[Inhibition of TRPV2 Channel Activation by NK-4, a Cryptocyanine Dye]

Autor: Satomi Koya-Miyata, Keizo Kohno, Takashi Morimoto, Akira Harashima, Yuko Iwata, Toshio Ariyasu
Rok vydání: 2022
Předmět:
Zdroj: Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan. 142(5)
ISSN: 1347-5231
Popis: Transient receptor potential vanilloid 2 (TRPV2) channels are expressed and play functional roles in various immune cells. Physical stimuli leading to TRPV2 activation causes mast cell degranulation. Besides their roles in immune cells, it has been shown that TRPV2 channels are pathophysiologically relevant to degenerative muscular diseases such as dilated cardiomyopathy and muscular dystrophy. Hence, development of drug candidates that inhibit human TRPV2 activation is an urgent matter. NK-4, a cryptocyanine dye, inhibited agonist-induced TRPV2 activity in mouse TRPV2-transfected HEK293 cells. However, it remains unclear whether NK-4 exerts regulatory effects on the activation of human TRPV2 channels. In this study, we show that NK-4 inhibits intracellular Ca
Databáze: OpenAIRE