Figure 1
![Figure 1. Identification of 2 classes of PAR1 antagonists. (A) Structure of parmodulins. (B) Structure of orthosteric inhibitors. The effect of vehicle (N/A), 10 μM parmodulin 1 (PM1), 3 μM parmodulin 2 (PM2), 10 μM parmodulin 3 (PM3), 10 μM parmodulin 4 (PM4), 0.3 μM vorapaxar (V), 0.3 μM atopaxar (A), 3 μM SCH79797 (S), or 3 μM BMS-200261 (B) on SFLLRN-induced [Ca2+]i was evaluated in COS-7 transfected with (C) PAR1 or (D) PAR1/PAR4CT, in which the cytoplasmic tail of PAR1 (white) is replaced with that of PAR4 (gray). Increase in [Ca2+]i flux after stimulation with 5 μM SFLLRN was evaluated. Data are presented as means ± standard error of the mean (SEM) (n = 6).](https://ash.silverchair-cdn.com/ash/content_public/journal/blood/125/12/10.1182_blood-2014-09-599910/4/1976f1.jpeg?Expires=1736048360&Signature=wUyJ01PH8xytqdoWURLUho0CORs1GZnxxmXq8TTQEzEiwHoKV3WKmTzUbiiNCCyCwx35acVG-GmCC89CG8Pgf9DDR2tRIFHiyu~41sycogCyUAzevQZXcdJ0VNBdiQpWSqTsqF2XqPpoAciS-aCjgNQ7GVMH9nDRJOhN9wx4CCjrYyg4dtTlK~G1L0wf5cU0hWmQkGfvlo6bPhGtQYNXQmrPfmj1ucyPWw1F3zvdOI1s~Dm-15ttmHNy9Bz3BaV7ExBs9SmkV9wxsp4GWjHBlKH0SdqhUhHR672L4Dfm3EsjUIGyH9U~BVZ2nfS~Z0yGOEcrZ-ycNn2gmNorb4xEMg__&Key-Pair-Id=APKAIE5G5CRDK6RD3PGA)
Identification of 2 classes of PAR1 antagonists. (A) Structure of parmodulins. (B) Structure of orthosteric inhibitors. The effect of vehicle (N/A), 10 μM parmodulin 1 (PM1), 3 μM parmodulin 2 (PM2), 10 μM parmodulin 3 (PM3), 10 μM parmodulin 4 (PM4), 0.3 μM vorapaxar (V), 0.3 μM atopaxar (A), 3 μM SCH79797 (S), or 3 μM BMS-200261 (B) on SFLLRN-induced [Ca2+]i was evaluated in COS-7 transfected with (C) PAR1 or (D) PAR1/PAR4CT, in which the cytoplasmic tail of PAR1 (white) is replaced with that of PAR4 (gray). Increase in [Ca2+]i flux after stimulation with 5 μM SFLLRN was evaluated. Data are presented as means ± standard error of the mean (SEM) (n = 6).
