1α,25-Dihydroxyvitamin D3-3β-bromoacetate, an Affinity-Labeling Analog of 1α,25-Dihydroxyvitamin D3 Receptor

✍ Scribed by R. Ray; S. Ray; M.F. Holick

• Publisher: Elsevier Science
• Year: 1994
• Tongue: English
• Weight: 373 KB
• Volume: 22
• Category: Article
• ISSN: 0045-2068
• DOI: 10.1006/bioo.1994.1021

✦ Synopsis

In this communication we describe the synthesis of (1 \alpha, 25)-dihydroxyvitamin (\mathrm{D}{3}) - (3 \beta)-bromoacetate (\left[1,25(\mathrm{OH}){2}-\mathrm{BE}\right]), an analog of (1 \alpha, 25)-dihydroxyvitamin (\mathrm{D}{3}\left[1,25(\mathrm{OH}){2} \mathrm{D}{3}\right]), as a part of our ongoing interest in characterizing the hormone-binding domain of the (1 \alpha, 25) dihydroxyvitamin (D{3}) receptor (VDR). We carried out several binding studies of (1,25(\mathrm{OH}){2}) (\mathrm{BE}) with chick intestinal VDR preparations to demonstrate that (1,25(\mathrm{OH}){2}-\mathrm{BE}) is capable of blocking the entry of (1,25(\mathrm{OH}){2} \mathrm{D}{3}) into its binding pocket and possibly covalently linking to the VDR molcule. 1994 Academic Press. Inc