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https://www.readbyqxmd.com/read/29031230/astatine-211-labeled-anti-her2-5f7-single-domain-antibody-fragment-conjugates-radiolabeling-and-preliminary-evaluation
#1
Jaeyeon Choi, Ganesan Vaidyanathan, Eftychia Koumarianou, Choong Mo Kang, Michael R Zalutsky
INTRODUCTION: Derived from heavy chain only camelid antibodies, ~15-kDa single-domain antibody fragments (sdAbs) are an attractive platform for developing molecularly specific imaging probes and targeted radiotherapeutics. The rapid tumor accumulation and normal tissue clearance of sdAbs might be ideal for use with (211)At, a 7.2-h half-life α-emitter, if appropriate labeling chemistry can be devised to trap (211)At in cancer cells after sdAb binding. This study evaluated two reagents, [(211)At]SAGMB and iso-[(211)At]SAGMB, for this purpose...
September 19, 2017: Nuclear Medicine and Biology
https://www.readbyqxmd.com/read/29031225/cube-shaped-theranostic-paclitaxel-prodrug-nanocrystals-with-surface-functionalization-of-spc-and-mpeg-dspe-for-imaging-and-chemotherapy
#2
Fuqiang Guo, Jiajia Shang, Hai Zhao, Kangrong Lai, Yang Li, Zhongxiong Fan, Zhenqing Hou, Guanghao Su
As one of nanomedicine delivery systems (NDSs), drug nanocrystals exhibited an excellent anticancer effect. Recently, differences of internalization mechanisms and subcellular localization of both drug nanocrystals and small molecular free drug have drawn much attention. In this paper, paclitaxel (PTX) as a model anticancer drug was directly labeled with 4-chloro-7-nitro-1, 2, 3-benzoxadiazole (NBD-Cl) (a drug-fluorophore conjugate Ma et al. (2016) and Wang et al. (2016) [1,2] (PTX-NBD)). PTX-NBD was synthesized by nucleophilic substitution reaction of PTX with NBD-Cl in high yield and characterized by fluorescence, XRD, ESI-MS, and FT-IR analysis...
October 5, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29031215/comprehensive-multipathway-risk-assessment-of-chemicals-associated-with-recycled-crumb-rubber-in-synthetic-turf-fields
#3
Michael K Peterson, Julie C Lemay, Sara Pacheco Shubin, Robyn L Prueitt
BACKGROUND: Thousands of synthetic turf fields in the US are regularly used by millions of individuals (particularly children and adolescents). Although many safety assessments have concluded that there are low or negligible risks related to exposure to chemicals found in the recycled rubber used to make these fields, concerns remain about the safety of this product. Existing studies of recycled rubber's potential health risks have limitations such as small sample sizes and limited evaluation of relevant exposure pathways and scenarios...
October 11, 2017: Environmental Research
https://www.readbyqxmd.com/read/29031211/cyanidin-3-o-glucoside-inhibits-the-uvb-induced-ros-cox-2-pathway-in-hacat-cells
#4
Yong He, Yunfeng Hu, Xinwei Jiang, Tianfeng Chen, Yuetang Ma, Shi Wu, Jianxia Sun, Rui Jiao, Xiaoling Li, Liehua Deng, Weibin Bai
Ultraviolet (UV) radiation from sunlight, especially UVB (290-320nm), is one of the most important environmental factors that destroys the integrity of the skin and causes epidermal cell apoptosis, potentially even leading to skin cancer. UVB irradiation can cause skin damage by stimulating inflammatory and apoptotic pathways. Anthocyanins are flavonoids that are common in many vegetable foods, and have also demonstrated chemopreventive effects. Cyanidin-3-O-glucoside, as a typical anthocyanin, exhibits anti-inflammatory and anti-oxidant effects...
