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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/28430745/bortezomib-pharmacokinetics-in-tumor-response-and-peripheral-neuropathy-in-multiple-myeloma-patients-receiving-bortezomib-containing-therapy
#1
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...
April 20, 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
#2
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...
April 20, 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
#3
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...
April 20, 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
#4
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...
April 18, 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
#5
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...
April 13, 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
#6
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...
April 4, 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
#7
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...
April 4, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28379898/protein-kinase-b-emerging-mechanisms-of-isoform-specific-regulation-of-cellular-signaling-in-cancer
#8
Bhumika Wadhwa, Ubaid Makhdoomi, Ram Vishwakarma, Fayaz Malik
The serine/threonine protein kinase B (PKB), also known as Akt, is one of the multifaceted kinases in the human kinome, existing in three isoforms. PKB plays a vital role in phosphoinositide 3-kinase (PI3K)-mediated oncogenesis in various malignancies and is one of the attractive targets for cancer drug discovery. Recent studies have shown that the functional significance of an individual isoform of PKB is not redundant in cancer. It has been found that PKB isoforms play distinct roles in the regulation of cellular invasion and migration during tumorigenesis...
April 4, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28368904/preparation-and-anticancer-activity-evaluation-of-an-amorphous-drug-nanocomposite-by-simple-heat-treatment
#9
Honglei Zhan, Jun F Liang
The solubility of drug molecules is closely related to its bioactivity as it affects the dissolution rate and bioavailability, especially in the case of BCS IV drugs like camptothecin (CPT), a potential broad-spectrum anticancer agent. In this study, we construct a novel boric acid (BA)-coated CPT nanocomposite by means of a simple heat-treatment approach, which combines nanoscale size range and amorphous solid state together to improve the overall dissolution rate of CPT. This new CPT formulation showed a rod-like structure with nanoscale size and amorphous solid nature...
March 31, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28368903/the-incidence-of-radiation-necrosis-following-stereotactic-radiotherapy-for-melanoma-brain-metastases-the-potential-impact-of-immunotherapy
#10
Orit Kaidar-Person, Timothy M Zagar, Allison Deal, Stergios J Moschos, Matthew G Ewend, Deanna Sasaki-Adams, Carrie B Lee, Frances A Collichio, David Fried, Lawrence B Marks, Bhishamjit S Chera
Stereotactic radiotherapy (SRT) is the standard treatment for patients with limited number of brain metastases. In the past few years, newer immunotherapies (immune checkpoint inhibitors) have been proven to prolong survival in patients with metastatic melanoma. The safety of the combination of SRT and immunotherapy for brain metastases is unknown. We retrospectively identified patients with melanoma brain metastases treated with SRT between 2007 and 2015. Patients who did not have at least 3 months of follow-up with imaging after SRT were excluded from the analysis...
March 31, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28252532/weekly-paclitaxel-after-first-line-failure-in-patients-with-advanced-non-small-cell-lung-cancer-everyday-clinical-practice-in-a-single-centre
#11
Mariachiara Dipasquale, Viviana Murgia, Antonello Veccia, Sonia Brugnara, Alessia Caldara, Antonella Ferro, Michela Frisinghelli, Francesca Maines, Chiara Trentin, Francesco Valduga, Orazio Caffo
To assess the activity of weekly paclitaxel (wPCT) in pretreated patients with advanced non-small-cell lung cancer (aNSCLC). In 2005, we included wPCT 80 mg/m for 6 consecutive weeks, followed by a 2-week interval in our department's everyday clinical practice guidelines for the second-line (or subsequent) treatment of patients with nonsquamous histologies who have previously received pemetrexed-based treatments and patients with squamous histology. In the absence of clinical evidence of disease progression, patients repeat the pretreatment staging procedures after 16 weeks (two cycles) and, in the absence of disease progression or severe toxicity, continue treatment for a maximum of four courses...
