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https://www.readbyqxmd.com/read/29149720/a-robust-strategy-for-preparation-of-sequential-stimuli-responsive-block-copolymer-prodrugs-via-thiolactone-chemistry-to-overcome-multiple-anticancer-drug-delivery-barriers
#1
Wendong Ke, Wei Yin, Zengshi Zha, Jean Felix Mukerabigwi, Weijian Chen, Yuheng Wang, Chuanxin He, Zhishen Ge
Block copolymer prodrugs (BCPs) have attracted considerable attentions in clinical translation of nanomedicine owing to their self-assembly into well-defined core-shell nanoparticles for improved pharmacokinetics, stability in blood circulation without drug leakage, and optimized biodistribution. However, a cascade of physiological barriers against specific delivery of drugs into tumor cells limit the final therapeutic efficacy. Herein, we report a robust and facile strategy based on thiolactone chemistry to fabricate well-defined BCPs with sequential tumor pH-promoted cellular internalization and intracellular stimuli-responsive drug release...
November 9, 2017: Biomaterials
https://www.readbyqxmd.com/read/29149148/current-impact-and-application-of-abuse-deterrent-opioid-formulations-in-clinical-practice
#2
Ya-Han Lee, Daniel L Brown, Hsiang-Yin Chen
BACKGROUND: Abuse-deterrent formulations (ADFs) represent one novel strategy for curbing the potential of opioid abuse. OBJECTIVE: We aim to compare and contrast the characteristics and applications of current abuse-deterrent opioid products in clinical practice. METHODS: Literature searches were conducted in databases (Pubmed Medline, International Pharmaceutical Abstracts, Google Scholar) and official reports. Relevant data were screened and organized into: 1) epidemiology of opioid abuse, 2) mitigation strategies for reducing opioid abuse, 3) development of ADFs, and 4) clinical experience with these formulations...
November 2017: Pain Physician
https://www.readbyqxmd.com/read/29147875/evaluation-of-nfsa-like-nitroreductases-from-neisseria-meningitidis-and-bartonella-henselae-for-enzyme-prodrug-therapy-targeted-cellular-ablation-and-dinitrotoluene-bioremediation
#3
Michelle H Rich, Abigail V Sharrock, Kelsi R Hall, David F Ackerley, Joanna K MacKichan
OBJECTIVES: To characterize the activities of two candidate nitroreductases, Neisseria meningitidis NfsA (NfsA_Nm) and Bartonella henselae (PnbA_Bh), with the nitro-prodrugs, CB1954 and metronidazole, and the environmental pollutants 2,4- and 2,6-dinitrotoluene. RESULTS: NfsA_Nm and PnbA_Bh were evaluated in Escherichia coli over-expression assays and as His6-tagged proteins in vitro. With the anti-cancer prodrug CB1954, both enzymes were more effective than the canonical O2-insensitive nitroreductase E...
November 17, 2017: Biotechnology Letters
https://www.readbyqxmd.com/read/29146242/acid-activatable-oxidative-stress-inducing-polysaccharide-nanoparticles-for-anticancer-therapy
#4
Wooyoung Yoo, Donghyuck Yoo, Eunmi Hong, Eunkyeong Jung, Yebin Go, Berwin Singh, Gilson Khang, Dongwon Lee
Drug delivery systems have been extensively developed to enhance the therapeutic efficacy of drugs by altering their pharmacokinetics and biodistribution. However, the use of high quantities of drug delivery systems can cause toxicity due to their poor metabolism and elimination. In this study, we developed polysaccharide-based drug delivery systems which exert potent therapeutic effects and could display synergistic therapeutic effects with drug payloads, leading to dose reduction. Cinnamaldehyde, a major component of cinnamon is known to induce anticancer activity by generating ROS (reactive oxygen species)...
