CD38-IN-78c explained

CD38-IN-78c is a drug which acts as a potent and selective inhibitor of the glycoprotein enzyme CD38.^[1] In animal studies it boosts levels of nicotinamide adenine dinucleotide (NAD+) in tissues via inhibition of CD38 mediated breakdown of nicotinamide riboside (NR) and nicotinamide mononucleotide (NMN), and has been shown to ameliorate metabolic dysfunction associated with the aging process.^[2] It also has potential therapeutic application in the treatment of asthma.^[3]

Notes and References

1. Haffner CD, Becherer JD, Boros EE, Cadilla R, Carpenter T, Cowan D, Deaton DN, Guo Y, Harrington W, Henke BR, Jeune MR, Kaldor I, Milliken N, Petrov KG, Preugschat F, Schulte C, Shearer BG, Shearer T, Smalley TL, Stewart EL, Stuart JD, Ulrich JC . 6 . Discovery, Synthesis, and Biological Evaluation of Thiazoloquin(az)olin(on)es as Potent CD38 Inhibitors . Journal of Medicinal Chemistry . 58 . 8 . 3548–71 . April 2015 . 25828863 . 10.1021/jm502009h . 43192793 .
2. Tarragó MG, Chini CC, Kanamori KS, Warner GM, Caride A, de Oliveira GC, Rud M, Samani A, Hein KZ, Huang R, Jurk D, Cho DS, Boslett JJ, Miller JD, Zweier JL, Passos JF, Doles JD, Becherer DJ, Chini EN . A Potent and Specific CD38 Inhibitor Ameliorates Age-Related Metabolic Dysfunction by Reversing Tissue NAD+ Decline . Cell Metabolism . 27 . 5 . 1081–1095.e10 . May 2018 . 29719225 . 5935140 . 10.1016/j.cmet.2018.03.016 .
3. Deshpande DA, Guedes AG, Lund FE, Kannan MS . CD38 in the pathogenesis of allergic airway disease: Potential therapeutic targets . . 172 . 116–126 . 2017 . 10.1016/j.pharmthera.2016.12.002 . 5346344 . 27939939.