Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
Agonists of NR2E3 (PNR, RNR) have been identified and optimized to EC(50)< 200 nM. A tritiated analogue of one agonist was prepared to aid in the development of a binding assay.
Wolkenberg
Scott E
SE
Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. scott_wolkenberg@merck.com
Zhao
Zhijian
Z
Kapitskaya
Marianna
M
Webber
Andrea L
AL
Petrukhin
Konstantin
K
Tang
Yui Sing
YS
Dean
Dennis C
DC
Hartman
George D
GD
Lindsley
Craig W
CW
D001562:Benzimidazoles / Q000633:toxicity*; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006801:Humans; D008024:Ligands; D008268:Macular Degeneration / Q000188:drug therapy* / Q000209:etiology; D009687:Nuclear Proteins / Q000378:metabolism; D056971:Nuclear Receptor Co-Repressor 1; D057093:Orphan Nuclear Receptors; D010786:Photoreceptor Cells; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D012097:Repressor Proteins / Q000819:agonists / Q000378:metabolism; D013329:Structure-Activity Relationship; D014157:Transcription Factors / Q000819:agonists*; D015533:Transcriptional Activation; D001618:beta-Lactamases / Q000235:genetics
D001562:Benzimidazoles; D008024:Ligands; C539127:NCOR1 protein, human; C403073:NR2E3 protein, human; D009687:Nuclear Proteins; D056971:Nuclear Receptor Co-Repressor 1; D057093:Orphan Nuclear Receptors; D018160:Receptors, Cytoplasmic and Nuclear; D012097:Repressor Proteins; D014157:Transcription Factors; D001618:beta-Lactamases