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Drug: Fortamet

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Total 55 results found since Jan 2013.

Cancers, Vol. 13, Pages 739: Metformin Reduces Histone H3K4me3 at the Promoter Regions of Positive Cell Cycle Regulatory Genes in Lung Cancer Cells
This study aimed at understanding the effect of metformin on histone H3 methylation, DNA methylation, and chromatin accessibility in lung cancer cells. Metformin significantly reduced H3K4me3 level at the promoters of positive cell cycle regulatory genes such as CCNB2, CDK1, CDK6, and E2F8. Eighty-eight genes involved in cell cycle showed reduced H3K4me3 levels in response to metformin, and 27% of them showed mRNA downregulation. Metformin suppressed the expression of H3K4 methyltransferases MLL1, MLL2, and WDR82. The siRNA-mediated knockdown of MLL2 significantly downregulated global H3K4me3 level and inhibited lung cance...
Source: Cancers - February 10, 2021 Category: Cancer & Oncology Authors: Dongho Kim Yujin Kim Bo Bin Lee Eun Yoon Cho Joungho Han Young Mog Shim Duk-Hwan Kim Tags: Article Source Type: research

AMPK inhibits Smad3-mediated autoinduction of TGF- β1 in gastric cancer cells.
AMPK inhibits Smad3-mediated autoinduction of TGF-β1 in gastric cancer cells. J Cell Mol Med. 2021 Feb 03;: Authors: Zou J, Li C, Jiang S, Luo L, Yan X, Huang D, Luo Z Abstract We have previously shown that adenine monophosphate-activated protein kinase (AMPK) regulates transforming growth factor β (TGF-β)-triggered Smad3 phosphorylation. Here we report that AMPK inhibits TGF-β1 production. First, metformin reduced mRNA levels of TGF-β1 in gastric cancer cells, in parallel to the decrease of its protein abundance. The effects were more prominent in the cells containing LKB1, an upstream kinase of...
Source: J Cell Mol Med - February 3, 2021 Category: Molecular Biology Authors: Zou J, Li C, Jiang S, Luo L, Yan X, Huang D, Luo Z Tags: J Cell Mol Med Source Type: research

Metformin-conjugated micellar system with intratumoral pH responsive de-shielding for co-delivery of doxorubicin and nucleic acid.
Abstract A novel PMet-P(cdmPEG2K) polymeric micellar carrier was developed for tumor-targeted co-delivery of DOX and nucleic acids (NA), based on polymetformin and a structure designed to lose the PEG shell in response to the acidic extracellular tumor environment. NA/DOX co-loaded micelleplexes exhibited enhanced inhibition of cell proliferation compared to DOX-loaded micelles, and displayed a higher level of cytotoxicity at an acidic pH (6.8) which mimicks the tumor microenvironment. The PMet-P(cdmPEG2K) micelles achieved significantly improved transfection with either a reporter plasmid or Cy3-siRNA, and enhanc...
Source: Biochemical Pharmacology - February 2, 2021 Category: Drugs & Pharmacology Authors: Liu Y, Sun J, Huang Y, Chen Y, Li J, Liang L, Xu J, Wan Z, Zhang B, Li Z, Li S Tags: Biochem Pharmacol Source Type: research

CXCR3 confers sorafenib resistance of HCC cells through regulating metabolic alteration and AMPK pathway.
Authors: Ren Y, Gu YK, Li Z, Xu GZ, Zhang YM, Dong MX, Wang Y, Zhou XB Abstract Currently, the acquired resistance of the hepatocellular carcinoma (HCC) first-line therapeutic agent-sorafenib (SOR) remains a major challenge for HCC management. Recent evidence suggested the association between CXCL/CXCRs chemokines and chemotherapy resistant in cancer cells. Hence, exploring the internal mechanism of CXCRs involved in SOR resistance will help to improve the efficacy of HCC. SOR-resistant HCC cells (Huh7-SOR) were established through escalating concentration of SOR. Glucose consumption, lactate production, intracellu...
Source: American Journal of Translational Research - April 11, 2020 Category: Research Tags: Am J Transl Res Source Type: research

