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Author, reference, year | Drug/s | Tumor target | Molecular mechanisms of action | Results |
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Chakrabarti et al. [57] 2009 | tranilast | several mouse, rat and human breast cancer cell lines | (1) down-regulation of TGF-β pathway (2) inhibition of MAPK pathway | inhibition of tumor cell proliferation, angiogenesis, apoptosis, migration |
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Subramaniam et al. [58] 2010 | tranilast | mouse breast cancer cell line (4T1) | (1) down-regulation of TGF-β pathway (2) induction cell arrest in the G0/G1 transition, PARP cleavage, AKT1 phosphorylation (3) up-regulation of p53 (4) reduction of ERK1/2 phosphorylation | inhibition of tumor cell proliferation, angiogenesis, apoptosis, migration |
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Hiroi et al. [59] 2002 | tranilast | hamster pancreatic cancer cell line (PGHAM-1) | (1) down-regulation of TGF-β pathway with reduction of MMP-9 and VEGF levels (2) induction cell arrest in the G0/G1 transition | inhibition of tumor cell proliferation, angiogenesis |
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Mitsuno et al. [60] 2010 | (1) tranilast plus gemcitabine (2) gemcitabine | human pancreatic cancer cell line (KP4) | decrease of RRM1 expression | (1) inhibition of tumor cell proliferation, angiogenesis, apoptosis (2) synergistic cytotoxic effect of combination therapy |
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Izumi et al. [61] 2009 | tranilast | (1) prostate cancer cell lines and bone-derived stromal cells (2) SCID mice (3) advanced hormone-refractory prostaste cancer (21 pts) | down-regulation of TGF-β1 pathway | (1) induction of apoptosis (2) reduction of invasion and bone metastasis, PSA levels, improve prognosis |
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Noguchi et al. [62] 2003 | tranilast | mouse model of oral squamous cell carcinoma | not analyzed | decrease of tumor growth, angiogenesis, cervical lymph node metastases |
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Yashiro et al. [63] 2003 | tranilast | human gastric carcinoma cell line (OCUM-2D) and gastric fibroblast cell line (NF-10) | down-regulation of TGF-β pathway | decrease of tumor growth, angiogenesis, invasion |
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Platten et al. [64] 2001 | tranilast | human malignant glioma cell line | down-regulation of TGF-β1-2 pathway | decrease of tumor growth, angiogenesis, migration, invasion |
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Nie et al. [65] 1997 | tranilast | breast cancer cell lines (MCF-7) | induction cell arrest in the G0/G1 transition | decrease of tumor growth |
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Subramaniam et al. [66] 2011 | tranilast | human breast cancer cell lines (triple positive-BT-474, triple negative-MDA-MB-231) | (1) up-regulation of p53 (2) induction cell arrest in the G0/G1 transition, AKT1 and ERK2 phosphorylation, PARP-cleavage product | induction of apoptosis, tumor growth, migration |
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Zhang et al. [67] 2009 | tranilast | several ER negative human breast cancer cell lines | agonizing ARH with down-regulation of TGF-β and NF-κB pathways | (1) induction of apoptosis (2) inhibition of angiogenesis, cell growth, invasion and metastasis |
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Hall et al. [68] 2010 | tranilast | several human breast cancer cell lines | agonizing ARH with down-regulation of TGF-β and NF-κB pathways | (1) induction of apoptosis (2) inhibition of angiogenesis, cell growth, invasion and metastasis |
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Isaji et al. [69] 1997 | tranilast | human pancreatic cancer cell lines | decrease of VEGF and MMPs levels | inhibition of angiogenesis, cell growth, migration |
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