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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/28542039/role-of-the-uridine-cytidine-kinase-2-mutation-in-cellular-sensitiveness-toward-3-ethynylcytidine-treatment-of-human-cancer-cells
#1
Akira Sato, Takeshi Takano, Akiko Hiramoto, Tomoharu Naito, Akira Matsuda, Masakazu Fukushima, Yusuke Wataya, Hye-Sook Kim
A nucleosidic medicine, 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine [3'-ethynylcytidine (ECyd)], is a potent inhibitor of RNA polymerase I and shows anticancer activity to various human solid tumors in vitro and in vivo. ECyd is phosphorylated to 3'-ethyntlcytidine 5'-monophosphate by uridine/cytidine kinase 2 (UCK2) and subsequently further to diphosphate and triphosphate (3'-ethyntlcytidine 5'-diphosphate, 3'-ethyntlcytidine 5'-triphosphate). 3'-Ethyntlcytidine 5'-triphosphate is an active metabolite that can inhibit RNA polymerase I competitively, causing cancer cell death...
May 24, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28542038/hypoxia-as-a-target-for-drug-combination-therapy-of-liver-cancer
#2
Cressida Bowyer, Andrew L Lewis, Andrew W Lloyd, Gary J Phillips, Wendy M Macfarlane
Hepatocellular carcinoma (HCC) is the third most frequent cause of cancer deaths worldwide. The standard of care for intermediate HCC is transarterial chemoembolization, which combines tumour embolization with locoregional delivery of the chemotherapeutic doxorubicin. Embolization therapies induce hypoxia, leading to the escape and proliferation of hypoxia-adapted cancer cells. The transcription factor that orchestrates responses to hypoxia is hypoxia-inducible factor 1 (HIF-1). The aim of this work is to show that targeting HIF-1 with combined drug therapy presents an opportunity for improving outcomes for HCC treatment...
May 24, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28542037/long-term-use-of-pegylated-liposomal-doxorubicin-to-a-cumulative-dose-of-4600%C3%A2-mg-m2-in-recurrent-ovarian-cancer
#3
Adam Pendlebury, Robert DeBernardo, Peter G Rose
Pegylated liposomal doxorubicin (PLD) is used widely in gynecologic oncology and other oncology disciplines. Native doxorubicin use is associated with the potential for significant toxicity. Cardiac toxicity in particular limits lifetime dose. PLD has not been shown to be associated with clinical cardiac toxicity. We report on the long-term use of PLD in a patient with recurrent high-grade serous ovarian cancer to a lifetime dose of 4600 mg/m. This therapy was associated with long-term stable disease, good performance status, and minimal adverse effects...
May 24, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28542036/a-survey-of-renal-impairment-pharmacokinetic-studies-for-new-oncology-drug-approvals-in-the-usa-from-2010-to-early-2015-a-focus-on-development-strategies-and-future-directions
#4
Jim J Xiao, Jiyun S Chen, Bert L Lum, Richard A Graham
The US Food and Drug Administration (FDA) issued a guidance document in 2010 on pharmacokinetic (PK) studies in renal impairment (RI) on the basis of observations that substances such as uremic toxins might result in altered drug metabolism and excretion. No specific recommendations for oncology drugs were included. We surveyed the publicly available FDA review documents of 29 small molecule oncology drugs approved between 2010 and the first quarter of 2015. The objectives were as follows: (i) summarize the impact of RI on PK at the time of the initial new drug application; (ii) identify limitations of the guidance; and (iii) outline an integrated approach to study the impact of RI on these drugs...
May 24, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28538017/feasibility-study-of-adjuvant-chemotherapy-with-modified-weekly-nab-paclitaxel-and-carboplatin-for-completely-resected-non-small-cell-lung-cancer-fast-nab
#5
Hisashi Saji, Hideki Marushima, Tomoyuki Miyazawa, Hiroki Sakai, Hiroyuki Kimura, Noriaki Kurimoto, Haruhiko Nakamura
The aim of this study was to determine the feasibility of adjuvant administration of nab-paclitaxel (nab-P) plus carboplatin and for completely resected patients with stage IB, II, and IIIA non-small-cell lung cancer (NSCLC) (FAST-nab study, UMIN000011225). Twenty-nine eligible NSCLC patients received surgical resection for pathological stage IB, II, or IIIA, followed by postoperative adjuvant chemotherapy with modified 3-week cycles of either nab-P (100 mg/m) on days 1 and 8, followed by carboplatin area (area under the curve=6) on day 1...