November 13, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/29145770/camptothecin-prodrug-nanomicelle-based-on-a-boronate-ester-linked-diblock-copolymer-as-the-carrier-of-doxorubicin-with-enhanced-cellular-uptake
#5
Ya Gao, Yi Xiao, Shiyuan Liu, Jiahui Yu
A novel pH-sensitive polymeric prodrug of camptothecin (CPT) by polymerizing γ-camptothecin-glutamate N-carboxyanhydride (Glu (CPT)-NCA) on boronate ester-linked poly (ethyleneglycol) (PEG) directly via the amine-initiated ring open polymerization (ROP) has been developed. The resulting amphiphilic prodrug (mPEG-BC-PGluCPT) could self-assemble into nanoparticles and encapsulate doxorubicin (Dox) simultaneously in aqueous solution for dual-drug delivery. The formation of polymeric prodrug micelles (mPEG-BC@PGluCPT) was confirmed by the measurements of critical aggregation concentration (CAC), particle size, and morphology observations...
November 17, 2017: Journal of Biomaterials Science. Polymer Edition
https://www.readbyqxmd.com/read/29144412/pancreatic-cancer-chemoresistance-to-gemcitabine
#6
REVIEW
Manoj Amrutkar, Ivar P Gladhaug
Pancreatic ductal adenocarcinoma (PDAC), commonly referred to as pancreatic cancer, ranks among the leading causes of cancer-related deaths in the Western world due to disease presentation at an advanced stage, early metastasis and generally a very limited response to chemotherapy or radiotherapy. Gemcitabine remains a cornerstone of PDAC treatment in all stages of the disease despite suboptimal clinical effects primarily caused by molecular mechanisms limiting its cellular uptake and activation and overall efficacy, as well as the development of chemoresistance within weeks of treatment initiation...
November 16, 2017: Cancers
https://www.readbyqxmd.com/read/29143021/reversing-the-undesirable-ph-profile-of-doxorubicin-via-activation-of-a-di-substituted-maleamic-acid-prodrug-at-tumor-acidity
#7
Anqi Zhang, Lan Yao, Ming An
The acid-labile behavior of di-substituted maleamic acid (DMA) and its equilibrium with di-substituted maleimide (DMI) are exploited to build an ultra acid-sensitive, small molecule prodrug that can be activated by tumor extracellular pH (pHe) in the range of 6.5-6.9. Such a DMA prodrug reversed the unfavorable pH-profile of doxorubicin (Dox), which may improve its therapeutic window.
November 16, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29138559/human-mesenchymal-stem-cell-derived-iron-oxide-exosomes-allow-targeted-ablation-of-tumor-cells-via-magnetic-hyperthermia
#8
U Altanerova, M Babincova, P Babinec, K Benejova, J Jakubechova, V Altanerova, M Zduriencikova, V Repiska, C Altaner
Magnetic hyperthermia, or the heating of tissues using magnetic materials, is a promising approach for treating cancer. We found that human mesenchymal stem cells (MSCs) isolated from various tissues and MSCs expressing the yeast cytosine deaminase∷uracil phosphoribosyl transferase suicide fusion gene (yCD∷UPRT) can be labeled with Venofer, an iron oxide carbohydrate nanoparticle. Venofer labeling did not affect cell proliferation or the ability to home to tumors. All Venofer-labeled MSCs released exosomes that contained iron oxide...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29138558/%C3%AE-v%C3%AE-3-integrin-targeted-micellar-mertansine-prodrug-effectively-inhibits-triple-negative-breast-cancer-in-vivo
#9
Ping Zhong, Xiaolei Gu, Ru Cheng, Chao Deng, Fenghua Meng, Zhiyuan Zhong
Antibody-mertansine (DM1) conjugates (AMCs) are among the very few active targeting therapeutics that are approved or clinically investigated for treating various cancers including metastatic breast cancer. However, none of the AMCs are effective for the treatment of triple-negative breast cancers (TNBCs). Here, we show that cRGD-decorated, redox-activatable micellar mertansine prodrug (cRGD-MMP) can effectively target and deliver DM1 to αvβ3 integrin overexpressing MDA-MB-231 TNBC xenografts in nude mice, resulting in potent tumor growth inhibition...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29135083/comparison-of-the-anticancer-properties-of-a-novel-valproic-acid-prodrug-to-leading-histone-deacetylase-inhibitors
#10
Nataly Tarasenko, Hanna Chekroun-Setti, Abraham Nudelman, Ada Rephaeli
The HDAC inhibitory activity of valproic acid (VPA) has led to on-going evaluation of it as an anticancer agent. The histone deacetylase (HDAC) inhibitor AN446, a prodrug of VPA, releases the acid upon metabolic degradation. AN446 is >60 fold more potent than VPA in killing cancer cells in vitro. Herein, we compare the activities of AN446, as an anticancer agent, to those of representative types from each of the four major classes of HDAC inhibitors (HDACIs): vorinostat, romidepsin, entinostat and VPA. AN446 exhibited the greatest selectivity and HDAC inhibitory activity against cancer cells...
