The positive inotropic agent DPI-201106 selectively reverses ABCB1-mediated multidrug resistance in cancer cell lines
The overexpression of ABCB1 in cancer cells is a major factor contributing to the development of multidrug resistance (MDR) and treatment failure in cancer patients. Therefore, re-sensitization of MDR cancer cells to anticancer drugs remains an important aspect in chemotherapy. The progress in developing clinically applicable synthetic inhibitors of ABCB1 has been slow, mostly due to complications associated with intrinsic toxicities and unforeseen drug-drug interactions. Here, we explored the drug-repositioning approach for cancer therapy by targeting ABCB1-mediated MDR in human cancer cells. (Source: Cancer Letters)
Source: Cancer Letters - July 18, 2018 Category: Cancer & Oncology Authors: Sung-Han Hsiao, Megumi Murakami, Ni Yeh, Yan-Qing Li, Tai-Ho Hung, Yu-Shan Wu, Suresh V. Ambudkar, Chung-Pu Wu Tags: Original Articles Source Type: research

Patient Derived Xenografts as Models for Head and Neck Cancer
Translational cancer research has benefitted significantly from the generation of preclinical models that recapitulate the native tumour environment. While conventional cell models have contributed substantially to the current understanding of cancer biology and therapeutic development, a missing link between cell culture and their clinical applications is evident. Patient derived xenograft (PDX) models represent this missing link as they enable the examination of patient tumour tissue in a native environment without significantly affecting the cellular complexity, genomics, and stromal architecture of the neoplasms. (Source: Cancer Letters)
Source: Cancer Letters - July 18, 2018 Category: Cancer & Oncology Authors: Nitschinsk Km, Idris A, McMillan Na Tags: Mini-review Source Type: research

LncRNA-p23154 promotes the invasion-metastasis potential of oral squamous cell carcinoma by regulating Glut1-mediated glycolysis
In this study, we identified a novel lncRNA lnc-p23154 which is associated with OSCC patient metastasis and the promotion of OSCC cell migration and invasion in vitro and in vivo. (Source: Cancer Letters)
Source: Cancer Letters - July 17, 2018 Category: Cancer & Oncology Authors: Yun Wang, Xiaojie Zhang, Zhi Wang, Qinchao Hu, Jie Wu, Yuanyuan Li, Xianyue Ren, Tong Wu, Xiaoan Tao, Xiaobing Chen, Xiaoxu Li, Juan Xia, Bin Cheng Tags: Original Articles Source Type: research

Relevance of the natural HDAC inhibitor sulforaphane as a chemopreventive agent in urologic tumors
Due to an increased understanding of molecular biology and the genomics of cancer, new and potent agents have been approved by the Food and Drug Administration (FDA) to fight this disease. However, all of these drugs cause severe side effects and resistance inevitably develops, re-activating tumor growth and dissemination. For this reason, patients turn to natural compounds as alternative or complementary treatment options, since it has been found that natural plant products may block, inhibit, or reverse cancer development. (Source: Cancer Letters)
Source: Cancer Letters - July 17, 2018 Category: Cancer & Oncology Authors: Eva Juengel, Holger H.H. Erb, Axel Haferkamp, Jochen Rutz, Felix K.-H. Chun, Roman A. Blaheta Source Type: research

Targeting Ubiquitin-proteasome pathway by natural, in particular polyphenols, anticancer agents: lessons learned from clinical trials
The ubiquitin-proteasome pathway (UPP) is the main non-lysosomal proteolytic system responsible for degradation of most intracellular proteins, specifically damaged and regulatory proteins. The UPP is implicated in all aspects of the cellular metabolic networks including physiological or pathological conditions. Alterations in the components of the UPP can lead to stabilization of oncoproteins or augmented degradation of tumour suppressor favouring cancer appearance and progression. Polyphenols are natural compounds that can modulate proteasome activity or the expression of proteasome subunits. (Source: Cancer Letters)
Source: Cancer Letters - July 17, 2018 Category: Cancer & Oncology Authors: Seyed Fazel Nabavi, Atanas G. Atanasov, Haroon Khan, Davide Barreca, Domenico Trombetta, Lara Testai, Antoni Sureda, Silvia Tejada, Rosa Anna Vacca, Valeria Pittala, Diana Gulei, Ioana Berindan-Neagoe, Samira Shirooie, Seyed Mohammad Nabavi Source Type: research

