Small molecule Photoregulin3 prevents retinal degeneration in the <i>Rho<sup>P23H</sup></i> mouse model of retinitis pigmentosa.

Nakamura, Paul A; Shimchuk, Andy A; Tang, Shibing; Wang, Zhizhi; DeGolier, Kole; Ding, Sheng; Reh, Thomas A · Elife · 2017

basic_science · Level V

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Abstract

Regulation of rod gene expression has emerged as a potential therapeutic strategy to treat retinal degenerative diseases like retinitis pigmentosa (RP). We previously reported on a small molecule modulator of the rod transcription factor Nr2e3, Photoregulin1 (PR1), that regulates the expression of photoreceptor-specific genes. Although PR1 slows the progression of retinal degeneration in models of RP in vitro, in vivo analyses were not possible with PR1. We now report a structurally unrelated compound, Photoregulin3 (PR3) that also inhibits rod photoreceptor gene expression, potentially though Nr2e3 modulation. To determine the effectiveness of PR3 as a potential therapy for RP, we treated <i>Rho<sup>P23H</sup></i> mice with PR3 and assessed retinal structure and function. PR3-treated <i>Rho<sup>P23H</sup></i> mice showed significant structural and functional photoreceptor rescue compared with vehicle-treated littermate control mice. These results provide further support that pharmacological modulation of rod gene expression provides a potential strategy for the treatment of RP.

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