Affinity labeling of the nuclear vitamin D receptor with nonsteroidal alkylating agents.
Synthesis of an affinity alkylating non steroidal mimic of 1alpha,25-dihydroxyvitamin D(3) and its radiolabeled counterpart is presented. We also report the affinity labeling of the VDR-ligand binding domain (VDR-LBD) with this analogue.
Fernández-Gacio
Ana
A
Bioorganic Chemistry and Structural Biology, Section in Endocrinology, Diabetes and Metabolism, Department of Medicine, Boston University School of Medicine, 85 East Newton Street, Boston, MA 02118, USA.
Fernández-Marcos
Carlos
C
Swamy
Narasimha
N
Ray
Rahul
R
D000345:Affinity Labels; D000477:Alkylating Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002117:Calcitriol / Q000737:chemistry; D004967:Estrogens / Q000737:chemistry / Q000494:pharmacology; D007202:Indicators and Reagents; D018716:Molecular Mimicry; D018167:Receptors, Calcitriol / Q000187:drug effects*; D018160:Receptors, Cytoplasmic and Nuclear / Q000187:drug effects*; D011960:Receptors, Estrogen / Q000187:drug effects
D000345:Affinity Labels; D000477:Alkylating Agents; D004967:Estrogens; D007202:Indicators and Reagents; D018167:Receptors, Calcitriol; D018160:Receptors, Cytoplasmic and Nuclear; D011960:Receptors, Estrogen; D002117:Calcitriol