Sensing estrogen's many pathways.
Estrogen receptor (ER) is an important drug target, but it has multiple signaling pathways that are difficult to dissect. A new study reports the development of a multicolor bioluminescent probe that can measure a compound's ability to modulate ER-mediated transcription and to promote an interaction between ER and Src, a key protein in a number of different cell signaling cascades. The discovery provides a new tool for quickly obtaining a more complete picture of the potential effects of a compound on estrogen signaling and could lead to more selective ER modulators with fewer side effects.
Weatherman
Ross V
RV
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana 47907, USA. rossw@pharmacy.purdue.edu
D000818:Animals; D018931:Antineoplastic Agents, Hormonal / Q000378:metabolism / Q000627:therapeutic use; D015374:Biosensing Techniques / Q000379:methods*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D020847:Estrogen Receptor Modulators / Q000378:metabolism / Q000627:therapeutic use; D004967:Estrogens / Q000032:analysis / Q000235:genetics / Q000378:metabolism*; D005260:Female; D006801:Humans; D049408:Luminescent Agents / Q000737:chemistry*; D008163:Luminescent Measurements / Q000379:methods*; D011960:Receptors, Estrogen / Q000032:analysis / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction; D014158:Transcription, Genetic; D019061:src-Family Kinases / Q000032:analysis / Q000235:genetics / Q000378:metabolism
D018931:Antineoplastic Agents, Hormonal; D020847:Estrogen Receptor Modulators; D004967:Estrogens; D049408:Luminescent Agents; D011960:Receptors, Estrogen; D019061:src-Family Kinases