Alanine scanning mutational analysis of the ligand binding pocket of the human Vitamin D receptor

Keiko Yamamoto, Mihwa Choi, Daijiro Abe, Masato Shimizu, Sachiko Yamada

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

We achieved exhaustive alanine scanning mutational analysis of the amino acid residues lining the ligand binding pocket of the Vitamin D receptor to investigate the mechanism of the ligand recognition by the receptor. This is the first exhaustive analysis in the nuclear receptor superfamily. Our results demonstrated the role and importance of all the residues lining the ligand binding pocket. In addition, this analysis was found to indicate ligand-specific ligand-protein interactions, which have key importance in determining the transactivation potency of the individual ligands. Thus, the analysis using 1β-methyl-1α,25-dihydroxyvitamin D3 revealed the specific van der Waals interactions of 1β-methyl group with the receptor.

Original languageEnglish (US)
Pages (from-to)282-285
Number of pages4
JournalJournal of Steroid Biochemistry and Molecular Biology
Volume103
Issue number3-5
DOIs
StatePublished - Mar 1 2007
Externally publishedYes

Keywords

  • 1α,25-Dihydroxyvitamin D
  • Alanine scanning mutational analysis
  • Ligand binding
  • Ligand recognition
  • Vitamin D
  • Vitamin D receptor

ASJC Scopus subject areas

  • Endocrinology, Diabetes and Metabolism
  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Endocrinology
  • Clinical Biochemistry
  • Cell Biology

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