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. 2019 Aug 28;11(9):1258. doi: 10.3390/cancers11091258

Table 1.

The SP/NK-1R system in human HB cell lines (HepT1; HepG2; HuH6).

NK-1R Express mRNA for the NK-1R
Expression of the TAC1R gene is increased
Express full and truncated isoforms of the NK-1R. The HB cells express essentially the truncated form. Expression of the full form is higher in non-tumor cells
SP A universal mitogen (at nanomolar concentration) of tumor cells, including HB cells
Non-peptide NK-1R antagonists Antiproliferative action in a concentration-dependent manner: The higher the concentration, the greater the antitumor activity
Induce cell death by apoptosis, cleavage of caspase-3and proteolysis of poly (ADP-ribose) polymerase
Aprepitant (IC50) for HepT1 (31.1 µM), HuH6 (33.18 µM), HepG2 (38.61 µM)
L-732,138 (IC50) for HepT1 (42 µM), HuH6 (41 µM), HepG2 (110 µM)
L-733,060 (IC50) for HepT1 (15 µM), HuH6 (14 µM), HepG2 (17 µM)
Co-administration of aprepitant and cytostatics exerts a synergistic antitumor effect
Pretreatment of non-tumor cells (human embryonic kidney (HEK)-293) with aprepitant, protected these cells from cytostatic toxicity