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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/29782351/role-of-lkb1-in-migration-and-invasion-of-cr-vi-transformed-human-bronchial-epithelial-beas-2b-cells
#1
Jian Lu, Zhongping Zhou, Miaomiao Tang, Haijun Shen, Yi Liu, Jin Wang, Yewen Jiang, Yifan Chen, Zhanao Wu
Hexavalent chromium [Cr(VI)] is a common human carcinogen associated with lung cancer and other pulmonary diseases as exposure to excessive Cr(VI) induces malignant transformation in human lung epithelial cells. The mechanism underlying its carcinogenicity is unclear in terms of how it facilitates metastases. Cr(VI) compounds are reported to briefly promote cell migration in a concentration-dependent manner and oncogene liver kinase B1 (LKB1) was reduced in Cr(VI)-transformed cells. Overexpression of LKB1 in Beas-2B-Cr [Cr(VI) malignantly transformed Beas-2B cells] suppressed cell migration and invasion and inactivated FAK, Src, MMP-2, GSK3β, β-catenin, and HEF1, which contribute to cell migration and invasion...
May 18, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29782350/effect-of-pyruvate-kinase-m2-regulating-aerobic-glycolysis-on-chemotherapy-resistance-of-estrogen-receptor-positive-breast-cancer
#2
Yuejun Qian, Lina Bi, Yingxu Yang, Dong Wang
This study aims to explore the effect and mechanism of pyruvate kinase M2 (PKM2) on chemotherapy resistance of estrogen receptor-positive breast cancer (ER BC) by regulating aerobic glycolysis. The expression of PKM2 in ER BC MCF-7 cells, T47D cells and MCF-7/ADR cells (which are subject to adriamycin/ADR induction) were determined by quantitative real-time PCR and western blot. MCF-7/ADR (M/A) cells were grouped into blank group (M/A), negative group (M/A+NC), low expression of PKM2 group (M/A+si-PKM2 group), overexpression of PKM2 group (M/A+PKM2 group) and glycolysis inhibition group (M/A+PKM2+2-DG group)...
May 18, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29782349/lncrna-malat-1-competitively-regulates-mir-124-to-promote-emt-and-development-of-non-small-cell-lung-cancer
#3
Jiasheng Wu, Yueyue Weng, Fei He, Dong Liang, Lin Cai
This study was carried out to explore the mechanism of LncRNA MALAT-1 as a competing endogenous RNA to regulate miR-124 in epithelial-mesenchymal transition and development of non-small-cell lung cancer (NSCLC). NSCLC and adjacent tissues were collected for RT-qPCR. The correlation of MALAT-1 and miR-124 was analyzed by Pearson. MALAT-1 expression was measured in NSCLC A549, NCI-H460, NCI-H529, SK-MES-1 cells, and 16HBE cells. A549 cells were selected for cell transfection experiments after the creation of six groups...
May 18, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29782348/renal-ewing-sarcoma-treated-with-apatinib
#4
Yang Zhao, Ye Chen, Ke Cheng, Zhi-Ping Li, Hao Zeng, Ji-Yan Liu
Renal Ewing sarcoma (RES) is an extremely rare disease. The standard treatment for this disease is lacking, and clinical experience needs to be accumulated. Here, we report a case of RES that rapidly developed to metastatic disease and was refractory to radiotherapy and chemotherapy; however, the case obtained a partial response based on Choi criteria by orally taking antiangiogenic drug apatinib. Our case suggests that apatinib may be a therapeutic option for RES.
May 18, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29782352/an-update-on-the-management-of-pancreatic-neuroendocrine-tumors
#5
Limin Gao, Nikola S Natov, Kevin P Daly, Faisal Masud, Sadia Chaudhry, Mark J Sterling, Muhammad W Saif
Pancreatic neuroendocrine tumors (PNETs) are a rare and heterogeneous group of neoplasia and differ in their clinical presentation, behavior, and prognosis based on both histological features and cancer stage at the time of diagnosis. Although small-sized tumors can be surgically resected, locally advanced and metastatic tumors confer a poor prognosis. In addition, only limited treatment options are available to the latter group of patients with PNETs, such as hormonal analogs, cytotoxic agents, and targeted therapy...
