Hear from over 50 peptide drug commercialization experts on a variety of sessions including peptide engineering,
peptidomimetics, peptide conjugation, and cell-penetrating peptides for molecular imaging.
Initially, Nimble Therapeutics will leverage the speed and flexibility of its proprietary chemical synthesis platform, developed at Roche, to accelerate the discovery and optimization of macrocyclic
peptidomimetics as novel therapeutics.
Daneshtalab, "Discovery of chlorogenic acid-based
peptidomimetics as a novel class of antifungals.
A number of peptides and
peptidomimetics have shown encouraging results for binding to [[alpha].sub.v][[beta].sub.3] integrins.
Therefore, using the high affinity of RGD to [[alpha].sub.v][[beta].sub.3] and [[alpha].sub.v][[beta].sub.5] integrins, researchers [124-127] synthesized some Pt(IV) prodrugs based on RGD-containing peptides or
peptidomimetics to deliver platinum drugs to cancer cells or for tumor imaging (Figure 21(75 and 76)).
The largest group is radiolabelled peptide ligands comprising arginine-glycine-aspartic acid (RGD) sequence and
peptidomimetics targeting [alpha]v[beta]3 integrin receptors.
The prodrug approach, structural modifications, and
peptidomimetics, targeting the membrane transporters, receptors, and tissues, are the basic chemical modification approaches for protein drugs (18, 20).
Another strategy to improve the therapeutic potential of AMPs maybe the engineering of
peptidomimetics. These synthetic molecules mimic AMP structure but are constructed with an altered number of charged amino acids, reducing hydrophobicity and thus decreasing toxicity to host cells [86].
Tardella, "Short malonyl dehydro peptides as potential scaffolds for
peptidomimetics by an efficient Knoevenagel reaction," Amino Acids, vol.
Small molecules or
peptidomimetics are promising directions, but their rationalized development may need 3D structures of MTG16 with and without its binding partners.
Gurny, "Polymeric nano- and microparticles for the oral delivery of peptides and
peptidomimetics," Advanced Drug Delivery Reviews, vol.