October 4, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/29031204/ginkgetin-inhibits-growth-of-breast-carcinoma-via-regulating-mapks-pathway
#5
Jun Cao, Chuang Tong, Yanyan Liu, Jianguo Wang, Xiaoyan Ni, Mao-Ming Xiong
The purpose of present study was to investigate anti-tumor activity of Ginkgetin (GK) and its mechanism of action in breast cancer. The effects of GK on growth of human breast cancer cell lines MDA-MB-231, BT-474 and MCF-7 were examined by MTT assay. Cells apoptosis in MCF-7 cells were analyzed by TUNEL staining and annexin-V and propidium iodide double staining. The effects of GK on expression of apoptotic associated proteins and mitogen-activated protein kinases (MAPKs) were determined by western blotting...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031202/targeting-of-cell-cycle-and-let-7a-stat3-pathway-by-niclosamide-inhibits-proliferation-migration-and-invasion-in-oral-squamous-cell-carcinoma-cells
#6
Xiaoxu Li, Ruiyu Ding, Zewen Han, Zeyun Ma, Yixiang Wang
The low median survival rate of oral squamous cell carcinoma (OSCC) is associated with chemotherapeutic resistance. Niclosamide is an oral anti-helminthic drug, its anti-cancer effect has been reported in recent years. However, the effect of niclosamide on OSCC remains largely unknown. In this study, we, for the first time, investigated the underlying mechanisms from cell cycle arrest and let-7a/STAT3 axis through CCK-8, cell cycle, apoptosis, wound healing, Transwell invasion, generation of stable cell line, real-time PCR, and western blot assays using two OSCC cell lines WSU-HN6 and Tca83...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031201/long-non-coding-rna-or3a4-promotes-proliferation-and-migration-in-breast-cancer
#7
Genxiang Liu, Xingchi Hu, Guangjun Zhou
More and more researches have shown the vital functions of long non-coding RNAs (LncRNAs) in modulating the biological progresses in tumorigenesis. OR3A4 is such a type of lncRNA. The long non-coding RNA (lncRNA) OR3A4 has recently been exposed to be exceptionally expressed and referred to the development of several cancers. Nevertheless, the biological function and clinical significance of OR3A4 in the carcinogenesis of breast cancer (BC) are still blurry. Therefore, we carried out the following study to make sure the underlying functions of OR3A4 in breast cancer...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031200/oleanolic-acid-methyl-ester-a-novel-cytotoxic-mitocan-induces-cell-cycle-arrest-and-ros-mediated-cell-death-in-castration-resistant-prostate-cancer-pc-3-cells
#8
Noha Abdelmageed, Samy A F Morad, Ashraf A Elghoneimy, Tatiana Syrovets, Thomas Simmet, Hesham El-Zorba, Hossney A El-Banna, Myles Cabot, Magdy I Abdel-Aziz
Oleanolic acid derivatives exhibit potent anticancer activities against numerous types of cancer. However, the antitumor activity of oleanolic acid methylester (OAME), an oleanolic acid derivative, against prostate cancer has not been studied. Hence, the present work was conducted to study the anticancer activities of OAME. Viability assay showed that treatment of cancer cells with OAME induced a significant cell death in concentration- and time-dependent manner. Of note, OAME displayed a selective cytotoxicity against cancer cells compared to normal epithelial cells...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031198/tretinoin-loaded-lipid-core-nanocapsules-overcome-the-triple-negative-breast-cancer-cell-resistance-to-tretinoin-and-show-synergistic-effect-on-cytotoxicity-induced-by-doxorubicin-and-5-fluororacil
#9
Eduarda Schultze, Julieti Buss, Karine Coradini, Karine Rech Begnini, Silvia S Guterres, Tiago Collares, Ruy Carlos Ruver Beck, Adriana R Pohlmann, Fabiana Kömmling Seixas
Nanostructured drug delivery systems have been extensively studied, mainly for applications in cancer therapy. The advantages of these materials include protection against drug degradation and improvement in both the relative solubility of poorly water soluble drugs as in targeting of therapy, due to the enhanced permeability and retention effect on tumor sites. In this work, we evaluate the antitumor activity of tretinoin-loaded lipid core nanocapsules (TT-LNC) in a tretinoin-resistant breast cancer cell-line, MDA-MB- 231, as well as the synergistic effect of combination of this treatment with 5-FU or DOXO...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031197/mitochondrial-dysfunction-is-responsible-for-fatty-acid-synthase-inhibition-induced-apoptosis-in-breast-cancer-cells-by-pdpamn
#10
Qiang Wang, Xia Du, Bingjie Zhou, Jing Li, Wenlong Lu, Qiuyun Chen, Jing Gao
Targeting cellular metabolism is becoming a hallmark to overcome drug resistance in breast cancer treatment. Activation of fatty acid synthase (FASN) has been shown to promote breast cancer cell growth. However, there is no concrete report underlying the mechanism associated with mitochondrial dysfunction in relation to fatty acid synthase inhibition-induced apoptosis in breast cancer cells. The current study is aimed at exploring the effect of the novel manganese (Mn) complex, labeled as PdpaMn, on lipid metabolism and mitochondrial function in breast cancer cells...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031195/ginsenoside-rg3-attenuates-cisplatin-resistance-in-lung-cancer-by-downregulating-pd-l1-and-resuming-immune
#11
Zhansheng Jiang, Yanfang Yang, Yinli Yang, Yu Zhang, Zhensong Yue, Zhanyu Pan, Xiubao Ren
Programmed death ligand 1 (PD-L1) as one the most important immune checkpoint was verified to involve in chemotherapy resistance in non-small cell lung cancer (NSCLC). Ginsenoside Rg3 is isolated from Chinese herb-Panax ginseng which is recognized to boost immune and has anti-cancer activity against a majority of carcinomas including NSCLC. In this study, we aim to identify whether Rg3 could attenuate the PD-L1 expression induced by resistance to cisplatin and draw out the underlying mechanisms of PD-L1 in this process...