Dysregulation of miRNA in chronic hepatitis B is associated with hepatocellular carcinoma risk after nucleos(t)ide analogue treatment
Hepatitis B virus (HBV) infection is a major cause of hepatocellular carcinoma (HCC). Nucleos(t)ide analogue (NA) therapy effectively reduces the incidence of HCC, but it does not completely prevent the disease. Here, we show that dysregulation of microRNAs (miRNAs) is involved in post-NA HCC development. We divided chronic hepatitis B (CHB) patients who received NA therapy into two groups: 1) those who did not develop HCC during the follow-up period after NA therapy (no-HCC group) and 2) those who did (HCC group). (Source: Cancer Letters)
Source: Cancer Letters - July 16, 2018 Category: Cancer & Oncology Authors: Hideki Wakasugi, Hideaki Takahashi, Takeshi Niinuma, Hiroshi Kitajima, Ritsuko Oikawa, Naoki Matsumoto, Yuko Takeba, Takehito Otsubo, Masayuki Takagi, Yasushi Ariizumi, Michihiro Suzuki, Chiaki Okuse, Shogo Iwabuchi, Masayuki Nakano, Noriyuki Akutsu, Jong Tags: Original Articles Source Type: research

2 ’-Hydroxycinnamaldehyde inhibits cancer cell proliferation and tumor growth by targeting the pyruvate kinase M2
In this study, we identified pyruvate kinase M2 (PKM2) as a direct target of HCA by use of biochemical methods including affinity chromatography, drug affinity responsive target stability, and cellular thermal shift assay. PKM2 is up-regulated in multiple cancer types and is considered as a potential target for cancer therapy. HCA binds directly to PKM2 and selectively decreases the phosphorylation of PKM2 at Tyr105, indicating a potential anti-proliferative effect on prostate cancer cells. (Source: Cancer Letters)
Source: Cancer Letters - July 15, 2018 Category: Cancer & Oncology Authors: Yae Jin Yoon, Young-Hwan Kim, Yena Jin, Seung-Wook Chi, Jeong Hee Moon, Dong Cho Han, Byoung-Mog Kwon Tags: Original Articles Source Type: research

Retraction notice to “Sun exposure related methylation in malignant and non-malignant skin lesions” [Cancer Letters 245/1-2 (2007) 112-120]
This article has been retracted: please see Elsevier Policy on Article Withdrawal (http://www.elsevier.com/locate/withdrawalpolicy). (Source: Cancer Letters)
Source: Cancer Letters - July 12, 2018 Category: Cancer & Oncology Authors: Ubaradka G. Sathyanarayana, Angela Yen Moore, Lin Li, Asha Padar, Kuntal Majmudar, Victor Stastny, Prakash Makarla, Makoto Suzuki, John D. Minna, Ziding Feng, Adi F. Gazdar Source Type: research

Editorial Board
(Source: Cancer Letters)
Source: Cancer Letters - July 12, 2018 Category: Cancer & Oncology Source Type: research

DCZ3112, a novel Hsp90 inhibitor, exerts potent antitumor activity against HER2-positive breast cancer through disruption of Hsp90-Cdc37 interaction
In this study, we discovered a new Hsp90 inhibitor, DCZ3112, with a novel mechanism of action. DCZ3112 directly bound to the N-terminal domain of Hsp90 and inhibited Hsp90-Cdc37 interaction without inhibiting ATPase activity. (Source: Cancer Letters)
Source: Cancer Letters - July 12, 2018 Category: Cancer & Oncology Authors: Xiangling Chen, Peng Liu, Quanren Wang, Yun Li, Li Fu, Haoyu Fu, Jianming Zhu, Zhaoqiang Chen, Weiliang Zhu, Chengying Xie, Liguang Lou Tags: Original Articles Source Type: research

Telomerase reverse transcriptase regulates DNMT3B expression/aberrant DNA methylation phenotype and AKT activation in hepatocellular carcinoma
Telomerase reverse transcriptase (TERT)1 acts as a master regulator of cancer hallmarks, but underlying mechanisms remain incompletely understood. We show that TERT is required for the aberrant DNA methyltransferase 3  B (DNMT3B)2 expression and cancer-specific methylation in hepatocellular carcinoma (HCC)3, through which AKT is activated. TERT depletion inhibited, while its over-expression promoted DNMT3B expression in HCC cells, respectively. Mechanistically, TERT cooperates with the transcription factor Sp1 to stimulate DNMT3B transcription. (Source: Cancer Letters)
Source: Cancer Letters - July 12, 2018 Category: Cancer & Oncology Authors: Jingya Yu, Xiaotian Yuan, Louise Sj öholm, Tiantian Liu, Feng Kong, Tomas J. Ekström, Magnus Björkholm, Dawei Xu Tags: Original Articles Source Type: research

