Novel CoA-polyamine conjugates for effective inhibition of spermine/spermidine-N1-acetyltransferase.
New mimics of the transition state of spermine/spermidine-N(1)-acetyltransferase reaction were prepared starting from aminooxy analogues of spermidine or spermine and SH-CoA. The activity depended on the structure of polyamine fragment of the conjugate and best of the synthesized compounds were active at micromolar concentrations.
Simonian
Alina
A
Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilov Street 32, Moscow 119991, Russia.
Khomutov
Alex
A
Hyvonen
Tapani
T
Grigorenko
Nikolay
N
Keinanen
Tuomo
T
Vepsalainen
Jouko
J
Alhonen
Leena
L
Janne
Juhani
J
D000123:Acetyltransferases / Q000037:antagonists & inhibitors*; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003065:Coenzyme A / Q000737:chemistry; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D018716:Molecular Mimicry; D013095:Spermidine / Q000031:analogs & derivatives*; D013096:Spermine / Q000031:analogs & derivatives*; D013329:Structure-Activity Relationship; D000099228:Diamine N-Acetyltransferase
D000123:Acetyltransferases; D000970:Antineoplastic Agents; D003065:Coenzyme A; D004791:Enzyme Inhibitors; D013095:Spermidine; D013096:Spermine; D000099228:Diamine N-Acetyltransferase