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Anti-cancer Drugs

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https://www.readbyqxmd.com/read/28906258/early-tumor-shrinkage-indicates-a-favorable-response-to-bevacizumab-based-first-line-chemotherapy-for-metastatic-colorectal-cancer
#1
Mamoru Ito, Hitoshi Kusaba, Satomi Mukaide, Junji Kishimoto, Hozumi Shimokawa, Shingo Tamura, Akitaka Makiyama, Gen Hirano, Hisanobu Oda, Tsuyoshi Shirakawa, Masato Komoda, Keita Uchino, Risa Tanaka, Kenji Mitsugi, Taito Esaki, Shuji Arita, Hiroshi Ariyama, Koichi Akashi, Eishi Baba
A close correlation between early tumor shrinkage (ETS) and overall survival (OS) has been shown in antiepidermal growth factor receptor antibody-based chemotherapies for metastatic colorectal cancer (mCRC), but the clinical impact of ETS in bevacizumab-based chemotherapy has not been adequately clarified. Clinical data of mCRC patients who started initial chemotherapy without antiepidermal growth factor receptor antibody from 2005 to 2010 were retrospectively evaluated. The relative change in tumor size after 8 weeks of chemotherapy expected from the first image assessment [estimated ETS (EETS)] and the relative change in the tumor size at the nadir compared with the baseline [depth of response (DPR)] were examined...
September 12, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28901962/ability-of-polymer-bound-p-glycoprotein-inhibitor-ritonavir-to-overcome-multidrug-resistance-in-various-resistant-neuroblastoma-cell-lines
#2
Eva Koziolová, Petr Chytil, Tomáš Etrych, Olga Janoušková
Polymer prodrugs can considerably improve the treatment of tumors with multidrug resistance, often caused by overexpression of P-glycoprotein (P-gp). Here, we present the effect of the N-(2-hydroxypropyl) methacrylamide-based polymer conjugate with P-gp inhibitor ritonavir (RIT) on the increase of free doxorubicin (DOX) and polymer-bound DOX cytotoxicity in the human neuroblastoma 4 cell line and its resistant clones to different cytostatics. The increase in cytotoxicity after polymer-RIT conjugate pretreatment was higher for the lines overexpressing P-gp and less pronounced for those with decreased P-gp levels...
September 8, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28885268/n1-guanyl-1-7-diaminoheptane-enhances-the-chemosensitivity-of-acute-lymphoblastic-leukemia-cells-to-vincristine-through-inhibition-of-eif5a-2-activation
#3
Yanhui Liu, Fei Xue, Yin Zhang, Pingchong Lei, Zhen Wang, Zunmin Zhu, Kai Sun
N1-guanyl-1,7-diaminoheptane (GC7), a deoxyhypusine synthase inhibitor, has been shown to exert antiproliferation effects in many solid tumors by regulating eukaryotic translation initiation factor 5a2 (eif5a-2). However, little is known about the role of GC7 and eif5a-2 in drug resistance in acute lymphoblastic leukemia (ALL). In the present study, we investigated the effect of GC7 on drug-resistant ALL and its potential mechanism. We found that using the CCK-8 assay that combined treatment with GC7 and vincristine (VCR) significantly inhibited the cell viability of two ALL cell lines...
September 6, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28885267/bcl-2-and-bcl-xl-mediate-resistance-to-receptor-tyrosine-kinase-targeted-therapy-in-lung-and-gastric-cancer
#4
Junfei Jin, Ying Xiong, Bo Cen
Promising clinical efficacy has been observed with receptor tyrosine kinase inhibitors (TKIs) particularly in lung and gastric cancers with mutations or amplifications in the targeted receptor tyrosine kinases (RTKs). However, the efficacy and the duration of the response to these inhibitors are limited by the emergence of drug resistance. Here, we report treatment of RTK-dependent lung and gastric cancer cell lines with TKIs increased protein levels of Bcl-2 and Bcl-xL. The combination of the Bcl-2 and Bcl-xL inhibitor ABT-263 and TKIs was superior to TKIs alone in reducing cell viability and capacity of resistant colony formation...
September 6, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28863036/clinical-activity-of-eribulin-in-advanced-desmoplastic-small-round-cell-tumor
#5
Sheik Emambux, Michele Kind, Francois Le Loarer, Maud Toulmonde, Eberhard Stoeckle, Antoine Italiano
Desmoplastic small round-cell tumor is a rare but highly aggressive tumor occurring mainly in adolescents and young adults. Prolonged progression-free survival has been documented in patients who have undergone aggressive multimodality therapy - that is, multiagent intensive chemotherapy, debulking surgery, and radiation therapy. Eribulin is a microtubule-dynamics inhibitor, and it has recently been shown to be active in liposarcomas. In preclinical models, eribulin activities have also been shown to occur in Ewing's sarcoma cell lines, rhabdomyosarcomas and osteosarcomas...
