Pallerla S1, Gauthier T2, Sable R1, Jois SD3.
Eur J Med Chem. 2017 Jan 5;125:914-924. doi: 10.1016/j.ejmech.2016.10.015. Epub 2016 Oct 10.Doxorubicin (DOX) belongs to the anthracycline class of drugs that are used in the treatment of various cancers. It has limited cystostatic effects in therapeutic doses, but higher doses can cause cardiotoxicity. In the current approach, we conjugated a peptidomimetic (Arg-aminonaphthylpropionic acid-Phe, compound 5) known to bind to HER2 protein to DOX via a glutaric anhydride linker. Antiproliferative assays suggest that the DOX-peptidomimetic conjugate has activity in the lower micromolar range. Read More