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SRC2-3 binds to vitamin D receptor with high sensitivity and strong affinity.

Abstract：

:Vitamin D receptor (VDR) is a member of the nuclear receptor superfamily and regulates the expression of target genes through ligand binding. To express the target gene, coactivator binding to the VDR/ligand complex is essential. Although there are many coactivators in living cells, precise interactions between coactivators and VDR have not been clarified. Here, we synthesized two coactivator peptides, DRIP205-2 and SRC2-3, evaluated their affinity for the ligand-binding domain (LBD) of VDR using 1α,25-dihydroxyvitamin D3, partial agonist 1, and antagonist 2 by surface plasmon resonance (SPR), and assessed their interaction modes with VDR-LBD using X-ray crystallographic analysis. This study showed that the SRC2-3 peptide is more sensitive to the ligands (agonist, partial agonist, and antagonist) and shows more intimate interactions with VDR-LBD than DRIP205-2 peptide.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Egawa D,Itoh T,Kato A,Kataoka S,Anami Y,Yamamoto K

doi

10.1016/j.bmc.2016.11.020

subject

Has Abstract

pub_date

2017-01-15 00:00:00

pages

568-574

issue

2

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30847-1

journal_volume

25

pub_type

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