Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand

Scott E Wolkenberg; Zhijian Zhao; Marianna Kapitskaya; Andrea L Webber; Konstantin Petrukhin; Yui Sing Tang; Dennis C Dean; George D Hartman; Craig W Lindsley

doi:10.1016/j.bmcl.2006.07.056

Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand

Bioorg Med Chem Lett. 2006 Oct 1;16(19):5001-4. doi: 10.1016/j.bmcl.2006.07.056. Epub 2006 Aug 1.

Authors

Scott E Wolkenberg¹, Zhijian Zhao, Marianna Kapitskaya, Andrea L Webber, Konstantin Petrukhin, Yui Sing Tang, Dennis C Dean, George D Hartman, Craig W Lindsley

Affiliation

¹ Department of Medicinal Chemistry, Technology Enabled Synthesis Group, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. scott_wolkenberg@merck.com

PMID: 16879962
DOI: 10.1016/j.bmcl.2006.07.056

Abstract

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.

MeSH terms

Benzimidazoles / toxicity*
Cell Line
Cell Survival / drug effects
Humans
Ligands
Macular Degeneration / drug therapy*
Macular Degeneration / etiology
Nuclear Proteins / metabolism
Nuclear Receptor Co-Repressor 1
Orphan Nuclear Receptors
Photoreceptor Cells*
Receptors, Cytoplasmic and Nuclear / agonists*
Repressor Proteins / agonists
Repressor Proteins / metabolism
Structure-Activity Relationship
Transcription Factors / agonists*
Transcriptional Activation
beta-Lactamases / genetics

Substances

Benzimidazoles
Ligands
NCOR1 protein, human
NR2E3 protein, human
Nuclear Proteins
Nuclear Receptor Co-Repressor 1
Orphan Nuclear Receptors
Receptors, Cytoplasmic and Nuclear
Repressor Proteins
Transcription Factors
beta-Lactamases