Background:

Pentamidine(MP-601205) is an antimicrobial agent.Target: AntiparasiticPentamidine has a potent in vitro antiprotozoal activity. Pentamidine displays cytotoxic activity against L. infantum promastigotes with IC50 of 2.5 μM. 2.5 μM Pentamidine induces early programmed cell death in 49.6% of L. infantum promastigotes. 2.5 μM Pentamidine induces a notorious decrease in promastigotes in both G1 and S phases relative to the control-untreated samples (G1:77.0 vs 15.0%; S:11.0 vs 2.4% for control- and pentamidine-treated promastigotes, resp). Pentamidine is able to bind with calf-thymus DNA (CT-DNA) and induces conformational changes in the DNA double helix. Pentamidine also binds with ubiquitin to modifiy the β-cluster of ubiquitin [1]. Pentamidine is an inhibitor of phosphatase of regenerating liver (PRLs). 1 μg/mL of Pentamidine complete inhibits the activity of recombinant PTP1B in dephosphorylating a phos-photyrosine peptide. 10 μg/mL of Pentamidine completely inhibits the activities of recombinant PRL-1, PRL-2 and PRL-3 in dephosphorylating a phosphotyrosine peptide substrate. Incubation with Pentamidine (1 μg/mL) for 48 h reduces the activity of intracellular PRL phosphatases in transfected NIH3T3 cells by more than 85%. 10 μg/mL Pentamidine completely inhibits the growth of melanoma cell line (WM9), prostate carcinoma cell line (DU145 and C4-2), ovarian carcinoma cell line (Hey), colon carcinoma cell line (WM480), and lung carcinoma cell line (A549) which all express endogenous PRLs [2].

参考文献:
[1]. Nguewa, P.A., et al., Pentamidine is an antiparasitic and apoptotic drug that selectively modifies ubiquitin. Chem Biodivers, 2005. 2(10): p. 1387-400.
[2]. Pathak, M.K., et al., Pentamidine is an inhibitor of PRL phosphatases with anticancer activity. Mol Cancer Ther, 2002. 1(14): p. 1255-64.