Responses of GPCR135 to human gene 3 (H3) relaxin in CHO-K1 cells determined by microphysiometry.
This study examined the functional response to human relaxin 2 (H2 relaxin), human relaxin 3 (H3 relaxin), porcine relaxin, and human INSL3 in the cytosensor microphysiometer, using CHO-K1 cells stably expressing human GPCR135. CHO-K1 cells stably expressing GPCR135 were generated by the serial dilution method and receptor properties were assessed. Saturation studies of [125I] H3 relaxin binding to GPCR135 in these cells gave a Bmax of 32.61 +/- 6.5 fmol/mg protein and Kd of 0.12 +/- 0.08 nM. The functional response to H3 relaxin and other relaxin/insulin peptides of GPCR135 expressed in CHO-K1 cells was measured in the cytosensor microphysiometer and analyzed using inhibitors of signal transduction proteins.
Van der Westhuizen
Emma T
ET
Department of Pharmacology, Monash University, Clayton 3168, Australia.
Sexton
Patrick M
PM
Bathgate
Ross A D
RA
Summers
Roger J
RJ
D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D043562:Receptors, G-Protein-Coupled / Q000235:genetics / Q000378:metabolism*; D012065:Relaxin / Q000031:analogs & derivatives* / Q000235:genetics / Q000378:metabolism; D015398:Signal Transduction
C480238:RLN3 protein, human; C410092:RXFP3 protein, human; D043562:Receptors, G-Protein-Coupled; D012065:Relaxin