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 |