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https://www.readbyqxmd.com/read/29786931/real-time-monitoring-of-prodrug-activation-by-direct-mode-of-chemiluminescence
#1
Doron Shabat, Samer Gnaim, Anna Scomparin, Sayantan Das, Ronit Satchi-Fainaro
The majority of theranostic prodrugs reported so far relay information through a fluorogenic response generated upon release of the active chemotherapeutic agent. A chemiluminescence detection mode offers significant advantages over fluorescence, mainly due to the superior signal-to-noise ratio of chemiluminescence. Here we report the design and synthesis of the first theranostic prodrug monitored by a chemiluminescence diagnostic mode. As a representative model we prepared a prodrug from the chemotherapeutic monomethyl auristatin E designed for activation by β-galactosidase...
May 22, 2018: Angewandte Chemie
https://www.readbyqxmd.com/read/29786792/protocols-for-the-study-of-taxanes-chemosensitivity-in-prostate-cancer
#2
M Luz Flores, Carmen Sáez
Prostate cancer is major cause of cancer-related death among men in Western countries. Locally advanced prostate cancers are treated with castration therapy, which is initially effective, but after months the disease progresses to a hormone-refractory state whose treatment is chemotherapy based on taxanes. Although taxanes improve the survival of patients with castration-resistant prostate cancers, these patients often develop chemotherapy resistance, and new therapeutic strategies are necessary. Taxanes exert their action through interaction with β-tubulin which triggers cell cycle arrest in mitosis and the subsequent induction of the intrinsic apoptotic pathway...
2018: Methods in Molecular Biology
https://www.readbyqxmd.com/read/29786670/deubiquitinylase-usp47-promotes-rela-phosphorylation-and-survival-in-gastric-cancer-cells
#3
Lara Naghavi, Martin Schwalbe, Ahmed Ghanem, Michael Naumann
Every year, gastric cancer causes around 819,000 deaths worldwide. The incidence of gastric cancer in the western world is slowly declining, but the prognosis is unpromising. In Germany, the 5-year-survival rate is around 32%, and the average life span after diagnosis is 6 to 9 months. Therapy of gastric cancer patients comprises a gastrectomy and perioperative or adjuvant chemotherapy. However, resistance of gastric cancer cells to these agents is widespread; thus, improved chemotherapeutic approaches are required...
May 22, 2018: Biomedicines
https://www.readbyqxmd.com/read/29785244/more-than-just-an-immunosuppressant-the-emerging-role-of-fty720-as-a-novel-inducer-of-ros-and-apoptosis
#4
REVIEW
Teruaki Takasaki, Kanako Hagihara, Ryosuke Satoh, Reiko Sugiura
Fingolimod hydrochloride (FTY720) is a first-in-class of sphingosine-1-phosphate (S1P) receptor modulator approved to treat multiple sclerosis by its phosphorylated form (FTY720-P). Recently, a novel role of FTY720 as a potential anticancer drug has emerged. One of the anticancer mechanisms of FTY720 involves the induction of reactive oxygen species (ROS) and subsequent apoptosis, which is largely independent of its property as an S1P modulator. ROS have been considered as a double-edged sword in tumor initiation/progression...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29784906/the-anti-cancer-activity-of-an-andrographolide-analogue-functions-through-a-gsk-3%C3%AE-independent-wnt-%C3%AE-catenin-signaling-pathway-in-colorectal-cancer-cells
#5
Somrudee Reabroi, Rungnapha Saeeng, Nittaya Boonmuen, Teerapich Kasemsuk, Witchuda Saengsawang, Kanoknetr Suksen, Weiming Zhu, Pawinee Piyachaturawat, Arthit Chairoungdua
The Wnt/β-catenin signaling pathway plays a key role in the progression of human colorectal cancers (CRCs) and is one of the leading targets of chemotherapy agents developed for CRC. The present study aimed to investigate the anti-cancer effects and molecular mechanisms of 19-O-triphenylmethyl andrographolide (RS-PP-050), an andrographolide analogue and determine its activity in the Wnt/β-catenin pathway. RS-PP-050 was found to potently inhibit the proliferation and survival of HT-29 CRC cells. It induces cell cycle arrest and promotes apoptotic cell death which was associated with the activation of PARP-1 and p53...
