In the last few years macrocyclic peptides have emerged as a better class of lead candidates for inhibition of protein-protein interactions with respect to conventional small molecules. The IRBM peptide chemistry team collaborated with the teams at Merck & co. and RaPharma to develop potent macrocyclic peptide inhibitors of PCSK9 a key regulator of plasma LDL-cholesterol.
New IRBM Contribution to Pharmaceutics Journal
We are delighted that positive outcomes of our contribution to the “Magic Bullet” project developed under the Marie Skłodowska-Curie Actions research fellowship program are being recognized. One important example is this recently published paper in Pharmaceutics that we co-authored.
The study focused on the synthesis and evaluation of multiple RGD-cryptophycin conjugates for targeted delivery to treat multi-drug resistant cancer cells. These small molecule drug conjugates were comprehensively assessed for stability, anti-proliferative effects, selectivity and drug delivery. The results of these evaluations enabled the research team to conclude that there are exciting future opportunities in the design of novel cryptophycin-based therapeutic agents.