October 11, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29031179/carbosilane-metallodendrimers-based-on-copper-ii-complexes-synthesis-epr-characterization-and-anticancer-activity
#12
Natalia Sanz Del Olmo, Marta Maroto-Díaz, Rafael Gómez, Paula Ortega, Michela Cangiotti, M Francesca Ottaviani, F Javier de la Mata
A series of new organometallic carbosilane dendrimers functionalized with Copper(II) complex on the surface were synthesized and characterized as potential anticancer agents. These metallodendrimers were synthesized through the reaction of dendritic ligands containing N,N- and N,O- donor atoms able to act as chelating agents with CuCl2 as metallic ion precursor. The structural characterization of these complexes was addressed through the use of different analytical and spectroscopical techniques. Particularly, an electron paramagnetic resonance study was performed to corroborate the coordination properties of these dendritic ligands...
September 27, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29031170/a-dose-escalation-study-of-bi-daily-once-weekly-oral-docetaxel-either-as-modradoc001-or-modradoc006-combined-with-ritonavir
#13
Vincent A de Weger, Frederik E Stuurman, Jeroen J M A Hendrikx, Johannes J Moes, Emilia Sawicki, Alwin D R Huitema, Bastiaan Nuijen, Bas Thijssen, Hilde Rosing, Marianne Keessen, Marja Mergui-Roelvink, Jos H Beijnen, Jan H M Schellens, Serena Marchetti
INTRODUCTION: Two solid dispersions of docetaxel (denoted ModraDoc001 capsule and ModraDoc006 tablet (both 10 mg)) were co-administered with 100 mg ritonavir (/r) and investigated in a bi-daily once weekly (BIDW) schedule. Safety, maximum tolerated dose (MTD), pharmacokinetics (PK) and preliminary activity were explored. METHODS: Adult patients with metastatic solid tumours were included in two dose-escalation arms. PK sampling was performed during the first week and the second or third week...
October 11, 2017: European Journal of Cancer
https://www.readbyqxmd.com/read/29031121/facilitating-decision-making-in-women-undergoing-genetic-testing-for-hereditary-breast-cancer-breconda-randomized-controlled-trial-results
#14
Kerry A Sherman, Christopher J Kilby, Laura-Kate Shaw, Caleb Winch, Judy Kirk, Kathy Tucker, Elisabeth Elder
BACKGROUND: Decision-making concerning risk-reducing mastectomy for women at hereditary risk of breast cancer entails complex personal choices. Deciding whether and how to restore breast shape after risk-reducing mastectomy is a key part of this process. We developed a web-based decision aid, BRECONDA (Breast Reconstruction Decision Aid), to assist women in decision-making regarding breast reconstruction. METHOD: This study assessed the efficacy of BRECONDA to assist women at increased risk of breast cancer in making decisions regarding risk-reducing mastectomy in terms of decisional conflict, knowledge, and satisfaction with information...
October 11, 2017: Breast: Official Journal of the European Society of Mastology
https://www.readbyqxmd.com/read/29031119/index-analysis-and-human-health-risk-model-application-for-evaluating-ambient-air-heavy-metal-contamination-in-chemical-valley-sarnia
#15
Richard Olawoyin, Linda Schweitzer, Kuangyuan Zhang, Oladapo Okareh, Kevin Slates
The impacts of air emissions as a consequence of industrial activities around communities of human habitation have been extensively reported. This study is the first to assess potential adverse human health effects in the Chemical Valley Sarnia (CVS) area, around the St. Clair River, using health risk models, ecological and pollution indices. Large quantities of particulate matters (PM) are generated from anthropogenic activities, which contain several heavy metals in trace quantities with potentially adverse effects to humans and environmental health...