May 19, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28520570/long-term-exposure-to-mst-312-leads-to-telomerase-reverse-transcriptase-overexpression-in-mcf-7-breast-cancer-cells
#6
Karollyne S Morais, Ana Flávia R Guimarãesb, Doralina A R Ramos, Fábio P Silva, Diêgo M de Oliveira
Telomerase is an enzyme responsible for telomere maintenance in almost all human cancer cells, but generally not expressed in somatic ones. Therefore, antitelomerase therapy is a potentially revolutionary therapeutic strategy, and the antitumor activity of telomerase inhibitors (TI) has been studied extensively recently, mainly for breast cancer. However, the effects expected from treatment with TI will appear only after many cell divisions, but the effects of this long-term approach are unknown. In this work, the consequences of 3120 h exposure of human breast cancer cells to TI MST-312 were investigated...
May 17, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28489616/complete-response-to-anti-pd-1-nivolumab-in-massive-skin-metastasis-from-melanoma-efficacy-and-tolerability-in-an-elderly-patient
#7
Andrea Sponghini, Federica Patrucco, Roberto Giorgione, Pamela Farinelli, Francesca Zottarelli, David Rondonotti, Paola Savoia
The advent of immune checkpoint inhibitors anti-PD-1/PD-L1 has delivered new and effective treatment options with proven clinical benefits for patients affected by metastatic melanoma. The 30-40% of treated patients experience an objective tumour regression, with a significantly prolonged survival and an improved quality of life. Here, we report a case of a 75-year-old Caucasian woman affected by a massive cutaneous metastasis from a BRAF wild-type melanoma who experienced multiple relapses after surgery and repeated electrochemotherapy treatments...
May 9, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28489615/report-of-two-cases-of-acute-cardiac-adverse-events-in-patients-with-colorectal-carcinoma-receiving-oral-capecitabine
#8
Stylianos Lampropoulos, Pavlos Roditis, Efstathios Koulouris, Aristides Zafiris, Mirto Tzimou, Konstantinos Kyratlidis, Konstantinos Pavlidis, Solace A Godwin, Christos Kosmas
Capecitabine is an oral fluoropyrimidine chemotherapeutic agent, which, after oral administration, is metabolized to its active cytotoxic compound: 5-fluorouracil (5-FU). Cardiotoxicity is a recognized side effect of 5-FU, a closely related fluorinated pyrimidine antagonist. In the present report, we report on two patients who were admitted to our department after being treated with oral capecitabine for colorectal carcinoma and developed symptoms and signs of acute myocardial infarction that resolved after appropriate treatment and monitoring...
May 9, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28471809/antitumor-activities-of-the-synthetic-retinoid-st1926-in-two-dimensional-and-three-dimensional-human-breast-cancer-models
#9
Patrick Aouad, Melody Saikali, Rana Abdel-Samad, Sabreen Fostok, Leeanna El-Houjeiri, Claudio Pisano, Rabih Talhouk, Nadine Darwiche
Despite recent advances in chemotherapy, aggressive and metastatic breast cancers remain refractory to targeted therapy and the development of novel drugs is urgently needed. Retinoids are crucial regulators of cellular proliferation, differentiation, and cell death, and have shown potent chemotherapeutic and chemopreventive properties. The major drawback of the use of all-trans retinoic acid (ATRA) in cancer therapy is disease relapse. Therefore, synthetic retinoids, specifically ST1926, have emerged as potent anticancer agents...
May 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28471808/3-bromopyruvate-enhances-trail-induced-apoptosis-in-human-nasopharyngeal-carcinoma-cells-through-chop-dependent-upregulation-of-trail-r2
#10
Zhou Can, Song Lele, Zhang Zhirui, Pan Qiong, Chen Yuzhong, Liu Lingling, Zhao Surong, Sun Yiming, Zhang Pei, Jiang Chenchen, Hao Liu
Past reports have shown that the sensitivity of cancer cells to TRAIL-induced apoptosis is related to their expression of TRAIL-death receptors on the cell surface. However, the level of TRAIL-death receptors expression on cancer cells is always low. Our previous research showed that nasopharyngeal carcinoma (NPC) cells have a poor sensitivity to low doses of TRAIL. Here, we evaluated combined treatment with the energy inhibitor 3-bromopyruvate (3BP) and TRAIL as a method to produce an increased apoptotic response in NPC cells...