Resveratrol attenuates diabetes-associated cell centrosome amplification via inhibiting the PKC α-p38 to c-myc/c-jun pathway.
In conclusion, our results suggest that PKCα-p38 to c-myc/c-jun is the signaling pathway of the diabetes-associated centrosome amplification, and resveratrol attenuates the centrosome amplification by inhibiting this signaling pathway. PMID: 31844893 [PubMed - as supplied by publisher]
Source: Acta Biochimica et Biophysica Sinica - December 15, 2019 Category: Biochemistry Authors: Wu Q, Chen X, He Q, Lang L, Xu P, Wang P, Lee SC Tags: Acta Biochim Biophys Sin (Shanghai) Source Type: research

Metformin ‐sensitized NSCLC cells to osimertinib via AMPK‐dependent autophagy inhibition
ConclusionMetformin inhibited autophagy and enhanced osimertinib sensitivity via inducing AMPK activation in a time ‐dependent manner.
Source: The Clinical Respiratory Journal - October 6, 2019 Category: Respiratory Medicine Authors: Hengyi Chen, Caiyu Lin, Conghua Lu, Yubo Wang, Rui Han, Li Li, Shuai Hao, Yong He Tags: ORIGINAL ARTICLE Source Type: research

Combination simvastatin and metformin synergistically inhibits endometrial cancer cell growth.
CONCLUSIONS: MET+SIM treatment synergistically inhibits endometrial cancer cell viability. This may be mediated by apoptosis and mTOR pathway inhibition. Our results provide preclinical evidence that the combination of these well-tolerated drugs may warrant further clinical investigation for endometrial cancer treatment. PMID: 31178149 [PubMed - as supplied by publisher]
Source: Gynecologic Oncology - June 5, 2019 Category: Cancer & Oncology Authors: Kim JS, Turbov J, Rosales R, Thaete LG, Rodriguez GC Tags: Gynecol Oncol Source Type: research

Myeloid Derived Suppressor Cells Interactions With Natural Killer Cells and Pro-angiogenic Activities: Roles in Tumor Progression
Conclusions MDSC are major players in the immunosuppressive scenario in cancer, thanks to their phenotype heterogeneity and critical interaction with several innate immune cells, thus representing a crucial target in oncology. Here we reviewed the interactions of MDSCs with NK cells. The contribution of key cytokines, chemokines and mediators active in this process have been discussed. We also described the contribution of MDSC on angiogenesis directly or indirectly through interactions with NK and immunosuppressive activities. A parallel of the cancer associated to the decidual counterpart of these cells is discussed, a...
Source: Frontiers in Immunology - April 17, 2019 Category: Allergy & Immunology Source Type: research

Cisplatin resistance involves a metabolic reprogramming through ROS and PGC-1 α in NSCLC which can be overcome by OXPHOS inhibition.
CONCLUSION: These results describe a new cisplatin resistance mechanism in NSCLC based on a metabolic reprogramming that is therapeutically exploitable through PGC-1α downregulation or OXPHOS inhibitors. PMID: 30880247 [PubMed - as supplied by publisher]
Source: Free Radical Biology and Medicine - March 13, 2019 Category: Biology Authors: Cruz-Bermúdez A, Laza-Briviesca R, Vicente-Blanco RJ, García-Grande A, Coronado MJ, Laine-Menéndez S, Palacios-Zambrano S, Moreno-Villa MR, Ruiz-Valdepeñas AM, Lendinez C, Romero A, Franco F, Calvo V, Alfaro C, Acosta PM, Salas C, Garcia JM, Provencio Tags: Free Radic Biol Med Source Type: research

Metformin alters H2A.Z dynamics and regulates androgen dependent prostate cancer progression.
Authors: Tyagi M, Cheema MS, Dryhurst D, Eskiw CH, Ausió J Abstract Epigenetic mechanisms involved in prostate cancer include hypermethylation of tumor suppressor genes, general hypomethylation of the genome, and alterations in histone posttranslational modifications (PTMs). In addition, over expression of the histone variant H2A.Z as well as deregulated expression of Polycomb group proteins including EZH2 have been well-documented. Recent evidence supports a role for metformin in prostate cancer (PCa) treatment. However, the mechanism of action of metformin in PCa is poorly understood. We provide data showing tha...
Source: Oncotarget - January 18, 2019 Category: Cancer & Oncology Tags: Oncotarget Source Type: research