May 21, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29783752/pro-apoptotic-and-anti-cancer-properties-of-diosgenin-a-comprehensive-and-critical-review
#6
REVIEW
Gautam Sethi, Muthu K Shanmugam, Sudha Warrier, Myriam Merarchi, Frank Arfuso, Alan Prem Kumar, Anupam Bishayee
Novel and alternative options are being adopted to combat the initiation and progression of human cancers. One of the approaches is the use of molecules isolated from traditional medicinal herbs, edible dietary plants and seeds that play a pivotal role in the prevention/treatment of cancer, either alone or in combination with existing chemotherapeutic agents. Compounds that modulate these oncogenic processes are potential candidates for cancer therapy and may eventually make it to clinical applications. Diosgenin is a naturally occurring steroidal sapogenin and is one of the major bioactive compounds found in dietary fenugreek ( Trigonella foenum-graecum ) seeds...
May 19, 2018: Nutrients
https://www.readbyqxmd.com/read/29783721/azd1775-increases-sensitivity-to-olaparib-and-gemcitabine-in-cancer-cells-with-p53-mutations
#7
Xiangbing Meng, Jianling Bi, Yujun Li, Shujie Yang, Yuping Zhang, Mary Li, Haitao Liu, Yiyang Li, Megan E Mcdonald, Kristina W Thiel, Kuo-Kuang Wen, Xinhao Wang, Meng Wu, Kimberly K Leslie
Tumor suppressor p53 is responsible for enforcing cell cycle checkpoints at G1/S and G2/M in response to DNA damage, thereby allowing both normal and tumor cells to repair DNA before entering S and M. However, tumor cells with absent or mutated p53 are able to activate alternative signaling pathways that maintain the G2/M checkpoint, which becomes uniquely critical for the survival of such tumor cells. We hypothesized that abrogation of the G2 checkpoint might preferentially sensitize p53-defective tumor cells to DNA-damaging agents and spare normal cells with intact p53 function...
May 19, 2018: Cancers
https://www.readbyqxmd.com/read/29782974/molecular-therapy-using-sirna-recent-trends-and-advances-of-multi-target-inhibition-of-cancer-growth
#8
REVIEW
Shweta Jain, Kamla Pathak, Ankur Vaidya
RNA interference (RNAi) therapy, harnessed to produce a new class of drugs for treatment, has drawn attention and seen steady progress over the years. Molecular therapy using biological macromolecules small interfering RNA (siRNA) for gene silencing has received significant attention to target cancer-related genes. Basically, siRNA molecules bind to messenger RNAs (mRNA) by complementary base pairing, to induce degradation of the mRNA and/or block protein synthesis. Numerous genes and gene related proteins have been reported till date to target in siRNA based cancer therapy...
May 18, 2018: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/29782821/licoricidin-enhances-gemcitabine-induced-cytotoxicity-in-osteosarcoma-cells-by-suppressing-the-akt-and-nf-%C3%AE%C2%BAb-signal-pathways
#9
Yifei Wang, Shengli Wang, Jianhua Liu, Yanxiao Lu, Donghui Li
Osteosarcoma (OS) is the most common bone malignancy in children and adolescents. Combined treatments of anti-cancer drugs can remarkably improve chemotherapeutic outcomes. Gemcitabine and licoricidin both have potential anti-tumor activity in several cancers. However, the combined therapeutic efficiency of gemcitabine and licoricidin for OS has not been explored. Here, we found that licoricidin or gemcitabine inhibited OS cell viability in a dose-dependent manner. Cotreatment with licoricidin and gemcitabine enhanced gemcitabine-induced cytotoxicity in OS cells...
May 18, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29781276/light-induced-hypoxia-triggered-living-nanocarriers-for-synergistic-cancer-therapy
#10
Wenliang Wang, Lin Lin, Xiaojing Ma, Bo Wang, Sanrong Liu, Xinxin Yan, Shengran Li, Huayu Tian, Xifei Yu
Living drug delivery system has been proposed as new concept materials since it is able to communicate with biological system, sense subtle changes of body microenvironment caused by disease and then make rapid response to cure in early stage of disease. Herein, taking full advantage of the tumor hypoxia physiology and successive effects of photodynamic therapy (PDT), we designed a new living delivery system via combining the PDT and hypoxia-responsive chemotherapy, abbreviated as Ce6-PEG-Azo-PCL. Then, according to the facts that oxygen can be converted into reactive oxygen species during irradiation of the photosensitizer, tumor cells could be killed after the poly(ethylene glycol) (PEG) conjugated photosensitizer chlorine e6 were irradiated at tumor site...
May 21, 2018: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29780787/non-convulsive-seizure-related-to-cremophor-el%C3%A2-free-polymeric-micelle-formulation-of-paclitaxel-a-case-report
#11
Yoon Sun Shin, Kyung Jin Min, Seung Young Choi, Nak Woo Lee
Paclitaxel is a chemotherapeutic agent that is effective against ovarian, breast, lung, and other cancers. Although peripheral neurotoxicity is among the most common side effects of paclitaxel treatment, central neurotoxicity is rarely reported. When centrally mediated side effects are observed, they are attributed to Cremophor EL™ (CrEL), a surfactant-containing vehicle used for paclitaxel administration. In the present report, we discuss the case of a 72-year-old woman with ovarian carcinoma who experienced a non-convulsive seizure following administration of a CrEL-free, polymeric micelle formulation of paclitaxel...
