@article {Harrisjpet.116.237255, author = {Dorathy-Ann Harris and Ji-Min Park and Kyung Soon-Lee and Cong Xu and Nephi Stella and Chris Hague}, title = {Label-free dynamic mass redistribution reveals low density, pro-survival α1B-adrenergic receptors in human SW480 colon carcinoma cells}, elocation-id = {jpet.116.237255}, year = {2017}, doi = {10.1124/jpet.116.237255}, publisher = {American Society for Pharmacology and Experimental Therapeutics}, abstract = {Small molecules that target the adrenergic family of G protein-coupled receptors (GPCRs) show promising therapeutic efficacy for the treatment of various cancers. Herein, we report that human colon cancer cell line SW480 expresses low-density functional α1B-adrenergic receptors (ARs) as revealed by label-free dynamic mass redistribution (DMR) signaling technology and confirmed by quantitative reverse-transcriptase polymerase chain reaction analysis. Remarkably, while endogenous α1B-ARs are not detectable via either [3H]-prazosin binding analysis or phosphoinositol hydrolysis assays, their activation leads to robust DMR and enhanced cell viability. We provide pharmacological evidence that stimulation of α1B-ARs enhances SW480 cell viability without affecting proliferation, whereas stimulating β-ARs diminishes both viability and proliferation of SW480 cells. Our study illustrates the power of label-free DMR technology for identifying and characterizing low-density GPCRs in cells and suggests that drugs targeting both α1B- and β-ARs may represent valuable small molecule therapeutics for the treatment of colon cancer.}, issn = {0022-3565}, URL = {https://jpet.aspetjournals.org/content/early/2017/02/14/jpet.116.237255}, eprint = {https://jpet.aspetjournals.org/content/early/2017/02/14/jpet.116.237255.full.pdf}, journal = {Journal of Pharmacology and Experimental Therapeutics} }