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Functional expression of choline transporter-like protein 1 (CTL1) in small cell lung carcinoma cells: A target molecule for lung cancer therapy
We examined the molecular and functional characterization of choline uptake in the small cell lung carcinoma cell line NCI-H69. Choline uptake was saturable and mediated by a single transport system. Interestingly, removal of Na+ from the uptake buffer strongly enhanced choline uptake. This increase in choline uptake under the Na+-free conditions was inhibited by dimethylamiloride (DMA), a Na+/H+ exchanger (NHE) inhibitor. Various organic cations and the choline analog hemicholinium-3 (HC-3) inhibited the choline uptake and cell viability. A correlation analysis of the potencies of organic cations for the inhibition of cho...
Source: Pharmacological Research - November 9, 2014 Category: Drugs & Pharmacology Source Type: research

Delivery systems for siRNA drug development in cancer therapy
Publication date: Available online 28 August 2014 Source:Asian Journal of Pharmaceutical Sciences Author(s): Cong-fei Xu , Jun Wang Since the discovery of the Nobel prize-winning mechanism of RNA interference (RNAi) ten years ago, it has become a promising drug target for the treatment of multiple diseases, including cancer. There have already been some successful applications of siRNA drugs in the treatment of age-related macular degeneration and respiratory syncytial virus infection. However, significant barriers still exist on the road to clinical applications of siRNA drugs, including poor cellular uptake, instabilit...
Source: Asian Journal of Pharmaceutical Sciences - October 12, 2014 Category: Drugs & Pharmacology Source Type: research

Inhibition of Cancer Cell Growth by GRP78 siRNA Lipoplex via Activation of Unfolded Protein Response.
Abstract Proteasome inhibitors are a novel class of molecular-targeted anti-cancer drugs that suppress the degradation of malfolded proteins, trigger endoplasmic reticulum (ER) stress, and activate apoptosis signals. Glucose-regulated protein 78 (GRP78), a major ER chaperone, is one of the most important molecules for transduction of unfolded protein response (UPR) signals. In accordance with past findings that expression of GRP78 is elevated in cancer cells and helps to resist stress-induced apoptosis, GRP78 knockdown could be effective in anticancer therapy. We tested this hypothesis and found that transfection ...
Source: Biological and Pharmaceutical Bulletin - April 6, 2014 Category: Drugs & Pharmacology Authors: Matsumura K, Sakai C, Kawakami S, Yamashita F, Hashida M Tags: Biol Pharm Bull Source Type: research

Vimentin silencing effect on invasive and migration characteristics of doxorubicin resistant MCF-7 cells.
In this study, MCF-7 cell line which is a model for human mammary carcinoma, and a doxorubicin resistant subline (MCF-7/Dox) were used. The resistant subline was previously obtained by stepwise selection in our laboratory. In the resistant cells, high levels of vimentin expression were observed. The main purpose of this study was to investigate changes in invasive and migration characteristics of MCF-7/Dox cell line, after transient silencing of vimentin gene by specific siRNA. PMID: 24612689 [PubMed - as supplied by publisher]
Source: Biomedicine and pharmacotherapy = Biomedecine and pharmacotherapie - February 13, 2014 Category: Drugs & Pharmacology Authors: Tezcan O, Gündüz U Tags: Biomed Pharmacother Source Type: research

Liposomal siRNA nanocarriers for cancer therapy.
Abstract Small interfering RNAs (siRNA) have recently emerged as a new class of therapeutics with a great potential to revolutionize the treatment of cancer and other diseases. A specifically designed siRNA binds and induces post-transcriptional silencing of target genes (mRNA). Clinical applications of siRNA-based therapeutics have been limited by their rapid degradation, poor cellular uptake, and rapid renal clearance following systemic administration. A variety of synthetic and natural nanoparticles composed of lipids, polymers, and metals have been developed for siRNA delivery, with different efficacy and safe...
Source: Advanced Drug Delivery Reviews - December 30, 2013 Category: Drugs & Pharmacology Authors: Ozpolat B, Sood AK, Lopez-Berestein G Tags: Adv Drug Deliv Rev Source Type: research

Stable RNA Nanoparticles as Potential New Generation Drugs for Cancer Therapy.
Abstract Human genome sequencing reveals that only 1.5% of the DNA sequence codes for protein. More and more evidence reveals that a substantial part of the 98.5% so-called "junk" DNAs actually code for small noncoding RNAs. Two milestones, chemical drugs and protein drugs, have appeared in the history of drug development, and it is expected that a third milestone in drug development will be RNA drug or chemical drugs that target RNA. This review focuses on the development of RNA therapeutics for potential cancer treatment by applying RNA nanotechnology. A therapeutic RNA nanoparticle is so unique that in this par...
Source: Advanced Drug Delivery Reviews - November 21, 2013 Category: Drugs & Pharmacology Authors: Shu Y, Pi F, Sharma A, Rajabi M, Haque F, Shu D, Leggas M, Evers BM, Guo P Tags: Adv Drug Deliv Rev Source Type: research

Systemic delivery of small interfering RNA by use of targeted polycation liposomes for cancer therapy.
Abstract Novel polycation liposomes decorated with cyclic(Cys-Arg-Gly-Asp-D-Phe) peptide (cyclicRGD)-polyethylene glycol (PEG) (RGD-PEG-polycation liposomes (PCL)) were previously developed for cancer therapy based on RNA interference. Here, we demonstrate the in vivo delivery of small interfering RNA (siRNA) to tumors by use of RGD-PEG-PCL in B16F10 melanoma-bearing mice. Pharmacokinetic data obtained by positron emission tomography showed that cholesterol-conjugated siRNA formulated in RGD-PEG-PCL markedly accumulated in the tumors. Delivered by RGD-PEG-PCL, a therapeutic cocktail of siRNAs composed of cholester...
Source: Biological and Pharmaceutical Bulletin - February 10, 2013 Category: Drugs & Pharmacology Authors: Kenjo E, Asai T, Yonenaga N, Ando H, Ishii T, Hatanaka K, Shimizu K, Urita Y, Dewa T, Nango M, Tsukada H, Oku N Tags: Biol Pharm Bull Source Type: research

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