August 31, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28857768/treatment-with-abiraterone-in-metastatic-castration-resistant-prostate-cancer-patients-progressing-after-docetaxel-a-retrospective-study
#6
Giuseppe Cicero, Rossella De Luca, Livio Blasi, Alessio Pepe, Carlo Pavone, Alchiede Simonato, Francesco Dieli
The aim of this study was to evaluate abiraterone's efficacy in Italian patients affected with metastatic prostate cancer progressing after treatment with docetaxel. We conducted a retrospective analysis of 60 patients. Prostate-specific antigen (PSA) reduction in serum was the primary endpoint for evaluating the efficacy of abiraterone in combination with prednisone treatment, whereas reduced pain, safety, progression-free survival, response rate, and overall survival (OS) were secondary endpoints. A significant correlation was noticed between PSA response and OS...
August 28, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28857767/extended-topoisomerase-1-inhibition-through-liposomal-irinotecan-results-in-improved-efficacy-over-topotecan-and-irinotecan-in-models-of-small-cell-lung-cancer
#7
Shannon C Leonard, Helen Lee, Daniel F Gaddy, Stephan G Klinz, Nancy Paz, Ashish V Kalra, Daryl C Drummond, Daniel C Chan, Paul A Bunn, Jonathan B Fitzgerald, Bart S Hendriks
Liposomal irinotecan (irinotecan liposome injection, nal-IRI), a liposomal formulation of irinotecan, is designed for extended circulation relative to irinotecan and for exploiting discontinuous tumor vasculature for enhanced drug delivery to tumors. Following tumor deposition, nal-IRI is taken up by phagocytic cells followed by irinotecan release and conversion to its active metabolite, SN-38. Sustained inhibition of topoisomerase 1 by extended SN-38 exposure as a result of delivery by nal-IRI is hypothesized to enable superior antitumor activity compared with traditional topoisomerase 1 inhibitors such as conventional irinotecan and topotecan...
August 28, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28817386/cxcr4-blockade-with-amd3100-enhances-taxol-chemotherapy-to-limit-ovarian-cancer-cell-growth
#8
Patrick M Reeves, Mojgan A Abbaslou, Farah R W Kools, Mark C Poznansky
The standard of care for ovarian cancer includes initial treatment with chemotherapy. Despite initial efficacy, over 70% of patients develop recurrence; thus, there is a need to identify novel approaches that can improve therapeutic outcomes. We evaluated AMD3100 (Plerixafor), an FDA-approved CXCR4 inhibitor, as a potential adjunctive therapy for low-dose Taxol (Paclitaxel) by assessing the impact on in-vitro ovarian cancer cell proliferation. Proliferation was a measure for both human TOV-112D and murine ID8 ovarian cancer cells incubated with AMD3100 and Taxol, either individually or in combination...
August 16, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28799948/anticancer-drugs-and-the-regulation-of-hedgehog-genes-gli1-and-ptch1-a-comparative-study-in-nonmelanoma-skin-cancer-cell-lines
#9
Uffe H Olesen, Sophie Bojesen, Julie Gehl, Merete Haedersdal
Nonmelanoma skin cancer is the most common cancer in humans, comprising mainly basal cell carcinoma (BCC) and squamous cell carcinoma (SCC). BCC proliferation is highly dependent on the Hedgehog signaling pathway. We aimed to investigate a panel of anticancer drugs with known activity against skin cancer for their therapeutic potential in localized, enhanced topical treatment of SCC and BCC. Cytotoxicity profiles for vismodegib, 5-fluorouracil (5-FU), methotrexate (MTX), cisplatin, bleomycin, and vorinostat were established in terms of half maximal inhibitory concentration values in a panel of immortalized keratinocytes (HaCaT), BCC (UWBCC1 and BCC77015), and SCC (A431 and SCC25) cell lines...
August 9, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28746057/solid-lipid-nanoparticles-improve-octyl-gallate-antimetastatic-activity-and-ameliorate-its-renal-and-hepatic-toxic-effects
#10
Clarissa A S Cordova, Claudriana Locatelli, Evelyn Winter, Adny H Silva, Betina G Zanetti-Ramos, Raquel Jasper, Alessandra Mascarello, Rosendo A Yunes, Ricardo J Nunes, Tânia B Creczynski-Pasa
Metastasis is the main cause of cancer-related death and requires the development of effective treatments with reduced toxicity and effective anticancer activity. Gallic acid derivatives have shown significant biological properties including antitumoral activity as shown in a previous study with octyl gallate (G8) in vitro. Thus, the aim of this work was to evaluate the antimetastatic effect of free and solid lipid nanoparticle-loaded G8 in mice in a lung metastasis model. Animals inoculated with melanoma cells presented metastasis in lungs, which was significantly inhibited by treatment with G8 and solid lipid nanoparticle-loaded G8, named G8-NVM...
