1 research outputs found
Development of Clickable Monophosphoryl Lipid A Derivatives toward Semisynthetic Conjugates with Tumor-Associated Carbohydrate Antigens
A semisynthetic strategy to obtain
monophosphoryl lipid A derivatives
equipped with clickable (azide, alkyne, double bond, or thiol precursor)
moieties, starting from the native lipid A isolated from <i>Escherichia
coli</i>, is presented. These lipid A derivatives can be conjugated
with other interesting biomolecules, such as tumor-associated carbohydrate
antigens (TACAs). In this way, the immunostimulant activity of monophosphoryl
lipid A can significantly improve the immunogenicity of TACAs, thus
opening access to potential self-adjuvant anticancer vaccine candidates.
A monophosphoryl lipid A–Thomson-Friedenreich (TF) antigen
conjugate was obtained to demonstrate the feasibility of this methodology,
which stands as a valuable, rapid, and scalable alternative to the
highly complex approaches of total synthesis recently reported to
the same aim. A preliminary evaluation of the immunological activity
of this conjugate as well as of other semisynthetic lipid A derivatives
was also reported