Synthesis and structure of 16,22-diketocholesterol bound to oxysterol-binding protein Osh4

Myong Chul Koag; Young Cheun; Yi Kou; Hala Ouzon-Shubeita; Kyungjin Min; Arthur F Monzingo; Seongmin Lee

doi:10.1016/j.steroids.2013.05.016

Synthesis and structure of 16,22-diketocholesterol bound to oxysterol-binding protein Osh4

Steroids. 2013 Sep;78(9):938-44. doi: 10.1016/j.steroids.2013.05.016. Epub 2013 Jun 10.

Authors

Myong Chul Koag¹, Young Cheun, Yi Kou, Hala Ouzon-Shubeita, Kyungjin Min, Arthur F Monzingo, Seongmin Lee

Affiliation

¹ Division of Medicinal Chemistry, College of Pharmacy, The University of Texas at Austin, Austin, TX 78712, USA.

PMID: 23756172
DOI: 10.1016/j.steroids.2013.05.016

Abstract

We have synthesized 16,22-diketocholesterol, a novel ligand for oxysterol-binding protein Osh4, and determined X-ray structure of the diketocholesterol in complex with Osh4. The X-ray structure shows that α7 helix of Osh4 assumes open conformation while the rest of Osh4, closed conformation, implying this diketocholesterol-bound Osh4 structure may represent a structural intermediate between the two conformations.

Keywords: Osh4; Oxysterol-binding proteins; Oxystrerols.

Publication types

Research Support, N.I.H., Extramural
Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

Binding Sites
Cholesterol / analogs & derivatives*
Cholesterol / chemical synthesis
Cholesterol / chemistry
Crystallography, X-Ray
Hydrogen Bonding
Hydrophobic and Hydrophilic Interactions
Membrane Proteins / chemistry*
Models, Molecular
Protein Binding
Protein Structure, Secondary
Protein Structure, Tertiary
Receptors, Steroid / chemistry*
Saccharomyces cerevisiae Proteins / chemistry*
Saccharomyces cerevisiae*

Substances

16,22-diketocholesterol
KES1 protein, S cerevisiae
Membrane Proteins
Receptors, Steroid
Saccharomyces cerevisiae Proteins
Cholesterol

Associated data

PDB/4FES