May 2018: Obstetrics & Gynecology Science
https://www.readbyqxmd.com/read/29777858/cd44-targeted-plga-nanomedicines-for-cancer-chemotherapy
#12
REVIEW
Ankit Saneja, Divya Arora, Robin Kumar, Ravindra Dhar Dubey, Amulya K Panda, Prem N Gupta
In recent years scientific community has drawn a great deal of attention towards understanding the enigma of cluster of differentiation-44 (CD44) in order to deliver therapeutic agents more selectively towards tumor tissues. Moreover, its over-expression in variety of solid tumors has attracted drug delivery researchers to target this receptor with nanomedicines. Conventional nanomedicines based on biodegradable polymers such as poly(lactide-co-glycolide) (PLGA) are often associated with insufficient cellular uptake by cancer cells, due to lack of active targeting moiety on their surface...
May 16, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29777330/down-regulating-il-6-gp130-targets-improved-the-anti-tumor-effects-of-5-fluorouracil-in-colon-cancer
#13
Sanhong Li, Jilai Tian, Hongming Zhang, Shoubing Zhou, Xiyong Wang, Lei Zhang, Jiapeng Yang, Zhigang Zhang, Zhenling Ji
Recent studies have confirmed that IL-6/GP130 targets are closely associated with tumor growth, metastasis and drug resistance. 5-Fluorouracil (5-FU) is the most common chemotherapeutic agent for colon cancer but is limited due to chemoresistance and high cytotoxicity. Bazedoxifene (BZA), a third-generation selective estrogen receptor modulator, was discovered by multiple ligand simultaneous docking and drug repositioning approaches to have a novel function as an IL-6/GP130 target inhibitor. Thus, we speculated that in colon cancer, the anti-tumor efficacy of 5-FU might be increased in combination with IL-6/GP130 inhibitors...
May 18, 2018: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/29775627/acquisition-of-tumorigenic-potential-and-therapeutic-resistance-in-cd133-subpopulation-of-prostate-cancer-cells-exhibiting-stem-cell-like-characteristics
#14
Rajnee Kanwal, Sanjeev Shukla, Ethan Walker, Sanjay Gupta
The role of CD133 (Prominin-1) as a cancer stem cell marker may be useful for therapeutic approaches and prognostication in prostate cancer patients. We investigated the stem-cell-related function and biological features of a subpopulation of CD133+ cells isolated from established primary human prostate cancer cell lines. The CD133+ cells sorted from human prostate cancer 22Rv1 exhibited high clonogenic and tumorigenic capabilities, sphere forming capacity and serially reinitiated transplantable tumors in NOD-SCID mice...
May 15, 2018: Cancer Letters
https://www.readbyqxmd.com/read/29775411/humanin-analogue-hng-enhances-the-protective-effect-of-dexrazoxane-against-doxorubicin-induced-cardiotoxicity
#15
YanHe Lue, Chen Gao, Ronald S Swerdloff, James Hoang, Rozeta Avetisyan, Yue Jia, Meng Rao, Shuxun Ren, Vince Atienza, Junyi Yu, Yie Zhang, Mengping Chen, Yang Song, Yibin Wang, Christina Wang
The chemotherapeutic effect of Doxorubicin (Dox) is limited by cumulative dose-dependent cardiotoxicity in cancer survivors. Dexrazoxane (DRZ) is approved to prevent Dox-induced cardiotoxicity. Humanin and its synthetic analog HNG have cytoprotective effect on the heart. To investigate the cardioprotective efficacy of HNG alone or in combination with DRZ against Dox-induced cardiotoxicity, eighty adult male mice were randomly divided into 8 groups to receive the following treatments via intraperitoneal injection: saline daily; HNG (5mg/kg) daily; DRZ (60mg/kg) weekly; Dox (3mg/kg) weekly; DRZ+HNG, Dox+HNG; Dox+DRZ and Dox+HNG+DRZ...