October 11, 2017: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/29031099/shear-wave-elastography-for-characterization-of-breast-lesions-shearlet-transform-and-local-binary-pattern-histogram-techniques
#16
U Rajendra Acharya, Wei Lin Ng, Kartini Rahmat, Vidya K Sudarshan, Joel E W Koh, Jen Hong Tan, Yuki Hagiwara, Arkadiusz Gertych, Farhana Fadzli, Chai Hong Yeong, Kwan Hoong Ng
Shear wave elastography (SWE) examination using ultrasound elastography (USE) is a popular imaging procedure for obtaining elasticity information of breast lesions. Elasticity parameters obtained through SWE can be used as biomarkers that can distinguish malignant breast lesions from benign ones. Furthermore, the elasticity parameters extracted from SWE can speed up the diagnosis and possibly reduce human errors. In this paper, Shearlet transform and local binary pattern histograms (LBPH) are proposed as an original algorithm to differentiate malignant and benign breast lesions...
October 2, 2017: Computers in Biology and Medicine
https://www.readbyqxmd.com/read/29031074/synthesis-antiproliferative-anti-tubulin-activity-and-docking-study-of-new-1-2-4-triazoles-as-potential-combretastatin-analogues
#17
Muhamad Mustafa, Dalia Abdelhamid, ElShimaa M N Abdelhafez, Mahmoud A A Ibrahim, Amira M Gamal-Eldeen, Omar M Aly
Combretastatin A4 (CA4) is a natural product characterized by a powerful inhibition of tubulin polymerization and a potential anticancer activity. However, therapeutic application of CA4 is substantially hindered due to geometric isomerization. In the current study, new cis-restricted Combretastatin A4 analogues containing 1,2,4-triazle in place of the olefinic bond were designed and synthesized. The synthesized compounds were evaluated for their in vitro antiproliferative activity in human hepatocellular carcinoma HepG2 and leukemia HL-60 cell lines using MTT assay...
September 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031069/synthesis-and-biological-evaluation-of-a-platinum-ii-c-rgdyk-conjugate-for-integrin-targeted-photodynamic-therapy
#18
T Chatzisideri, S Thysiadis, S Katsamakas, P Dalezis, I Sigala, T Lazarides, E Nikolakaki, D Trafalis, O A Gederaas, M Lindgren, V Sarli
A cancer-targeting conjugate 4 of a cyclometalated [N,C,N-Pt(II)] complex bearing a NˆCˆN 1,3-di(2-pyridyl)-benzene with c(RGDyK) peptide as guiding molecule was designed and synthesized for real-time drug delivery monitoring in cancer cells and photodynamic therapy (PDT). This conjugate demonstrates a mild cytostatic effect to six cancer cell lines expressing integrins at different extent, while possessing promising features for PDT. Conjugate 4 demonstrated rapid cell uptake by receptor-mediated endocytosis and efficient generation of (1)O2 upon irradiation...
September 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031068/platinum-iv-prodrugs-multiply-targeting-genomic-dna-histone-deacetylases-and-parp-1
#19
Zichen Xu, Weiwei Hu, Zhimei Wang, Shaohua Gou
Several Pt(IV) prodrugs containing SAA, a histone deacetylases inhibitor, were designed and prepared for multiply targeting genomic DNA, histone deacetylases and PARP-1. The resulting Pt(IV) prodrug had significantly strong antiproliferative activity against the tested cancer cell lines, especially SAA1, derived from the conjugation of cisplatin and SAA, had potent ability to overcome cisplatin resistance. Under the combined action of DNA platination and inhibition of HDACs and PARP-1 activity, the cytotoxic activity of SAA1 was 174-fold higher than cisplatin against cisplatin-resistant SGC7901/CDDP cancer cells...
October 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031066/serendipitous-discovery-of-potent-human-head-and-neck-squamous-cell-carcinoma-anti-cancer-molecules-a-fortunate-failure-of-a-rational-molecular-design
#20
Chiara Zagni, Venerando Pistarà, Luciana A Oliveira, Rogerio M Castilho, Giovanni Romeo, Ugo Chiacchio, Antonio Rescifina
Histone deacetylase inhibitors (HDACis) play an important role as valuable drugs targeted to cancer therapy: several HDACis are currently being tested in clinical trials. Two new potential HDACis 1a and 1d, characterized by the presence of a biphenyl-4-sulfonamide group as a connection unit between the N-{4-[(E)-(2-formylhydrazinylidene)methyl]-3-hydroxyphenyl} and the 2-hydroxy-N-(trifluoroacetyl)benzamide moiety, respectively, as two zinc-binding group (ZBG), have been designed, synthesized and tested for their biological activity...
October 5, 2017: European Journal of Medicinal Chemistry
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