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Discovery of a First-in-Class CD38 Inhibitor for the Treatment of Mitochondrial Myopathy

11 Sept 2023

Abstract excerpt

CD38 is a crucial NADase in mammalian tissues that degrades NAD + and thus regulates cellular NAD + levels. Abnormal CD38 expression is linked to mitochondrial dysfunction under several pathological conditions. We present a novel CD38 inhibitor, compound 1, with high potency for CD38 (IC 50 of 11 nM) and minimal activity against other targets. In a Pus1 knockout (Pus1 –/– ) mouse model of mitochondrial myopathy,...

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PMID: 37696000
DOI: 10.1021/acs.jmedchem.3c00391

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