Molecular mechanism of LKB1 in the invasion and metastasis of colorectal cancer.
Authors: Chen Y, Liu Y, Zhou Y, You H Abstract The occurrence of colorectal cancer (CRC) is associated with a variety of oncogenes and tumor‑suppressor genes. As a tumor‑suppressor gene, the liver kinase B1 gene (LKB1, also known as serine/threonine kinase 11, STK11) is closely related to tumor angiogenesis, invasion and metastasis, but its molecular mechanisms remain unclear. The aim of the present study was to investigate the effects of LKB1 on the invasion and metastasis of CRC, and to explore its molecular mechanisms. By detecting the expression of LKB1 in CRC, we can provide a reference index for diagnosin...
Source: Oncology Reports - December 1, 2018 Category: Cancer & Oncology Tags: Oncol Rep Source Type: research

Anticancer Activity of Metformin, an Antidiabetic Drug, Against Ovarian Cancer Cells Involves Inhibition of Cysteine-Rich 61 (Cyr61)/Akt/Mammalian Target of Rapamycin (mTOR) Signaling Pathway.
CONCLUSIONS Taken together, we concluded that metformin exhibits anticancer effects and Cyr61 acts as a direct target for metformin in ovarian cancer cells. PMID: 30171812 [PubMed - in process]
Source: Medical Science Monitor - September 2, 2018 Category: Research Tags: Med Sci Monit Source Type: research

Down-regulation of PKM2 enhances anticancer efficiency of THP on bladder cancer.
This study aims to investigate the effect of down-regulation of PKM2 on THP efficiency. Via inhibitor or siRNA, the effects of reduced PKM2 on the efficiency of THP were determined in 2 human and 1 murine bladder cancer cell lines, using MTT, cologenic and fluorescence approaches. Molecular mechanisms of PKM2 on THP sensitization were explored by probing p-AMPK and p-STAT3 levels via WB. Syngeneic orthotopic bladder tumour model was applied to evaluate this efficiency in vivo, analysed by Kaplan-Meier survival curves, body and bladder weights plus immunohistochemistric tumour biomarkers. PKM2 was overexpressed in bladder c...
Source: J Cell Mol Med - March 7, 2018 Category: Molecular Biology Authors: Su Q, Tao T, Tang L, Deng J, Darko KO, Zhou S, Peng M, He S, Zeng Q, Chen AF, Yang X Tags: J Cell Mol Med Source Type: research

Down ‐regulation of PKM2 enhances anticancer efficiency of THP on bladder cancer
This study aims to investigate the effect of down‐regulation of PKM2 on THP efficiency. Via inhibitor or siRNA, the effects of reduced PKM2 on the efficiency of THP were determined in 2 human and 1 murine bladder cancer cell lines, using MTT, cologenic and fluorescence approaches. Molecular mechanisms of PKM2 on THP sensitization were explored by probing p‐AMPK and p‐STAT3 levels via WB. Syngeneic orthotopic bladder tumour model was applied to evaluate this efficiency in vivo, analysed by Kaplan‐Meier survival curves, body and bladder weights plus immunohistochemistric tumour biomarkers. PKM2 was overexpressed in b...
Source: Journal of Cellular and Molecular Medicine - March 1, 2018 Category: Molecular Biology Authors: Qiongli Su, Ting Tao, Lei Tang, Jun Deng, Kwame Oteng Darko, Sichun Zhou, Mei Peng, Shanping He, Qing Zeng, Alex F. Chen, Xiaoping Yang Tags: ORIGINAL ARTICLE Source Type: research

Metformin Promotes 2-Deoxy-2- 18 FFluoro-D-Glucose Uptake in Hepatocellular Carcinoma Cells Through FoxO1-Mediated Downregulation of Glucose-6-Phosphatase
ConclusionsWe propose that treatment of HCC cells with Met may be a useful strategy for improving the efficacy of [18F]FDG as a tracer for PET/CT imaging of HCC tumors in patients.
Source: Molecular Imaging and Biology - December 18, 2017 Category: Molecular Biology Source Type: research