title: Novel CoA-polyamine conjugates for effective inhibition of spermine/spermidine-N1-acetyltransferase.
abstract: 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.
authors: Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Vavilov Street 32, Moscow 119991, Russia.
authors: Alina
authors: A
authors: Simonian
authors: Alex
authors: A
authors: Khomutov
authors: Tapani
authors: T
authors: Hyvonen
authors: Nikolay
authors: N
authors: Grigorenko
authors: Tuomo
authors: T
authors: Keinanen
authors: Jouko
authors: J
authors: Vepsalainen
authors: Leena
authors: L
authors: Alhonen
authors: Juhani
authors: J
authors: Janne
mesh_terms: 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
chemical_list: D000123:Acetyltransferases; D000970:Antineoplastic Agents; D003065:Coenzyme A; D004791:Enzyme Inhibitors; D013095:Spermidine; D013096:Spermine; D000099228:Diamine N-Acetyltransferase