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• W2174305362 abstract "Background: LSD-1 is an enzyme that removes methyl groups from lysine residues of histone proteins. LSD-1 inhibition decreases cellular proliferation and therefore represents a therapeutic target for cancer treatment. MAO and LSD-1 are both flavin adenine dinucleotide-dependent MAOs, and the MAO inhibitor, tranylcypromine, is currently undergoing clinical trials for cancer treatment because it acts as an irreversible LSD-1 inhibitor. Materials & methods: The present study investigated new reversible LSD-1 inhibitors, in order to develop novel selective anticancer agents. We constructed 2 and 3D quantitative structure–activity relationship models by using a series of 54 aminothiazole and thiazolesulfonamide derivatives. Results: The models were validated internally and externally (q 2 , 0.691 and 0.701; r 2 , 0.894 and 0.937; r 2 test , 0.785 and 0.644, for 2 and 3D models, respectively). Fragment contribution maps, as well as steric and electrostatic contour maps were generated in order to obtain chemical information related to LSD-1 inhibition. Conclusion: The thiazolesulfonamide group was fundamental to the inhibition of LSD-1 by these compounds and that bulky and aromatic substituents at the thiazole ring were important for their steric and electrostatic interactions with the active site of LSD-1." @default.
• W2174305362 created "2016-06-24" @default.
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• W2174305362 date "2015-08-01" @default.
• W2174305362 modified "2023-09-25" @default.
• W2174305362 title "Hologram quantitative structure–activity relationship and comparative molecular interaction field analysis of aminothiazole and thiazolesulfonamide as reversible LSD1 inhibitors" @default.
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• W2174305362 doi "https://doi.org/10.4155/fmc.15.68" @default.
• W2174305362 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26230878" @default.
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