May 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28471807/deguelin-induced-differentiation-of-mutated-npm1-acute-myeloid-leukemia-in-vivo-and-in-vitro
#11
Xia Zhang, Zichu Zhao, Sha Yi, Lu Wen, Jing He, Jingyu Hu, Jun Ruan, Jun Fang, Yan Chen
Nucleophosmin (NPM1), a restricted nucleolar localization protein, shuttles between the nucleus and the cytoplasm. Mutated (Mt)-NPM1 protein, which has aberrant cytoplasmic dislocation of nucleophosmin, occurs in approximately one-third of acute myeloid leukemia cases. Deguelin, a rotenoid isolated from several plant species, is a strong antitumor agent. NOD/SCID mice xenografted with human Mt-NPM1 OCI/AML3 cell lines served as in-vivo models. Wright-Giemsa staining and flow cytometry analysis were used for differentiation assays...
May 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28471806/clusterin-inhibition-mediates-sensitivity-to-chemotherapy-and-radiotherapy-in-human-cancer
#12
Marilina García-Aranda, Teresa Téllez, Miguel Muñoz, Maximino Redondo
Since its discovery in 1983, the protein clusterin (CLU) has been isolated from almost all human tissues and fluids and linked to the development of different physiopathological processes, including carcinogenesis and tumor progression. During the last few years, several studies have shown the cytoprotective role of secretory CLU in tumor cells, inhibiting their apoptosis and enhancing their resistance to conventional treatments including hormone depletion, chemotherapy, and radiotherapy. In an effort to determine the therapeutic potential that the inhibition of this protein could have on the development of new strategies for cancer treatment, numerous studies have been carried out in this field, with results, in most cases, satisfactory but sometimes contradictory...
May 3, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28452807/oxytocin-inhibits-head-and-neck-squamous-cell-carcinoma-cell-migration-by-early-growth-response-1-upregulation
#13
Jinkyung Kim, Sung-Min Kang, Heon-Jin Lee, So-Young Choi, Su-Hyung Hong
The effect of oxytocin (OXT) on cancer invasion is controversial. Few studies have examined the effect of early growth response-1 (EGR1) on the invasion of head and neck squamous cell carcinoma (HNSCC). Here, we evaluated how EGR1 affects HNSCC cell migration through the molecular mechanism of OXT in exerting anti-invasion activity. Matrigel invasion and wound-healing assays were used to measure the in-vitro cell migration. The molecular mechanism of OXT was assessed by knockdown or overexpression of EGR1 in HNSCC cells...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28430745/bortezomib-pharmacokinetics-in-tumor-response-and-peripheral-neuropathy-in-multiple-myeloma-patients-receiving-bortezomib-containing-therapy
#14
Sung-Eun Lee, Kyungmee Choi, Seunghoon Han, Jongtae Lee, Taegon Hong, Gab-Jin Park, Dong-Seok Yim, Chang-Ki Min
The usefulness of pharmacokinetics of bortezomib for multiple myeloma (MM) with respect to the maximum response to bortezomib and bortezomib-induced peripheral neuropathy (BIPN) development was studied. Maximum response to subcutaneous bortezomib therapy and BIPN occurrence for the first 12 weeks of treatment in 35 MM patients treated by bortezomib-dexamethasone (VD) and bortezomib-melphalan-prednisone (VMP) were evaluated. On day 1 of cycle 1, seven whole-blood samples were collected for 3 h after dosing completion to obtain the maximum plasma concentration and area under the time-concentration curve during 3 h postdose (AUC0-3) in each patient...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28430744/activation-of-a-c-jun-n-terminal-kinase-mediated-autophagy-pathway-attenuates-the-anticancer-activity-of-gemcitabine-in-human-bladder-cancer-cells
#15
Xiao-Long Huang, Hao Zhang, Xiao-Yu Yang, Xiao-Yong Dong, Xiang-Yu Xie, Hu-Bin Yin, Xin Gou, Yong Lin, Wei-Yang He
The role of autophagy in the anticancer activity of gemcitabine (GEM) in bladder cancer is unclear. The aim of this study is to determine whether GEM activates autophagy, the role of autophagy in the anticancer activity of GEM, and the underlying mechanism by which GEM induces autophagy. Human bladder cancer cell lines T24 and BIU87 were treated with GEM in vitro. Cell viability was measured using the Cell Counting Kit-8 assay. Apoptosis was detected by annexin V assay and western blot. Autophagy was measured by western blot and transmission electron microscopy...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28430743/microrna-148a-promotes-apoptosis-and-suppresses-growth-of-breast-cancer-cells-by-targeting-b-cell-lymphoma-2