November 14, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29134566/lisdexamfetamine-a-review-in-binge-eating-disorder
#11
Young-A Heo, Sean T Duggan
Oral lisdexamfetamine dimesylate (Vyvanse(®); lisdexamfetamine), a prodrug of dextroamfetamine, is currently the only drug to be approved in the USA for the treatment of moderate to severe binge eating disorder (BED) in adult patients. Its approval was based on the results of two pivotal short-term (12 weeks) phase III studies, which showed a significantly greater reduction in binge eating days/week at the end of the study with lisdexamfetamine 50-70 mg/day than with placebo. The findings of these studies have been supported and extended by the results of longer-term (≤ 52 weeks) phase III studies, including one with a randomized 26-week withdrawal phase, which showed that lisdexamfetamine markedly reduced the risk of BED relapse relative to placebo...
November 13, 2017: CNS Drugs
https://www.readbyqxmd.com/read/29133205/hpma-copolymer-conjugate-with-pirarubicin-in-vitro-and-ex-vivo-stability-and-drug-release-study
#12
Waliul Islam, Jun Fang, Tomas Etrych, Petr Chytil, Karel Ulbrich, Akihiro Sakoguchi, Katsuki Kusakabe, Hiroshi Maeda
We have developed a tumor environment-responsive polymeric anticancer prodrug containing pirarubicin (THP) conjugated to N-(2-hydroxypropyl) methacrylamide copolymer (PHPMA), [P-THP], through a spacer containing pH-sensitive hydrazone bond, that showed remarkable therapeutic effect against various tumor models and in a human pilot study. Toward clinical development, here we report THP release profile from its HPMA copolymer conjugate, the conjugate stability, protein and cell-binding and solubility of P-THP...
November 10, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29131563/sustained-codelivery-of-cisplatin-and-paclitaxel-via-an-injectable-prodrug-hydrogel-for-ovarian-cancer-treatment
#13
Wenjia Shen, Xiaobin Chen, Jiabin Luan, Danni Wang, Lin Yu, Jiandong Ding
The sustained release of both the hydrophilic drug and hydrophobic drug from one delivery system remains challenging in pharmaceutics and biomaterials science. The combination of hydrophilic cisplatin and hydrophobic paclitaxel (PTX) exhibits a clinical survival advantage compared with the individual drug therapy against various tumors such as ovarian cancer. In this study, a localized, long-term codelivery system of cisplatin and PTX was developed using an injectable and thermosensitive polymer-platinum(IV) conjugate hydrogel as the carrier...
November 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29131143/nonimmune-cells-equipped-with-t-cell-receptor-like-signaling-for-cancer-cell-ablation
#14
Ryosuke Kojima, Leo Scheller, Martin Fussenegger
The ability to engineer custom cell-contact-sensing output devices into human nonimmune cells would be useful for extending the applicability of cell-based cancer therapies and for avoiding risks associated with engineered immune cells. Here we have developed a new class of synthetic T-cell receptor-like signal-transduction device that functions efficiently in human nonimmune cells and triggers release of output molecules specifically upon sensing contact with a target cell. This device employs an interleukin signaling cascade, whose OFF/ON switching is controlled by biophysical segregation of a transmembrane signal-inhibitory protein from the sensor cell-target cell interface...
