In aggregate, all positive and innovative results obtained with the C22G1 pseudo-dendrimers as potential protamine replacers in heparin-induced anti-coagulation inhibition strongly encouraged us to embark on further studies focused on further design/optimization of self-assembling amphiphilic dendron structures and related structure-activity relationships aimed at gaining a more fundamental understanding of heparin binding phenomena with the ultimate goal of contributing in paving the way of these nanotechnologically-driven compounds to pre-clinical investigations.