#16
Qunying Li, Pingping Ren, Pengfei Shi, Yihan Chen, Feixiang Xiang, Li Zhang, Jing Wang, Qing Lv, Mingxing Xie
MicroRNAs (miRNAs) contribute toward tumorigenesis through the modulation of tumor-related genes. MiR-148a has been characterized as a tumor-suppressing miRNA and its downregulation has been reported in tumors of a variety of cancers. However, the functional role of miR-148a in breast cancer is not yet fully understood. Using both in-vitro and in-vivo models, we confirmed that miR-148a acts to inhibit the proliferation of breast cancer cells. Through the use of bioinformatic approaches in miRNA target prediction, we determined that B-cell lymphoma 2 (BCL-2) is a likely target of miR-148a...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28422767/pseudolaric-acid-b-induces-endometrial-cancer-ishikawa-cell-apoptosis-and-inhibits-metastasis-through-akt-gsk-3%C3%AE-and-erk1-2-signaling-pathways
#17
Dan Wang, Yanqiu Tian, Wenhua Feng, Li Zhao, Mingyi Zhao, Ju Liu, Qiuyu Wang
Pseudolaric acid B (PAB) is the most active constituent extracted from the bark of Pseudolarix kaempferi, which has been used as an antifungal remedy in traditional Chinese medicine. It is reported to have cytotoxicity to many tumor cell lines. In this study, we investigated the effects of PAB against human endometrial cancer Ishikawa cells. We found that PAB inhibited Ishikawa cell proliferation, and induced cell apoptosis and G2/M phase arrest through a mechanism involving AKT-GSK-3β and ERK1/2 signaling pathways...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28410270/the-aurora-kinase-inhibitor-amg-900-increases-apoptosis-and-induces-chemosensitivity-to-anticancer-drugs-in-the-nci-h295-adrenocortical-carcinoma-cell-line
#18
Kleiton S Borges, Augusto F Andrade, Vanessa S Silveira, David S Marco Antonio, Elton J R Vasconcelos, Sonir R R Antonini, Luiz G Tone, Carlos A Scrideli
Adrenocortical tumor (ACT) is a malignancy with a low incidence rate and the current therapy for advanced disease has a limited impact on overall patient survival. A previous study from our group suggested that elevated expression of aurora-A and aurora-B is associated with poor outcome in childhood ACT. Similar results were also reported for adult ACTs. The present in-vitro study shows that AMG 900 inhibits aurora kinases in adrenocortical carcinoma cells. AMG 900 inhibited cell proliferation in NCI-H295 cells as well as in the ACT primary cultures and caused apoptosis in the cell line NCI-H295...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28379900/baicalin-inhibits-human-osteosarcoma-cells-invasion-metastasis-and-anoikis-resistance-by-suppressing-the-transforming-growth-factor-%C3%AE-1-induced-epithelial-to-mesenchymal-transition
#19
Yanmao Wang, Huimin Wang, Runhua Zhou, Wanrun Zhong, Shengdi Lu, Zhongliang Ma, Yimin Chai
The epithelial-mesenchymal transition (EMT) plays an important role in inducing cancer metastasis. Baicalin, a flavone derivative isolated from Scutellaria spp., shows a series of pharmacological and physiological activities. However, the possible role of baicalin in the EMT is unclear. In this study, we attempted to investigate the potential use of baicalin as an inhibitor of transforming growth factor-β1 (TGF-β1)-induced EMT in U2OS cells. We found that TGF-β1 induced the EMT to promote U2OS cells migration, invasion, and anoikis resistance...
July 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28379899/isatin-inhibits-sh-sy5y-neuroblastoma-cell-invasion-and-metastasis-through-mao-hif-1%C3%AE-cxcr4-signaling
#20
Wenyan Sun, Li Zhang, Lin Hou, Chuanxia Ju, Shengmin Zhao, Yaoyue Wei
Isatin was reported to possess anticancer activities through its effect on tumor proliferation, apoptosis, and metastasis in vitro and in vivo. This study aimed to elucidate the underlying mechanism behind isatin's ability to inhibit neuroblastoma cell metastasis. Our results demonstrated that isatin could inhibit neuroblastoma cell proliferation, invasion, and migration in a dose-dependent manner. Moreover, isatin inhibited the expression level of monoamine oxidase A as well as that of its downstream protein hypoxia-inducible factor 1α...
July 2017: Anti-cancer Drugs
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