595608-06-3Relevant academic research and scientific papers
Analogues of the natural product sinefungin as inhibitors of EHMT1 and EHMT2
Devkota, Kanchan,Lohse, Brian,Liu, Qing,Wang, Ming-Wei,Staerk, Dan,Berthelsen, Jens,Clausen, Rasmus Praetorius
, p. 293 - 297 (2014/05/06)
A series of analogues of the natural product sinefungin lacking the amino acid moiety was synthesized and probed for their ability to inhibit EHMT1 and EHMT2. This study led to inhibitors 3b and 4d of methyltransferase activity of EHMT1 and EHMT2 and it demonstrates that such analogues constitute an interesting scaffold to develop selective methyltransferase inhibitors. Surprisingly, the inhibition was not competitive toward AdoMet.
Design, synthesis, and biological evaluation of novel human 5′-deoxy-5′-methylthioadenosine phosphorylase (MTAP) substrates
Kung, Pei-Pei,Zehnder, Luke R.,Meng, Jerry J.,Kupchinsky, Stanley W.,Skalitzky, Donald J.,Johnson, M. Catherine,Maegley, Karen A.,Ekker, Anne,Kuhn, Leslie A.,Rose, Peter W.,Bloom, Laura A.
, p. 2829 - 2833 (2007/10/03)
The structure-based design, chemical synthesis, and biological evaluation of novel MTAP substrates are described. These compounds incorporate various C5′-moieties and are shown to have different kcat/Km values compared with the natural MTAP substrate (MTA).
