Multidrug and toxin extrusion 1 and human organic cation transporter 1 polymorphisms in patients with castration-resistant prostate cancer receiving metformin (SAKK 08/09)

Multidrug and toxin extrusion 1 and human organic cation transporter 1 polymorphisms in patients with castration-resistant prostate cancer receiving metformin (SAKK 08/09) Prostate Cancer and Prostatic Diseases advance online publication, March 10 2015. doi:10.1038/pcan.2015.8 Authors: M Joerger, R H N van Schaik, M L Becker, S Hayoz, M Pollak, R Cathomas, R Winterhalder, S Gillessen &C Rothermundt
Source: Prostate Cancer and Prostatic Diseases - Category: Urology & Nephrology Authors: Source Type: research

Related Links:

Abstract Fourteen moxifloxacin-isatin hybrids 5, 6 and 13 tethered via 1,2,3-triazole were designed, and synthesized in this paper. The in vitro activities of the synthesized hybrids against a panel of cancer cell lines including HepG2 liver cancer cells, MCF-7, doxorubicin-resistant MCF-7 (MCF-7/DOX) breast cancer cells, DU-145 and multidrug-resistant DU-145 (MDR DU-145) prostate cancer cells were evaluated. The results indicated that most of them were active against the five cancer cells, whereas the parent moxifloxacin was devoid of activity. In particular, the hybrid 5b (IC50: 31.3-76.8μM) with the anticanc...
Source: Current Topics in Medicinal Chemistry - Category: Chemistry Authors: Tags: Curr Top Med Chem Source Type: research
Hong Chen Zampanolide is a promising microtubule-stabilizing agent (MSA) with a unique chemical structure. It is superior to the current clinically used MSAs due to the covalent nature of its binding to β-tubulin and high cytotoxic potency toward multidrug-resistant cancer cells. However, its further development as a viable drug candidate is hindered by its limited availability. More importantly, conversion of its chemically fragile side chain into a stabilized bioisostere is envisioned to enable zampanolide to possess more drug-like properties. As part of our ongoing project aiming to develop its mimics with ...
Source: Molecules - Category: Chemistry Authors: Tags: Article Source Type: research
ita Diterpenoid alkaloids are isolated from plants of the genera Aconitum, Delphinium, and Garrya (Ranunculaceae) and classified according to their chemical structures as C18-, C19- or C20-diterpenoid alkaloids. The extreme toxicity of certain compounds, e.g., aconitine, has prompted a thorough investigation of how structural features affect their bioactivities. Therefore, natural diterpenoid alkaloids and semi-synthetic alkaloid derivatives were evaluated for cytotoxic effects against human tumor cells [A549 (lung carcinoma), DU145 (prostate carcinoma), MDA-MB-231 (triple-negative breast cancer), MCF-7 (estrogen recep...
Source: Molecules - Category: Chemistry Authors: Tags: Review Source Type: research
Conclusions: We demonstrated specific bindings of [11C]MPC-6827 and [11C]HD-800 in breast cancer, GBM, and prostate cancer cell lines. Both tracers showed binding to taxane and colchicine sites of microtubule in MAD-MB-231 cells. This may be an advantage of these tracers for favoring high signal to noise ratio for in vivo imaging in cancer animal models. Combined with the previously established BBB permeability and in vivo binding specificity, [11C]MPC-6827 and [11C]HD-800 can be potential radiotracers for in vivo preclinical imaging of central and periphery cancers using PET. Research Support: Diane Goldberg Foundation (N...
Source: Journal of Nuclear Medicine - Category: Nuclear Medicine Authors: Tags: Oncology, Basic and Translational (Basic Science) Posters Source Type: research
