Identification of long chain alkylidenemalonates as novel small molecule modulators of histone acetyltransferases
Bioorganic & medicinal chemistry letters, 2008•Elsevier
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the
first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT
activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic
effect together with the ability to selectively acetylate histone versus non-histone substrates
appoint 1b as a lead for the development of anticancer drugs.
first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT
activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic
effect together with the ability to selectively acetylate histone versus non-histone substrates
appoint 1b as a lead for the development of anticancer drugs.
Pentadecylidenemalonate 1b, a simplified analogue of anacardic acid, was identified as the first mixed activator/inhibitor of histone acetyltransferases (HATs). It potentiates PCAF HAT activity while inhibiting those of p300/CBP and recombinant CBP. The remarkable apoptotic effect together with the ability to selectively acetylate histone versus non-histone substrates appoint 1b as a lead for the development of anticancer drugs.
Elsevier