transcriptional regulator, is an important target for multiple clinical applications, such as osteoporosis and cancer. Since exacerbated increase of calcium serum level is currently associated with VDR ligands action, ~~superagonists with low calcium serum levels have been developed. Based on~~ the ~~crystal structures of human VDR (hVDR) bound~~ to ~~1alpha,25-dihydroxyvitamin D~~(~~3) and superagonists-notably, KH1060-we designed a superagonist ligand~~. ~~In order to optimize the aliphatic side chain conformation with a subsequent entropy benefit, we incorporated an oxolane ring and generated two stereo diasteromers, AMCR277A and AMCR277B~~. ~~Only AMCR277A exhibits superagonist activity in vitro~~, ~~but~~ is ~~as calcemic in vivo as~~ the natural ligand. The crystal structures of the complexes between the ligand binding domain of hVDR and these ligands provide a rational approach to the design of more potent superagonist ligands for potential clinical application.

The line below this paragraph, {{ABSTRACT_PUBMED_18420145}}, adds the Publication Abstract to the page

(as it appears on PubMed at http://www.pubmed.gov), where 18420145 is the PubMed ID number.

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==About this Structure==

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[[Category: Zinc]]

[[Category: Zinc-finger]]

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on ~~Wed May~~ 28 09:23:32 2008''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:16:29 2008''

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-[[Image:3cs4.jpg|left|200px]]
+{{Seed}}
+[[Image:3cs4.png|left|200px]]
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 {{STRUCTURE_3cs4|  PDB=3cs4  |  SCENE=  }}
-'''Structure-based design of a superagonist ligand for the vitamin D nuclear receptor'''
+===Structure-based design of a superagonist ligand for the vitamin D nuclear receptor===
-==Overview==
+<!--
-Vitamin D nuclear receptor (VDR), a ligand-dependent transcriptional regulator, is an important target for multiple clinical applications, such as osteoporosis and cancer. Since exacerbated increase of calcium serum level is currently associated with VDR ligands action, superagonists with low calcium serum levels have been developed. Based on the crystal structures of human VDR (hVDR) bound to 1alpha,25-dihydroxyvitamin D(3) and superagonists-notably, KH1060-we designed a superagonist ligand. In order to optimize the aliphatic side chain conformation with a subsequent entropy benefit, we incorporated an oxolane ring and generated two stereo diasteromers, AMCR277A and AMCR277B. Only AMCR277A exhibits superagonist activity in vitro, but is as calcemic in vivo as the natural ligand. The crystal structures of the complexes between the ligand binding domain of hVDR and these ligands provide a rational approach to the design of more potent superagonist ligands for potential clinical application.
+The line below this paragraph, {{ABSTRACT_PUBMED_18420145}}, adds the Publication Abstract to the page
+(as it appears on PubMed at http://www.pubmed.gov), where 18420145 is the PubMed ID number.
+-->
+{{ABSTRACT_PUBMED_18420145}}
 ==About this Structure==
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 [[Category: Zinc]]
 [[Category: Zinc-finger]]
-''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed May 28 09:23:32 2008''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:16:29 2008''