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Photocaged Agonist for an Analogue‐Specific form of the Vitamin D Receptor
Author(s) -
Biggins John B.,
Hashimoto Atsushi,
Koh John T.
Publication year - 2007
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200600497
Subject(s) - agonist , calcitriol receptor , ligand (biochemistry) , receptor , nuclear receptor , chemistry , mutant , microbiology and biotechnology , computational biology , biology , gene , biochemistry , transcription factor
Nuclear hormone receptors (NHRs) represent a diverse class of ligand‐dependent transcriptional regulators. NHRs that have been rendered functionally inactive due to mutations that abrogate proper ligand binding can often be rescued by appropriately designed hormone analogues. The analogue‐specific receptor–ligand pairs provide an ideal platform from which to develop new chemogenomic tools for the spatial and temporal control of gene expression. Here, we describe the synthesis and in vitro assessment of a photocaged VDR agonist specific to a mutant NHR that is associated with vitamin D‐resistant rickets. The results provide insight into the utility of the agonist as a potential tool for photoinduced gene patterning.