Suppression of ribosomal protein RPS6KB1 by Nexrutine increases sensitivity of prostate tumors to radiation
Radiation therapy (XRT) is a standard treatment for prostate cancer (PCa). Although dose escalation increases local control, toxicity hampers further escalation. Broader improvement will be possible by the addition of adjuvant therapies, which can synergize with radiation and thus improve efficacy. We have identified a natural compound (Nexrutine, Nx) that inhibits the survival and growth of PCa cells in combination with radiation. Combination studies demonstrated strong interaction between Nx and radiation both in vitro in multiple PCa cell lines and in the Transgenic adenocarcinoma of mouse prostate (TRAMP) model. (Source: Cancer Letters)
Source: Cancer Letters - July 9, 2018 Category: Cancer & Oncology Authors: Suleman S. Hussain, Shih-Bo Huang, Roble G. Bedolla, Paul Rivas, Joseph W. Basler, Gregory P. Swanson, Tim Hui-Ming Huang, Ganesh Narayanasamy, Nikos Papanikolaou, Hiroshi Miyamoto, I-Tien Yeh, Robert L. Reddick, Brad H. Pollock, Rita Ghosh, Addanki P. Ku Tags: Original Articles Source Type: research

Decrease in phosphorylated ERK indicates the therapeutic efficacy of a clinical PI3K α-selective inhibitor CYH33 in breast cancer
PI3Ks are frequently hyper-activated in breast cancer and targeting PI3K α has exhibited promising but variable response in preclinical and clinical settings. CYH33 is a novel PI3Kα-selective inhibitor in phase I clinical trial. We investigated the efficacy of CYH33 against breast cancer and explored potential predictive biomarkers. CYH33 potently restrained tumor grow th in mice bearing human breast cancer cell xenografts and in R26-Pik3caH1047R;MMTV-Cre transgenic mice. CYH33 significantly inhibited proliferation of a panel of human breast cancer cells, while diversity in sensitivity has been observed. (Source: Cancer Letters)
Source: Cancer Letters - July 9, 2018 Category: Cancer & Oncology Authors: Xue-ling Liu, Yi-chao Xu, Yu-xiang Wang, Yi Chen, Bo-bo Wang, Yi Wang, Lan-ding Hu, Qing-yang Ma, Yu-chao Zhang, Yi-ming Sun, Ying-lei Gao, Chun-hao Yang, Jian Ding, Ling-hua Meng Tags: Original Articles Source Type: research

Cell surface vimentin-targeted monoclonal antibody 86C increases sensitivity to temozolomide in glioma stem cells
Glioblastoma multiforme (GBM) is the most prevalent and aggressive brain tumor. The current standard therapy, which includes radiation and chemotherapy, is frequently ineffective partially because of drug resistance and poor penetration of the blood-brain barrier. Reducing resistance and increasing sensitivity to chemotherapy may improve outcomes. Glioma stem cells (GSCs) are a source of relapse and chemoresistance in GBM; sensitization of GSCs to temozoliomide (TMZ), the primary chemotherapeutic agent used to treat GBM, is therefore integral for therapeutic efficacy. (Source: Cancer Letters)
Source: Cancer Letters - July 6, 2018 Category: Cancer & Oncology Authors: Hyangsoon Noh, Qingnan Zhao, Jun Yan, Ling-Yuan Kong, Konrad Gabrusiewicz, Sungguan Hong, Xueqing Xia, Amy B. Heimberger, Shulin Li Tags: Original Articles Source Type: research

SIS3, a specific inhibitor of Smad3 reverses ABCB1- and ABCG2-mediated multidrug resistance in cancer cell lines
One of the major challenges in cancer chemotherapy is the development of multidrug resistance phenomenon attributed to the overexpression of ATP-binding cassette (ABC) transporter ABCB1 or ABCG2 in cancer cells. Therefore, re-sensitizing MDR cancer cells to chemotherapy by directly inhibiting the activity of ABC transporters has clinical relevance. Unfortunately, previous attempts of developing clinically applicable synthetic inhibitors have failed, mostly due to problems associated with toxicity and unforeseen drug-drug interactions. (Source: Cancer Letters)
Source: Cancer Letters - July 6, 2018 Category: Cancer & Oncology Authors: Chung-Pu Wu, Megumi Murakami, Sung-Han Hsiao, Te-Chun Liu, Ni Yeh, Yan-Qing Li, Tai-Ho Hung, Yu-Shan Wu, Suresh. V. Ambudkar Tags: Original Articles Source Type: research