July 25, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28727579/enhanced-anticancer-efficacy-of-histone-deacetyl-inhibitor-suberoylanilide-hydroxamic-acid-in-combination-with-a-phosphodiesterase-inhibitor-pentoxifylline-in-human-cancer-cell-lines-and-in-vivo-tumor-xenografts
#11
Saranya Nidhyanandan, Boreddy S Thippeswamy, Kottapalli B Chandrasekhar, Neetinkumar D Reddy, Nagaraj M Kulkarni, Kandasamy Karthikeyan, Farhin R Khan, Jayaprakash Raghul, Govindharajan Vijaykanth, Shridhar Narayanan
Vorinostat [suberoylanilide hydroxamic acid (SAHA)], a histone deacetylase inhibitor, shows limited clinical activity against solid tumors when used alone. The methyl xanthine drug, pentoxifylline (PENT), has been described to have antitumor properties. The aim of this study was to look for the enhanced anticancer activities of both agents when used in combination at doses lower than their respective efficacy dose when used alone. We investigated the antitumor potential of this novel combination in vitro and in vivo...
July 19, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28723868/screening-of-medicinal-plant-phytochemicals-as-natural-antagonists-of-p53-mdm2-interaction-to-reactivate-p53-functioning
#12
Muhammad Riaz, Usman A Ashfaq, Muhammad Qasim, Erum Yasmeen, Muhammad T Ul Qamar, Farooq Anwar
In most types of cancer, overexpression of murine double minute 2 (MDM2) often leads to inactivation of p53. The crystal structure of MDM2, with a 109-residue amino-terminal domain, reveals that MDM2 has a core hydrophobic region to which p53 binds as an amphipathic α helix. The interface depends on the steric complementarity between MDM2 and the hydrophobic region of p53. Especially, on p53's triad, amino acids Phe19, Trp23 and Leu26 bind to the MDM2 core. Results from studies suggest that the structural motif of both p53 and MDM2 can be attributed to similarities in the amphipathic α helix...
July 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28723867/prediction-of-severe-toxicity-in-adult-patients-under-treatment-with-5-fluorouracil-a-prospective-cohort-study
#13
Carolina Vázquez, María Orlova, Federico Angriman, José N Minatta, Paula Scibona, María A Verzura, Esteban G Jáuregui, Heidy Díaz de Arce, María G Pallotta, Waldo H Belloso
5-Fluorouracil (5-FU) has long been used for the treatment of gastrointestinal tumors harboring interindividual variability in both the pharmacokinetic and the pharmacogenetic profiles, which in turn may lead to life-threatening toxicities. We carried out a prospective cohort study of adult patients initiating treatment with 5-FU between 2013 and 2015. Primary exposures of interest were the methylenetetrahydrofolate reductase single nucleotide polymorphism in exons 4 and 7 and 5'-untranslated region-thymidylate synthase VNTR genotypes, in addition to baseline clinical and demographic variables...
July 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28723866/a-case-of-resistance-to-tyrosine-kinase-inhibitor-therapy-small-cell-carcinoma-transformation-concomitant-with-plasma-genotyped-t790m-positivity
#14
Yanjun Xu, Zhiyu Huang, Lei Gong, Yun Fan
Although non-small-cell lung cancer patients with epidermal growth factor receptor (EGFR) mutations are responsive to EGFR-tyrosine kinase inhibitors, drug resistances are always inevitable. The secondary somatic EGFR threonine-methionine substitution at position 790 (T790M) mutation accounts for ∼50% of acquired resistance mechanisms. Small cell lung cancer (SCLC) transformation is a relatively rare mechanism, but has recently attracted considerable attention. The coexistence of both the mechanisms in one patient is much more scarce in clinic...
July 18, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28708672/artemisinin-disrupts-androgen-responsiveness-of-human-prostate-cancer-cells-by-stimulating-the-26s-proteasome-mediated-degradation-of-the-androgen-receptor-protein
#15
Andrea M Steely, Jamin A Willoughby, Shyam N Sundar, Vasiliki I Aivaliotis, Gary L Firestone
Androgen receptor (AR) expression and activity is highly linked to the development and progression of prostate cancer and is a target of therapeutic strategies for this disease. We investigated whether the antimalarial drug artemisinin, which is a sesquiterpene lactone isolated from the sweet wormwood plant Artemisia annua, could alter AR expression and responsiveness in cultured human prostate cancer cell lines. Artemisinin treatment induced the 26S proteasome-mediated degradation of the receptor protein, without altering AR transcript levels, in androgen-responsive LNCaP prostate cancer cells or PC-3 prostate cancer cells expressing exogenous wild-type AR...
