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.
Department of Medicinal Chemistry and Molecular Pharmacology, Purdue University, West Lafayette, Indiana 47907, USA. rossw@pharmacy.purdue.edu
Ross V
RV
Weatherman
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