RT Journal Article
SR Electronic
T1 Label-Free Dynamic Mass Redistribution Reveals Low-Density, Prosurvival <em>α</em><sub>1B</sub>-Adrenergic Receptors in Human SW480 Colon Carcinoma Cells
JF Journal of Pharmacology and Experimental Therapeutics
JO J Pharmacol Exp Ther
FD American Society for Pharmacology and Experimental Therapeutics
SP 219
OP 228
DO 10.1124/jpet.116.237255
VO 361
IS 2
A1 Harris, Dorathy-Ann
A1 Park, Ji-Min
A1 Lee, Kyung-Soon
A1 Xu, Cong
A1 Stella, Nephi
A1 Hague, Chris
YR 2017
UL http://jpet.aspetjournals.org/content/361/2/219.abstract
AB Small molecules that target the adrenergic family of G protein–coupled receptors (GPCRs) show promising therapeutic efficacy for the treatment of various cancers. In this study, 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, although 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.