1 research outputs found
Multivalent Interactions: Synthesis and Evaluation of Melanotropin MultimersTools for Melanoma Targeting
To develop agents for early detection and selective treatment
of melanomas, high affinity and high specificity molecular tools are
required. Enhanced specificity may be obtained by simultaneously binding
to multiple cell surface targets via the use of multimeric analogues
of naturally occurring ligands. Trimers targeting overexpressed melanocortin
receptors have been found to be potential candidates for this purpose.
In the present letter, we describe the synthesis and study of multimers
based on a dendrimer-like scaffold. The binding affinity and activity
results revealed that dendrimers promote multivalent interactions
via statistical and/or cooperative effects on binding. Moreover, viability
studies showed no significant toxicity at micromolar concentrations,
which will allow these molecular complexes to be used in vivo. Finally,
imaging studies showed effective internalization for all of the molecules,
confirming their potential as delivery agents