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Platinum(IV) complex LA-12 exerts higher ability than cisplatin to enhance TRAIL-induced cancer cell apoptosis via stimulation of mitochondrial pathway.
Abstract In search for novel strategies in colon cancer treatment, we investigated the unique ability of platinum(IV) complex LA-12 to efficiently enhance the killing effects of tumor necrosis factor-related apoptosis inducing ligand (TRAIL), and compared it with the sensitizing action of cisplatin. We provide the first evidence that LA-12 primes human colon cancer cells for TRAIL-induced cytotoxicity by p53-independent activation of the mitochondrial apoptotic pathway. The cooperative action of LA-12 and TRAIL was associated with stimulation of Bax/Bak activation, drop of mitochondrial membrane potential, caspase...
Source: Biochemical Pharmacology - October 3, 2014 Category: Drugs & Pharmacology Authors: Jelínková I, Safaříková B, Blanářová OV, Skender B, Hofmanová J, Sova P, Moyer MP, Kozubík A, Kolář Z, Ehrmann J, Vaculová AH Tags: Biochem Pharmacol Source Type: research

In vitro evaluation of inhibitory effect of nuclear factor-kappaB activity by small interfering RNA on pro-tumor characteristics of M2-like macrophages.
Abstract Tumor-associated macrophages (TAMs) have an alternatively activated macrophage phenotype (M2) and promote cancer cell proliferation, angiogenesis and metastasis. Nuclear factor-kappaB (NF-κB) is one of the master regulators of macrophage polarization. Here, we investigated the effect of inhibition of NF-κB activity by small interfering RNA (siRNA) on the pro-tumor response of macrophages located in the tumor microenvironment in vitro. We used mouse peritoneal macrophages cultured in conditioned medium from colon-26 cancer cells as an in vitro TAM model (M2-like macrophages). Transfection of NF-κB (p50)...
Source: Biological and Pharmaceutical Bulletin - August 30, 2014 Category: Drugs & Pharmacology Authors: Kono Y, Kawakami S, Higuchi Y, Yamashita F, Hashida M Tags: Biol Pharm Bull Source Type: research

A new bisphosphonate derivative, CP, induces gastric cancer cell apoptosis via activation of the ERK1/2 signaling pathway.
Conclusion:CP is a broad-spectrum inhibitor of human carcinoma cells in vitro, and it also exerts significant inhibition on gastric cancer cell growth in vivo. CP induces human gastric cancer apoptosis via activation of the ERK1/2 signaling pathway. PMID: 24241351 [PubMed - as supplied by publisher]
Source: Acta Pharmacologica Sinica - November 18, 2013 Category: Drugs & Pharmacology Authors: Wang HJ, Liu Y, Fan LQ, Han CL, Jiang Y, Cheng SJ, Li Y Tags: Acta Pharmacol Sin Source Type: research

Role of Hypoxia Inducible Factor-1α in the Regulation of the Cancer-Specific Variant of Organic Anion Transporting Polypeptide 1B3 (OATP1B3), in Colon and Pancreatic Cancer.
Abstract Organic anion transporting polypeptide 1B3 (OATP1B3) was initially considered to be a liver-specific transporter, mediating the uptake of a variety of endogenous and xenobiotic substances. Over the past decade, several investigations reported that OATP1B3 is also expressed across multiple types of cancers. Only recently, our laboratory and others demonstrated the identity of cancer-specific OATP1B3 variants (csOATP1B3) arising from the use of an alternative transcription initiation site, different from the wildtype (WT) OATP1B3 expressed in the normal liver. However, the mechanisms regulating the expressi...
Source: Biochemical Pharmacology - August 4, 2013 Category: Drugs & Pharmacology Authors: Han S, Kim K, Thakkar N, Kim D, Lee W Tags: Biochem Pharmacol Source Type: research

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