PGH1, the Precursor for the Anti-Inflammatory Prostaglandins of the 1-series, Is a Potent Activator of the Pro-Inflammatory Receptor CRTH2/DP2
Figure 1
Prostaglandin H1 (PGH1) fully activates CRTH2 in living CRTH2-HEK cell transfectants.
A–E, abilities of PGH1, selected prostaglandins, and the PGH1 precursor dihomo-γ-linolenic acid (DGLA) to stimulate CRTH2 signaling using dynamic mass redistribution (DMR) technology. Cells were challenged with increasing concentrations of the indicated ligands and DMR was recorded as a measure of receptor activity (representative optical traces). F, transformation of optical traces (A–E) into concentration effect curves. Molar log EC50 values were PGH1: −6.37±0.12; PGH2: −7.09±0.08; PGD1: −6.92±0.16; PGD2: −7.95±0.09 (mean values ± SEM, n = 3).