March 1, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28379897/targeted-radionuclide-therapy-for-lung-cancer-with-iodine-131-labeled-peptide-in-a-nude-mouse-model
#12
Zhenzhu Chen, Hongyi Gao, Man Li, Shun Fang, Guiping Li, Linlang Guo
Integrin α3β1 has been shown to be a novel candidate target for the imaging and specific therapy of non-small-cell lung cancer. We have previously reported on a peptide containing a novel motif of NGXG that specifically binds to the integrin α3 receptor on lung cancer cells using a one-bead one-peptide combinatorial library. In this study, we developed the peptide cNGEGQQc-based therapeutic agent labeling with radionuclide iodine-131 (I) and evaluated its characteristics including stability, biodistribution, antitumor activity, and safety...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28296649/a-nomogram-to-predict-5-fluorouracil-toxicity-when-pharmacogenomics-meets-the-patient
#13
Andrea Botticelli, Concetta E Onesti, Lidia Strigari, Mario Occhipinti, Francesca R Di Pietro, Bruna Cerbelli, Antonella Petremolo, Elisabetta Anselmi, Serena Macrini, Michela Roberto, Rosa Falcone, Luana Lionetto, Marina Borro, Annalisa Milano, Giovanna Gentile, Maurizio Simmaco, Paolo Marchetti, Federica Mazzuca
Fluoropyrimidines combined with other agents are commonly used for gastrointestinal cancer treatment. Considering that severe toxicities occur in 30% of patients, we aimed to structure a nomogram to predict toxicity, based on metabolic parameter and patients' characteristics. We retrospectively enrolled patients affected by gastrointestinal tract cancers. Pretreatment 5-fluorouracil (5-FU) degradation rate and DPYD, TSER, MTHFR A1298T, and C677T gene polymorphisms were characterized. Data on toxicities were collected according to CTCAE v3...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28272098/adriamycin-in-combination-with-dexamethasone-and-octreotide-lacks-activity-on-the-treatment-of-a-4t1-metastatic-breast-cancer-model
#14
Panayiotis Dalezis, Dimitrios T Trafalis, George D Geromichalos, Nikos Pissimissis, Dimitra Panagiotopoulou, Grammati Galaktidou, Efi Papageorgiou, Athanassios Papageorgiou, Maria Lymperi, Michael Koutsilieris
The aim of this study was to evaluate whether the palliative treatment for metastatic disease with dexamethasone (DEX) plus octreotide (OCT) can improve the anticancer effects of the standard treatment with adriamycin (ADR) on a 4T1 metastatic breast cancer (MBC) model. 4T1 cells were first characterized for the expression of the somatostatin receptors 1-5 and were then inoculated onto the femur of BALB/C mice. Investigation protocols used 4T1 cell proliferation and invasion assays, analysis of radiographic images of the bone metastatic lesions, and overall survival of the diseased animals...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28263201/a-systematic-review-and-pooled-analysis-of-retrospective-series-of-eribulin-in-metastatic-breast-cancer
#15
Ioannis A Voutsadakis
Eribulin is one of the newer chemotherapeutic agents approved for use in later line treatment of patients with metastatic breast cancer. Phase III studies have shown a useful clinical response rate for eribulin as well as equivalence to another commonly used drug in metastatic breast cancer, capecitabine. Nevertheless, whether this clinical value observed in trial patients is maintained in patients seen in clinical oncology practice, outside trials remains a question. Several series published over the last few years sought to answer this question...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28252533/derived-neutrophil-to-lymphocyte-ratio-as-a-prognostic-factor-in-patients-with-advanced-colorectal-cancer-according-to-ras-and-braf-status-a-post-hoc-analysis-of-the-mrc-coin-study
#16
Georgina Wood, Tal Grenader, Stephen Nash, Richard Adams, Richard Kaplan, David Fisher, Tim Maughan, John Bridgewater
