Phospholipidic Colchicinoids as Promising Prodrugs Incorporated into Enzyme-Responsive Liposomes: Chemical, Biophysical, and Enzymological Aspectsстатья
Статья опубликована в высокорейтинговом журнале
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Дата последнего поиска статьи во внешних источниках: 11 декабря 2019 г.
Аннотация:Enzyme-responsive liposomes release their
cargo in response to pathologically increased levels of
enzymes at the target site. We report herein an assembly of
phospholipase A2-responsive liposomes based on colchicinoid
lipid prodrugs incorporated into lipid bilayer of the nanosized
vesicles. The liposomes were constructed to addresses two
important issues: (i) the lipid prodrugs were designed to fit
the structure of the enzyme binding site; and (ii) the concept
of lateral pressure profile was used to design lipid prodrugs
that introduce almost no distortions into the lipid bilayer packing, thus ensuring that corresponding liposomes are stable. The
colchicinoid agents exhibit antiproliferative activity in subnanomolar range of concentrations.