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- W2085125891 abstract "Galectin‐1, a lectin implicated in several biological processes, selectively binds neuropilin‐1, enhances VEGFR2 signalling, and contributes to membrane anchorage of H‐RAS in cancer cells. PTX‐008 is a calyx[4]arene analogue designed as a galectin‐1 mimetic, showing antiangiogenic properties in vitro and in vivo in tumor models. In this study, we investigated the potential antiproliferative effects of PTX‐008 in a panel of colon (HT29, HCT116, COLO205, HCC2998), breast (MCF7, MDA‐MB‐435, SKBR3, ZR‐75‐1), ovarian (OVCAR3, IGROV1, SKOV3), lung (HOP62, HOP92), prostate (PC3, DU145), head and neck (SCC61, SQ20B, HEP2), hepatocellular carcinoma (SK‐HEP1) and renal (CAKI1) human cancer cell lines. Antiproliferative effects were detected in several cancer cell lines (SQ20B, HT29, and COLO205 cell lines, range 3–9µM). In contrast, HEP2 and DU145 cell lines appear to be resistant to PTX‐008 (>27µM). The antiproliferative effects of PTX‐008 were mainly associated with G2/M accumulation with marginal apoptosis induction. No correlation was found between the antiproliferative effects of PTX‐008 and the mRNA expression of several growth factors and tyrosine kinase receptors such as VEGF/VEGFR, EGF/EGFR, and PDGF/PDGFR as determined by qRT‐PCR analysis. In our panel, epithelial cancer cells ‐ expressing high mRNA levels of E‐cadherin and low levels of N‐cadherin and vimentin ‐ were more sensitive to PTX‐008 than mesenchymal cells. Interestingly, antiproliferative effects of PTX‐008 in cancer cells were more pronounced in cancer cells with low galectin‐1 mRNA and protein expression. Exogenous semaphorin‐3A exposure potently inhibits cell proliferation, mimicking the effects of PTX‐008, while concomitant exposure to PTX‐008 with exogenous semaphorin‐3A has strong antiproliferative effects in SQ20B cells. Furthermore, modulation of galectin‐1 with PTX‐008 followed by VEGFR/PDGFR inhibition with sunitinib resulted in enhanced antiproliferative effects in SQ20B. In SQ20B cells, PTX‐008 as well as exogenous semaphorin‐3A activate rapidly p‐AKT473 and p‐ERK1/2Thr202/Tyr204 but have no effect of p‐S6KSer235/236, further suggesting that some of the antiproliferative effects of PTX‐008 may be related to the modulation of neuropilin‐1. These findings suggest that PTX‐008 may have direct antiproliferative activity in cancer cells, with a novel mechanism that differs from the currently available kinase inhibitors. Citation Information: Mol Cancer Ther 2009;8(12 Suppl):B166." @default.
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- W2085125891 date "2009-12-10" @default.
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- W2085125891 title "Abstract B166: Effects of PTX‐008, a non‐peptidic topomimetic targeting galectin‐1 in human epithelial cancer cells" @default.
- W2085125891 doi "https://doi.org/10.1158/1535-7163.targ-09-b166" @default.
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