The phase III Continuous or Intermittent (COIN) trial failed to show a benefit in overall survival (OS) of cetuximab in combination with chemotherapy for patients with metastatic colorectal cancer. High derived neutrophil to lymphocyte ratio (dNLR) has been shown to be prognostic in patients with metastatic colorectal cancer. The aim of this analysis is to evaluate dNLR as a predictive biomarker of the survival according to RAS and BRAF mutations status within the COIN trial. A post-hoc exploratory analysis of the COIN trial arms A and B was carried out...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28244942/effects-of-natural-phenolic-compound-carvacrol-on-the-human-gastric-adenocarcinoma-ags-cells-in-vitro
#17
Ayse Günes-Bayir, Huriye S Kiziltan, Abdurrahim Kocyigit, Eray M Güler, Ersin Karataş, Ali Toprak
Gastric cancer (GC) is the most common cause of morbidity and mortality because of cancer. Medicinal plants containing polyphenolic compounds have gained importance in anticancer treatment. In this context, carvacrol is a main component of many plants in the family Lamiaceae that are frequently used in folk medicine and a good candidate to investigate for GC treatment. The present study aimed to explore the cytotoxic, genotoxic, apoptotic, and reactive oxygen species (ROS)-generating effects of carvacrol on gastric adenocarcinoma in vitro...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28240680/inhibition-of-wnt-signaling-reduces-differentiation-and-induces-sensitivity-to-doxorubicin-in-human-malignant-neuroblastoma-sh-sy5y-cells
#18
Junjira Suebsoonthron, Thiranut Jaroonwitchawan, Montarop Yamabhai, Parinya Noisa
Neuroblastoma is one of the most common cancers in infancy, arising from the neuroblasts during embryonic development. This cancer is difficult to treat and resistance to chemotherapy is often found; therefore, clinical trials of novel therapeutic approaches, such as targeted-cancer signaling, could be an alternative for a better treatment. WNT signaling plays significant roles in the survival, proliferation, and differentiation of human neuroblastoma. In this report, WNT signaling of a malignant human neuroblastoma cell line, SH-SY5Y cells, was inhibited by XAV939, a specific inhibitor of the Tankyrase enzyme...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28240679/in-vitro-and-in-vivo-combined-effect-of-arq-092-an-akt-inhibitor-with-arq-087-a-fgfr-inhibitor
#19
Yi Yu, Terence Hall, Sudharshan Eathiraj, Michael J Wick, Brian Schwartz, Giovanni Abbadessa
The PI3K/AKT pathway plays an important role in the initiation and progression of cancer, and the drug development efforts targeting this pathway with therapeutic interventions have been advanced by academic and industrial groups. However, the clinical outcome is moderate. Combination of inhibition of PI3K/AKT and other targeted agents became a feasible approach. In this study we assessed the combined effect of ARQ 092, a pan-AKT inhibitor, and ARQ 087, a pan-FGFR inhibitor, in vitro and in vivo. In a panel of 45 cancer cell lines, on 24% (11 out of 45) the compounds showed synergistic effect, on 62% (28 out of 45) additive, and on 13% (6 out of 45) antagonistic...
June 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28225458/prognostic-factors-and-outcome-of-patients-with-hematological-malignancies-in-phase-i-trials-the-gustave-roussy-scoring-system
#20
Lina Benajiba, Jean-Marie Michot, Capucine Baldini, Laura Faivre, Andrea Varga, Rastilav Balheda, Anas Gazzah, Ecaterina Ileana, Sophie Postel-Vinay, Christophe Massard, Stéphane de Botton, Jean-Charles Soria, Vincent Ribrag
Despite considerable progress in hematological malignancies (HM) biology during the last decades, translation into clinical benefit remains a major challenge. To improve patient selection and identify patients most likely to benefit from phase I trials, we designed and validated, in an independent cohort, a simple prognostic score. Treatment outcome, toxicity, and survival data from 82 consecutive patients enrolled in 14 phase I trials were reviewed (January 2008-February 2012). We validated these results on a prospectively collected cohort (17 phase I trials, February 2012-May 2014, 88 patients)...
June 2017: Anti-cancer Drugs
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