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Highly expressed SERCA2 triggers tumor cell autophagy and is a druggable vulnerability in triple-negative breast cancer

Study Duration: Four to six weeks

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Reported applications include NNMT enzyme inhibition assays measuring 1-methylnicotinamide formation or S-adenosylhomocysteine release, intracellular target-engagement assays in differentiated 3T3-L1 adipocytes where 5-Amino-1MQ reduced intracellular 1-methylnicotinamide with an EC near 2.3 M (Neelakantan et al., Biochem Pharmacol, 2018), membrane permeability and Caco-2 transport characterisation, methyltransferase selectivity panels covering COMT, DNMT1 and PRMT3, and rodent studies of NNMT inhibition in adipose tissue and liver following the antisense knockdown work of Kraus and colleagues (Nature, 2014)

The implications of this effect are not well understood

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