We examined the effects of pentacyclic triterpene pomolic acid (PA) on docetaxel‑resistant PC3 cells. Cell viability was evaluated using the MTT assay. Apoptosis was evaluated by cell cycle analysis using flow cytometry. The activity of multiple drug resistance (MDR) proteins was determined by the accumulation of specific substrates [mitoxantrone, rhodamine 123 and 5‑carboxyfluorescein diacetate (CFDA)]. The evaluation of epithelial to mesenchymal transition (EMT) proteins was conducted by immunocytochemical assays. It was demonstrated that PC3R cells presents multidrug resistance and EMT phenotype and express active P...
Source: Oncology Reports - Category: Cancer & Oncology Tags: Oncol Rep Source Type: research
CONCLUSION: Mathematical models can integrate evolutionary dynamics into multidrug cancer clinical trials. This has the potential to improve outcomes and to develop clinical trials in which these mathematical models are also used to estimate the mechanism(s) of treatment failure and explore alternative strategies to improve outcomes in future trials. PMID: 30992299 [PubMed - as supplied by publisher]
Source: Clinical Cancer Research - Category: Cancer & Oncology Authors: Tags: Clin Cancer Res Source Type: research
We examined whether the high charge on ZmD32 would allow this defensin to retain activity in media with elevated salt concentrations. ZmD32 inhibited C. albicans, C. auris, C. glabrata, C. krusei, C. parapsilosis, and C. tropicalis growth with IC50 values ranging from 0.7 to 3.0 in ½ PDB medium containing 100 mM NaCl. In contrast, NaD1 was only active against C. parapsilosis and C. tropicalis with IC50 values of 3.4 and 1.3 μM, respectively, in medium with added NaCl. ZmD32 also retained activity against E. coli when NaC1 concentrations were raised to 100 mM while NaD1 did not (Table 1). For C. albicans and C. kr...
Source: Frontiers in Microbiology - Category: Microbiology Source Type: research
In conclusion, osmotic burst of inflated complement-damaged cells may occur, but these bursts are most likely a consequence of metabolic collapse of the cell rather than the cause of cell death. The Complement Cell Death Mediator: A Concerted Action of Toxic Moieties Membrane pores caused by complement were first visualized by electron microscopy on red blood cell membranes as large ring structures (22). Similar lesions were viewed on E. coli cell walls (23). Over the years, ample information on the fine ultrastructure of the MAC that can activate cell death has been gathered (24) and has been recently further examined (...
Source: Frontiers in Immunology - Category: Allergy & Immunology Source Type: research
Publication date: Available online 28 March 2019Source: Life SciencesAuthor(s): Monika Pichla, Jolanta Sroka, Natalia Pienkowska, Katarzyna Piwowarczyk, Zbigniew Madeja, Grzegorz Bartosz, Izabela Sadowska-BartoszAbstractAims3-Bromopyruvate (3-BP), an alkylating agent and a glycolytic inhibitor, is a promising anticancer agent, which can be efficient also against multidrug-resistant cancer cells. The aim of this study was to examine how 3-BP affects the survival and mobility of rat (MAT-LyLu and AT-2) and human (DU-145 and PC-3) metastatic prostate cancer cell lines.Main methodsCytotoxicity was estimated with Neutral Red. C...
Source: Life Sciences - Category: Biology Source Type: research
as HR Abstract One of the factors promoting tumoral progress is the abnormal activation of the epithelial-mesenchymal transition (EMT) program which has been associated with chemoresistance in tumoral cells. The transcription factor zinc finger E-box-binding homeobox 1 (ZEB1), a key EMT activator, has recently been related to docetaxel resistance, the main chemotherapeutic used in advanced prostate cancer treatment. The mechanisms involved in this protective effect are still unclear. In a previous work, we demonstrated that ZEB1 expression induced an EMT-like phenotype in prostate cancer cell lines. In this work, ...
Source: Asian Journal of Andrology - Category: Urology & Nephrology Authors: Tags: Asian J Androl Source Type: research
More News: Cancer | Cancer & Oncology | Fortamet | Metformin | Multidrug Resistance | Prostate Cancer | Urology & Nephrology