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- W4377029376 abstract "<b>Abstract ID 14268</b> <b>Poster Board 314</b> Aberrant calcium signaling has intimate associations with multiple diseases. Upregulation of transient receptor potential canonical 3 (TRPC3), which is an ion channel that essentially mediates calcium influx, drives the progression of neurodegenerative diseases. We previously designed <b>JW-65</b>, a selective TRPC3 inhibitor with a favorable safety profile and good metabolic stability. However, <b>JW-65</b> has moderate potency (IC<sub>50</sub> = 330 nM) and selectivity for TRPC3 inhibition. Here we report a synthetic <b>JW-65</b> analog, <b>60a</b>, with significantly improved potency and selectivity. <b>60a</b> is a potent TRPC3 inhibitor (IC<sub>50</sub> = 90 nM) with no detectable inhibitory effect on the close homologs TRPC6/7, highlighting <b>60a</b> as the first truly selective TRPC3 inhibitor. <i>In vitro</i> evaluations of <b>60a</b> reveal its rescuing abilities on neuronal damage. <i>In vivo</i> studies indicate <b>60a</b> is a promising candidate for further development as a potential AD therapy with a novel mechanism of action. This work was supported by the University of Tennessee College of Pharmacy Drug Discovery Center and NIH grant R61NS124923 to WL." @default.
- W4377029376 created "2023-05-19" @default.
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- W4377029376 date "2023-05-18" @default.
- W4377029376 modified "2023-10-16" @default.
- W4377029376 title "A Selective TRPC3 Antagonist Rescues Neuronal Loss and Facilitates Spatial Learning and Memory in Alzheimer's Model" @default.
- W4377029376 doi "https://doi.org/10.1124/jpet.122.142680" @default.
- W4377029376 hasPublicationYear "2023" @default.
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