July 13, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28704237/geraniin-inhibits-migration-and-invasion-of-human-osteosarcoma-cancer-cells-through-regulation-of-pi3k-akt-and-erk1-2-signaling-pathways
#16
Yanmao Wang, Daqian Wan, Runhua Zhou, Wanrun Zhong, Shengdi Lu, Yimin Chai
Geraniin, an active compound isolated from Geranium sibiricum, was found to inhibit proliferation and induce apoptosis of tumor cells. However, the antimetastatic effects of geraniin remain elusive. Our study found the potential antitumor mechanisms of geraniin through inhibiting the migration and invasion of human osteosarcoma U2OS cells. The western blot, gelatin zymography, and reversed transcription-PCR analysis showed that geraniin suppressed matrix metalloproteinase-9 (MMP-9) expression in a concentration-dependent manner...
July 12, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28704236/liver-x-receptors-agonist-t0901317-downregulates-matrix-metalloproteinase-9-expression-in-non-small-cell-lung-cancer-by-repressing-nuclear-factor-%C3%AE%C2%BAb
#17
Qiong-Ju Chen, Ying Shi, Jun-Feng Shi, Zhen-Hua Yuan, Ji-Yong Ma, Su-Rong Fang, Wei Gu
The liver X receptors (LXRs) is an important component of the nuclear receptor (NR) superfamily. Previous studies have shown that the LXRs possessed antitumor activity in various types of tumor cells. However, the complicated mechanisms underlying the antitumor activity remain largely unexplored. In this study, we incubated A549 cells with the compound T0901317, a specific LXRs agonist, for 24 h. The MTT assay was used to assess cell viability. Transwell assays were used to evaluate cell migration and invasion...
July 12, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28692437/codelivery-of-salinomycin-and-docetaxel-using-poly-d-l-lactic-co-glycolic-acid-poly-ethylene-glycol-nanoparticles-to-target-both-gastric-cancer-cells-and-cancer-stem-cells
#18
Lan Li, Dejun Cui, Limin Ye, Yu Li, Liyi Zhu, Lanqun Yang, Banjun Bai, Zhao Nie, Jie Gao, Yu Cao
Cancer stem cells (CSCs) in gastric cancer (GC) have been established recently as key therapeutic targets for the successful treatment of GC. Emerging evidence suggests that both CSCs and cancer cells should be eradicated to achieve optimal therapeutic efficacy. In the present study, salinomycin, which has been reported to kill CSCs, was used in combination with docetaxel, a chemotherapeutic drug that is used as first-line therapy in GC, to eradicate both GC stem cells (SCs) and cancer cells. Salinomycin and docetaxel were loaded separately into poly(D,L-lactic-co-glycolic acid)-poly(ethylene glycol) nanoparticles of ∼140 nm with a narrow size distribution, high drug loading, and sustained drug release...
July 7, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28692436/andrographolide-enhances-cisplatin-mediated-anticancer-effects-in-lung-cancer-cells-through-blockade-of-autophagy
#19
Daolu Yuwen, Shanwei Mi, Yuzhu Ma, Wenjie Guo, Qiang Xu, Yan Shen, Yongqian Shu
Lung cancer is the most common cause of cancer-related death worldwide and the platinum-based drugs such as cisplatin have been used as the first line of the treatment. However, the clinical effectiveness of such chemotherapy is limited by intrinsic or acquired resistance. In this study, we found that cisplatin induced autophagy that attenuated the sensitivity of both A549 and Lewis lung cancer (LLC) cells to cisplatin. In contrast, the clinical drug andrographolide (Andro) suppressed autophagy and enhanced cisplatin-mediated apoptosis in these cells...
July 7, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28692435/prim-o-glucosylcimifugin-induces-cell-cycle-arrest-and-apoptosis-in-acute-lymphoblastic-leukemia-cells
#20
Lu Zhang, Xiaodi Liu, Xiongbin Lu, Cheng Huang
Prim-O-glucosylcimifugin is a major constituent in Radix Saposhnikovia that has been long used for the treatment of pyrexia, rheumatism, and cancer in traditional Chinese medicine. However, the molecular and cellular mechanisms remain unknown regarding the therapeutic effect of prim-O-lucosylcimifugin. Here, we investigated the effects of prim-O-glucosylcimifugin on cell cycle progression and apoptosis in human acute lymphoblastic leukemia cells. Prim-O-glucosylcimifugin treatment resulted in marked increases in cell apoptosis and cell cycle arrest at the G2/M phase...
July 7, 2017: Anti-cancer Drugs
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