Target Validation Information
TTD ID T92308
Target Name DNA [cytosine-5]-methyltransferase (DNMT)
Type of Target
Successful
Drug Potency against Target Azacitidine Drug Info IC50 = 36800 nM [4]
(L-)-S-adenosyl-L-homocysteine Drug Info IC50 = 4000 nM [3]
(L-)-S-adenosyl-L-homocysteine Drug Info IC50 = 800 nM [2]
S-tubercidinylhomocysteine Drug Info IC50 = 1500 nM [1]
References
REF 1 SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes. Bioorg Med Chem Lett. 2009 May 15;19(10):2747-51.
REF 2 Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors. Bioorg Med Chem Lett. 2009 May 15;19(10):2742-6.
REF 3 Novel and selective DNA methyltransferase inhibitors: Docking-based virtual screening and experimental evaluation. Bioorg Med Chem. 2010 Jan 15;18(2):822-9.
REF 4 Mechanism of action of key enzymes associated with cancer propagation and their inhibition by various chemotherapeutic agents. Mini Rev Med Chem. 2008 Apr;8(4):388-98.

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