biostudies-literatureMurray-Stewart TMaryland Cigarette Restitution FundSamuel Waxman Cancer Research FoundationNCI NIH HHSNational Institutes of HealthNational Institute of Biomedical Imaging and Bioengineeringe0175917https://www.ebi.ac.uk/biostudies/studies/S-EPMC5396973biostudies-literatureUnknown12(4)Synthesizing polycationic polymers directly from existing drugs overcomes the drug-loading limitations often associated with pharmacologically inert nanocarriers. We recently described nanocarriers formed from a first-generation polyamine analogue, bis(ethyl)norspermine (BENSpm), that could simultaneously target polyamine metabolism while delivering therapeutic nucleic acids. In the current study, we describe the synthesis and evaluation of self-immolative nanocarriers derived from the second-generation polyamine analogue PG-11047. Polyamines are absolutely essential for proliferation and their metabolism is frequently dysregulated in cancer. Through its effects on polyamine metabolism, PG-11047 effectively inhibits tumor growth in cancer cell lines of multiple origins as well as in human PloS oneBiochemical evaluation of the anticancer potential of the polyamine-based nanocarrier Nano11047.PMC5396973EB015216S30-CA006973R01-CA204345EB014570R01 CA204345Oupicky DXie YFerrari EMarton LJMurray-Stewart TYu FCasero RAfalseBiochemical evaluation of the anticancer potential of the polyamine-based nanocarrier Nano11047.Synthesizing polycationic polymers directly from existing drugs overcomes the drug-loading limitations often associated with pharmacologically inert nanocarriers. We recently described nanocarriers formed from a first-generation polyamine analogue, bis(ethyl)norspermine (BENSpm), that could simultaneously target polyamine metabolism while delivering therapeutic nucleic acids. In the current study, we describe the synthesis and evaluation of self-immolative nanocarriers derived from the second-generation polyamine analogue PG-11047. Polyamines are absolutely essential for proliferation and their metabolism is frequently dysregulated in cancer. Through its effects on polyamine metabolism, PG-11047 effectively inhibits tumor growth in cancer cell lines of multiple origins as well as in human 2017-01-01T00:00:00Z20172026-05-05T19:37:44.244Z2019-03-27T02:41:36ZS-EPMC53969732842306410.1371/journal.pone.0175917