May 8, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29738338/growth-arrest-and-apoptosis-induced-by-kinesin-eg5-inhibitor-k858-and-by-its-1-3-4-thiadiazoline-analogue-in-tumor-cells
#6
Sabrina Giantulli, Francesca De Iuliis, Ludovica Taglieri, Simone Carradori, Giusi Menichelli, Stefania Morrone, Susanna Scarpa, Ida Silvestri
Tumors are complex and heterogeneous but, despite this, they share the ability to proliferate continuously, irrespective of the presence of growth signals, leading to a higher fraction of actively growing and dividing cells compared with normal tissues. For this reason, the cytotoxic antimitotic treatments remain an important clinical tool for tumors. Among these drugs, antitubulin compounds constitute one of the most effective anticancer chemotherapies; however, they cause dose-limiting side effects. Therefore, it is still necessary to develop compounds with new targets and new mechanisms of action to reduce side effects or chemoresistance...
May 5, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29738337/biochemistry-of-n-mustard-tumour-control-compounds-reconsidered
#7
Daniel S Robertson
The biochemicals and reactions involved in the present mechanism of degradation of tumour cells during chemotherapy are reconsidered and limitations noted. Alternative mechanisms and treatment methods are detailed.
May 5, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29738336/in-vitro-antitumor-activity-of-new-quaternary-phosphonium-salts-derivatives-of-3-hydroxypyridine
#8
Alfiya G Iksanova, Raylya R Gabbasova, Tatyana V Kupriyanova, Almaz A Akhunzyanov, Michail V Pugachev, Ruzalia M Vafiva, Nikita V Shtyrlin, Konstantin V Balakin, Yurii G Shtyrlin
This work presents the results of in-vitro biological activity studies of three novel anticancer agents, phosphonium salts based on the 3-hydroxypyridine scaffold, including one derivative of 4-deoxypyridoxine. Proliferation and viability of cells treated with these compounds was assessed by the colony formation and 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays. Effects of the compounds on apoptosis and cell cycle were studied by flow cytometry using annexin V-FITC/propidium iodide and propidium iodide staining, respectively...
May 5, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29734209/continuous-low-dose-infusion-of-patupilone-increases-the-therapeutic-index-in-mouse-and-rat-tumour-models
#9
Mike Becquet, Laurent Laborde, Celine Texier, Dario Sterker, Hans-Peter Gschwind, Ulrike Pfaar, Markus Wartmann, Terry M O'Reilly, Paul M McSheehy
Patupilone is a microtubule-targeted cytotoxic agent with clinical efficacy, but causes diarrhoea in more than 80% of patients. The efficacy and tolerability of patupilone delivered continuously by subcutaneous (s.c.) mini-pumps [(mini-pump dose (MPD)] or by intravenous bolus administration [intravenous bolus dose (IVBD)] were compared preclinically to determine whether the therapeutic index could be improved. The antiproliferative potency in vitro of patupilone was determined by measuring total cell protein...
May 4, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29697413/inhibition-of-fibroblast-growth-factor-receptor-signaling-sensitizes-imatinib-resistant-gastrointestinal-stromal-tumors-to-low-doses-of-topoisomerase-ii-inhibitors
#10
Sergei Boichuk, Pavel Dunaev, Aigul Galembikova, Ilshat Mustafin, Elena Valeeva
The acquired resistance of gastrointestinal stromal tumors (GISTs) to the targeted-based therapy remains the driving force to identify the novel approaches that are capable of increasing the sensitivity of GISTs to the current therapeutic regimens. Our present data show that BGJ398, a selective fibroblast growth factor receptor (FGFR) inhibitor, sensitizes imatinib (IM)-resistant GIST cells with receptor tyrosine kinase (RTK) switch (loss of c-KIT/gain of pFGFR2a) to the low doses of topoisomerase II inhibitors - doxorubicin (Dox) and etoposide (Eto)...
April 24, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29697412/antineoplastic-activity-of-linear-leucine-homodipeptides-and-their-potential-mechanisms-of-action
#11
Yun Lei, Xiao-Xia Yang, Wei Guo, Fu-Yong Zhang, Xiao-Jian Liao, Hui-Fu Yang, Shi-Hai Xu, Sheng Xiong
Galaxamide is a rare cyclic homopentapeptide composed of three leucines and two N-methyl leucines isolated from marine algae Galaxaura filamentosa. The strong antitumor activity of this compound makes it a promising candidate for tumor therapy. The synthesis of galaxamide, however, is a complex process, and it has poor water solubility. On the basis of its special chemical composition, we designed a series of linear leucine homopeptides. Among seven dipeptide derivatives, five compounds with terminal protection groups and methyl substitution of the hydrogen in the amido group showed remarkable inhibitory effects against various cancer cells...
