1373432-58-6Relevant articles and documents
Development of rationally designed DNA N6 adenine methyltransferase inhibitors
Hobley, Gerard,McKelvie, Jennifer C.,Harmer, Jenny E.,Howe, Jason,Oyston, Petra C.F.,Roach, Peter L.
, p. 3079 - 3082 (2012/06/17)
A series of bisubstrate inhibitors for DNA N6 adenine methyltransferase (Dam) have been synthesized by linking an amine analogue of S-adenosylmethionine to an aryl moiety designed to probe the binding pocket of the DNA adenine base. An initial structure-activity relationship study has identified substituents that increase inhibitor potency to the ~10 μM range and improve selectivity against the human cytosine methyltransferase Dnmt1.