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=1722560852&Signature=ebPHxriQA5nM702zDrrbmErnQLip7cxXEkjzLg3Iuu-dHTQGHDnslPys~fBqs~AJmj7JWyP4kEmlqNxWt4T9cQe6OgcLw0~oKAihdUk~Bc53WHPwOOEvBTL-395Y~pKJOY5UslCsG3MQVC6aqPxwiI8L78BJE-pA7qYjMKbBcoVF1JHn5kHaV~YdHuzJbgzSzSnPRR~XFYj2ulYMic86fKbfhqGFCbNx4Rr8W3rwMmUEJ8vZ8BeIr50vJMYrzenSO2nv79fwKZ1a-xKdBhuzdo174kcxj4VFj2yizproC3sOOA9EKqI1cYSQNNbOP47DKae0SLUG8rl~MSVuoDN1sQ__&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).