April 24, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29683800/generation-and-characterization-of-a-paclitaxel-resistant-human-gastric-carcinoma-cell-line
#12
Ling Fu, Fen Yin, Xiao-Rui Li, Bing-Kai Han, Chuang Zhang, Jun-Wei Wang, Yu-Qing Wang, Yue-Feng Bi, Hong-Min Liu
The main aim of this study was to establish a novel paclitaxel (PTX)-resistant human gastric carcinoma cell line and to investigate its biological significance. A cell line, MGC803/PTX, was established by gradually increasing PTX density on the basis of MGC803 over a period of 10 months. In addition, a pair of resistant cell lines (SW620 and SW620/PTX) were added to further explain the resistant mechanism of PTX. The drug resistance index and stability of MGC803/PTX cells were detected using the Cell Counting Kit-8 method...
April 20, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29668485/prolonged-activity-and-toxicity-of-sirolimus-in-a-patient-with-metastatic-renal-perivascular-epithelioid-cell-tumor-a-case-report-and-literature-review
#13
Alessandra Raimondi, Francesca Colombo, Giulia Pintarelli, Carlo Morosi, Salvatore L Renne, Anna M Frezza, Maristella Saponara, Angelo P Dei Tos, Arabella Mazzocchi, Salvatore Provenzano, Paolo G Casali, Silvia Stacchiotti
Perivascular epithelioid cell tumor (PEComa) is a family of mesenchymal tumors. Conventional chemotherapy has little activity in this disease, but case reports are available on the activity of mammalian target of rapamycin inhibitors (e.g. sirolimus and temsirolimus). Pharmacokinetic assays of sirolimus are available as this drug has a precise therapeutic window and blood levels might be influenced by CYP3A4 polymorphisms and drug interactions. We report on a case of a patient with metastatic, progressive PEComa who started sirolimus at a dose of 5 mg/day with evidence of grade (G) 3 mucositis, G2 thrombocytopenia, and G1 leucopenia 10 days after the treatment started, in absence of concomitant medications or prohibited food assumption...
April 17, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29659371/real-world-use-safety-and-survival-of-ipilimumab-in-metastatic-cutaneous-melanoma-in-the-netherlands
#14
Anouk Jochems, Brenda Leeneman, Margreet G Franken, Maartje G Schouwenburg, Maureen J B Aarts, Alexander C J van Akkooi, Franchette W P J van den Berkmortel, Alfonsus J M van den Eertwegh, Gerard Groenewegen, Jan Willem B de Groot, John B A G Haanen, Geke A P Hospers, Ellen Kapiteijn, Rutger H Koornstra, Wim H J Kruit, Marieke W J Louwman, Djura Piersma, Rozemarijn S van Rijn, Albert J Ten Tije, Gerard Vreugdenhil, Michel W J M Wouters, Carin A Uyl-de Groot, Koos J M van der Hoeven
Phase III trials with ipilimumab showed an improved survival in patients with metastatic melanoma. We evaluated the use and safety of ipilimumab, and the survival of all patients with metastatic cutaneous melanoma (N=807) receiving ipilimumab in real-world clinical practice in The Netherlands using data from the Dutch Melanoma Treatment Registry. Patients who were registered between July 2012 and July 2015 were included and analyzed according to their treatment status: treatment-naive (N=344) versus previously-treated (N=463)...
April 13, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29649016/thyroid-cancer-management-from-a-suspicious-nodule-to-targeted-therapy
#15
Francesco Perri, Antonio Giordano, Salvatore Pisconti, Franco Ionna, Maria G Chiofalo, Francesco Longo, Davide Leopardo, Giuseppina Della Vittoria Scarpati, Luciano Pezzullo
Thyroid nodules are very common, and their frequency is four to five times higher in women than in men. Most of them are benign, with only a very little percentage revealing a malignant neoplasm. About 50% of thyroid nodules are detected by self-palpation of neck, whereas the other 50% are diagnosed by neck ultrasonography and following fine-needle aspiration. Management of thyroid nodules is very difficult, because benign nodules are prevalent, whereas thyroid carcinoma is uncommon, representing only 1% of all malignancies...