May 18, 2018: American Journal of Physiology. Heart and Circulatory Physiology
https://www.readbyqxmd.com/read/29774103/bevacizumab-exacerbates-sinusoidal-obstruction-syndrome-sos-in-the-animal-model-and-increases-mmp-9-production
#16
Azin Jafari, Hanno Matthaei, Sven Wehner, Tolga Tonguc, Jörg C Kalff, Steffen Manekeller
Background: Thanks to modern multimodal treatment the ouctome of patients with colorectal cancer has experienced significant improvements. As a downside, agent specific side effects have been observed such as sinusoidal obstruction syndrome (SOS) after oxaliplatin chemotherapy (OX). Bevazicumab targeting VEGF is nowadays comprehensively used in combination protocols with OX but its impact on hepatotoxicity is thus far elusive and focus of the present study. Results: After MCT administration 67% of animals developed SOS...
April 24, 2018: Oncotarget
https://www.readbyqxmd.com/read/29773888/antitumor-effect-of-axitinib-combined-with-dopamine-and-pk-pd-modeling-in-the-treatment-of-human-breast-cancer-xenograft
#17
Yuan-Heng Ma, Si-Yuan Wang, Yu-Peng Ren, Jian Li, Ting-Jie Guo, Wei Lu, Tian-Yan Zhou
Rising evidence has shown the development of resistance to vascular endothelial growth factor receptor (VEGFR) inhibitors in the practices of cancer therapy. It is reported that the efficacy of axitinib (AX), a VEGFR inhibitor, is limited in the treatment of breast cancer as a single agent or in combination with other chemotherapeutic drugs due to the probability of rising population of cancer stem-like cells (CSCs) caused by AX. The present study evaluated the effect of dopamine (DA) improving AX's efficacy on MCF-7/ADR breast cancer in vitro and in vivo, and developed a pharmacokinetic-pharmacodynamic (PK-PD) model describing the in vivo experimental data and characterizing the interaction of effect between AX and DA...
May 17, 2018: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29773172/seleno-l-methionine-and-l-ascorbic-acid-differentiate-the-biological-activity-of-doxorubicin-and-its-metal-complexes-as-a-new-anticancer-drugs-candidate
#18
Marzena Matejczyk, Grzegorz Świderski, Renata Świsłocka, Stanisław Józef Rosochacki, Włodzimierz Lewandowski
The most important problems of anti-cancer therapy include the toxicity of the drugs applied to healthy cells and the multi-drug cells resistance to chemotherapeutics. One of the most commonly used anticancer drugs is doxorubicin (DOX) used to treat certain leukemias and non-Hodgkin's lymphomas, as well as bladder, breast, stomach, lung, ovarian, thyroid, multiple myeloma and other cancers. Preliminary studies showed that metal complex with DOX improve its cytostatic activity with changes in their molecular structure and distribution of electrons, resulting in a substantial change of its biological activity (including antitumor activity)...
July 2018: Journal of Trace Elements in Medicine and Biology
https://www.readbyqxmd.com/read/29772746/design-synthesis-and-biological-evaluation-of-benzimidazole-derived-biocompatible-copper-ii-and-zinc-ii-complexes-as-anticancer-chemotherapeutics
#19
Mohamed F AlAjmi, Afzal Hussain, Md Tabish Rehman, Azmat Ali Khan, Perwez Alam Shaikh, Rais Ahmad Khan
Herein, we have synthesized and characterized a new benzimidazole-derived "BnI" ligand and its copper(II) complex, [Cu(BnI)₂], 1 , and zinc(II) complex, [Zn(BnI)₂], 2 , using elemental analysis and various spectroscopic techniques. Interaction of complexes 1 and 2 with the biomolecules viz. HSA (human serum albumin) and DNA were studied using absorption titration, fluorescence techniques, and in silico molecular docking studies. The results exhibited the significant binding propensity of both complexes 1 and 2 , but complex 1 showed more avid binding to HSA and DNA...
May 16, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29771490/photo-responsive-nanovehicle-for-two-independent-wavelength-light-triggered-sequential-release-of-p-gp-shrna-and-doxorubicin-to-optimize-and-enhance-synergistic-therapy-of-multidrug-resistant-cancer
#20
Ming Wu, Xinyi Lin, Xionghong Tan, Jiong Li, Zuwu Wei, Da Zhang, Youshi Zheng, Ai-Xian Zheng, Bixing Zhao, Yongyi Zeng, Xiaolong Liu, Jingfeng Liu
Pre-release of RNA molecules than chemotherapeutic drugs with a sufficient interval is a vital prerequisite for RNA/drug co-delivery strategy to overcome multidrug resistance (MDR) of cancer cells, but how to precisely control their release at different time points is still a grand challenge up to now. This study aims to on-demand remotely manipulate RNA and drug release in real time through single delivery system to sequentially play their respective roles for optimizing and enhancing their synergistic antitumor effects...
May 17, 2018: ACS Applied Materials & Interfaces
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