Beilstein J. Org. Chem.2019,15, 96–105, doi:10.3762/bjoc.15.11
tubugi-1–NPY conjugate), and native tubulysinA as reference were investigated by in vitro cell viability and proliferation screenings. The tumor cell lines HT-29, Colo320 (both colon cancer), PC-3 (prostate cancer), and in conjunction with RT-qPCR analyses of the hY1R expression, the cell lines SK-N-MC
triple-negative breast cancer MDA-MB-468 cells.
Keywords: drug targeting; neuropeptide Y; PDC; peptide–drug conjugate; targeted tumor therapy; tubugi; tubulysinA; Ugi reaction; Introduction
Until recently, the medication of tumor diseases was primarily based on more or less unspecific
well as a peptide–tubulysinA conjugate [K4(C(TubA)-βA-),F7,P34]-pNPY – representing a comparable PDC – compared to wildtype pNPY for their binding affinities at the NPY Y1 receptor subtype. While [F7,P34]-pNPY (IC50 = 1.3 nM) showed a comparable binding affinity as pNPY (IC50 = 1.8 nM), the Y1