April 11, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29634490/real-world-healthcare-costs-of-ipilimumab-in-patients-with-advanced-cutaneous-melanoma-in-the-netherlands
#16
Margreet G Franken, Brenda Leeneman, Anouk Jochems, Maartje G Schouwenburg, Maureen J B Aarts, Alexander C J van Akkooi, Franchette W P J van den Berkmortel, Alfonsus J M van den Eertwegh, Jan Willem B de Groot, Koos J M van der Hoeven, Geke A P Hospers, Ellen Kapiteijn, Rutger Koornstra, Wim H J Kruit, Marieke W J Louwman, Djura Piersma, Rozemarijn S van Rijn, Karijn P M Suijkerbuijk, Albert J Ten Tije, Gerard Vreugdenhil, Michel W J M Wouters, Michiel van Zeijl, John B A G Haanen, Carin A Uyl-de Groot
There is limited evidence on the costs associated with ipilimumab. We investigated healthcare costs of all Dutch patients with advanced cutaneous melanoma who were treated with ipilimumab. Data were retrieved from the nation-wide Dutch Melanoma Treatment Registry. Costs were determined by applying unit costs to individual patient resource use. A total of 807 patients who were diagnosed between July 2012 and July 2015 received ipilimumab in Dutch practice. The mean (median) episode duration was 6.27 (4.61) months (computed from the start of ipilimumab until the start of a next treatment, death, or the last date of follow-up)...
April 9, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29629905/presurgical-pazopanib-for-renal-cell-carcinoma-with-inferior-vena-caval-thrombus-a-single-institution-study
#17
Tomoaki Terakawa, Ahmed A Hussein, Yukari Bando, Khurshid A Guru, Junya Furukawa, Katsumi Shigemura, Kenichi Harada, Nobuyuki Hinata, Yuzou Nakano, Masato Fujisawa
The aim of this study was to investigate the clinical benefit of presurgical therapy with pazopanib in renal cell carcinoma (RCC) patients with a tumor thrombus extending to a high level in the vena cava. A retrospective review was performed for seven consecutive patients with RCC and tumor thrombus involving the vena cava above the hepatic vein (level 3-4, Mayo Clinic classification) treated with pazopanib without initial cytoreductive nephrectomy at our institution. The effect of pazopanib was assessed in terms of the primary site response, thrombus diameter, and height (before and after treatment) on computed tomography or MRI...
April 6, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29570101/venous-thromboembolic-events-in-patients-with-lung-cancer-treated-with-cisplatin-based-versus-carboplatin-nedaplatin-based-chemotherapy
#18
Akihisa Mitani, Taisuke Jo, Hideo Yasunaga, Yukiyo Sakamoto, Wakae Hasegawa, Hirokazu Urushiyama, Yasuhiro Yamauchi, Hiroki Matsui, Kiyohide Fushimi, Takahide Nagase
An association between chemotherapy and venous thromboembolic events (VTEs) in patients with cancer is well established, with cisplatin (CDDP) being one of the most well-studied risk factors. However, whether CDDP is more strongly associated with occurrence of VTEs than carboplatin (CBDCA) or nedaplatin (CDGP) is controversial. Our purposes were to characterize patients with lung cancer and in-hospital VTEs, identify risk factors associated with VTEs, and compare the risks associated with CDDP-based versus CBDCA/CDGP-based chemotherapy...
March 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29570100/inhibition-of-anaplastic-lymphoma-kinase-promotes-apoptosis-and-suppresses-proliferation-in-human-hepatocellular-carcinoma
#19
Zhen Yu, Ronglei Zhao
Our study was to examine the roles of crizotinib and ceritinib in hepatocellular carcinoma (HCC) cells and explore the possible mechanisms. MTT assay was employed to examine the proliferation of five HCC cell lines treated with various concentrations of crizotinib or ceritinib. HepG2 and HCCLM3 cells were incubated with 2 nmol/l ceritinib for 1 week, followed by crystal violet staining and cell counting. Protein amounts of t-ALK, p-ALK, t-AKT, p-AKT, t-ERK, p-ERK, Mcl-1, survivin, and XIAP in HepG2 cells under different culture conditions were evaluated by western blot...
March 21, 2018: Anti-cancer Drugs
https://www.readbyqxmd.com/read/29561309/acute-myositis-an-unusual-and-severe-side-effect-of-docetaxel-a-case-report-and-literature-review
#20
Philippe Rochigneux, Nicolas Schleinitz, Mikael Ebbo, Marie Aymonier, Bertrand Pourroy, Romain Boissier, Sébastien Salas, Jean-Laurent Deville
Docetaxel is an antimicrotubules cytotoxic agent prescribed widely by medical oncologists in multiple tumor types (breast, lung, prostate, stomach, head, and neck). However, the side effects of docetaxel are numerous (cytopenia, peripheral edema, myalgia, arthralgia, alopecia, and sensitive neuropathy) and recent concerns have been raised about neutropenic enterocolitis in France. Here, we report the case of a 57-year-old patient with metastatic prostatic cancer, who developed a severe myositis and fasciitis grade IV 1 week after his second docetaxel infusion...
March 20, 2018: Anti-cancer Drugs
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