November 13, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/29130344/neurokinin-1-receptor-antagonists-in-the-prevention-of-chemotherapy-induced-nausea-and-vomiting-focus-on-fosaprepitant
#15
Bernardo L Rapoport, Karin Jordan, Cindy Weinstein
Chemotherapy-induced nausea and vomiting (CINV) remains a challenge in cancer care. Improved understanding of CINV pathophysiology has triggered the development of new antiemetic therapeutic options, such as selective neurokinin-1 (NK1) receptor antagonists (RAs), which effectively prevent CINV when added to a standard antiemetic regimen (serotonin-3 RA and dexamethasone). Aprepitant and its water-soluble prodrug, fosaprepitant dimeglumine, are the most widely used NK1 RAs, with extensive clinical use worldwide...
November 13, 2017: Future Oncology
https://www.readbyqxmd.com/read/29129789/dual-ph-responsive-multifunctional-nanoparticles-for-targeted-treatment-of-breast-cancer-by-combining-immunotherapy-and-chemotherapy
#16
Yuanyuan Liu, Linan Qiao, Sipei Zhang, Guoyun Wan, Bowei Chen, Ping Zhou, Ning Zhang, Yinsong Wang
In the present study, a dual pH-responsive multifunctional nanoparticle system was designed for combining immunotherapy and chemotherapy to treat breast cancer through targeting immune cells and cancer cells. A proven anti-tumor immune regulator, R848, was encapsulated with poly(L-histidine) (PHIS) to form PHIS/R848 nanocores. Doxorubicin (DOX) was conjugated to hyaluronic acid (HA) through an acid-cleavable hydrazone bond linkage to synthesize polymeric prodrug HA-DOX, which was subsequently coated outside PHIS/R848 nanocores to form HA-DOX/PHIS/R848 nanoparticles...
November 9, 2017: Acta Biomaterialia
https://www.readbyqxmd.com/read/29128843/shape-controlled-magnetic-mesoporous-silica-nanoparticles-for-magnetically-mediated-suicide-gene-therapy-of-hepatocellular-carcinoma
#17
Zheng Wang, Zhimin Chang, Mengmeng Lu, Dan Shao, Juan Yue, Dian Yang, Xiao Zheng, Mingqiang Li, Kan He, Ming Zhang, Li Chen, Wen-Fei Dong
Magnetic nanoparticles (NPs) have emerged as a promising tool for suicide gene therapy. However, the separate delivery of the suicide gene and prodrug in current systems limits their clinical translation. Therefore, improving magnetically mediated suicide gene therapy by exploring higher performance magnetic NP-based hybrid nanoplatforms is an important challenge. In the current study, shape-controlled magnetic mesoporous silica nanoparticles (M-MSNs) were prepared, and their performance in magnetic resonance imaging (MRI)-guided, magnetically targeted and hyperthermia-enhanced suicide gene therapy of hepatocellular carcinoma (HCC) was investigated...
November 4, 2017: Biomaterials
https://www.readbyqxmd.com/read/29127937/reduction-sensitive-mixed-micelles-assembled-from-amphiphilic-prodrugs-for-self-codelivery-of-dox-and-dtx-with-synergistic-cancer-therapy
#18
Jilian Wu, Huiyuan Zhang, Xu Hu, Ruiling Liu, Wei Jiang, Zhonghao Li, Yuxia Luan
Clinically, codelivery of chemotherapeutics has been limited by poor water-solubility and severe systemic toxicity. In this work, we developed a new reduction-sensitive mixed micellar system for self-codelivery of doxorubicin (DOX) and docetaxel (DTX). Biodegradable methoxy poly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL) was coupled with DOX and DTX by a reduction-sensitive disulfide bond, resulting in mPEG-PCL-SS-DOX and mPEG-PCL-SS-DTX, respectively. mPEG-PCL-SS-DOX was mixed with mPEG-PCL-SS-DTX at a mole ratio of 1:1 in water, forming a mixed micellar system...
November 6, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/29127277/dual-protein-kinase-and-nucleoside-kinase-modulators-for-rationally-designed-polypharmacology
#19
Kahina Hammam, Magali Saez-Ayala, Etienne Rebuffet, Laurent Gros, Sophie Lopez, Berengere Hajem, Martine Humbert, Emilie Baudelet, Stephane Audebert, Stephane Betzi, Adrien Lugari, Sebastien Combes, Sebastien Letard, Nathalie Casteran, Colin Mansfield, Alain Moussy, Paulo De Sepulveda, Xavier Morelli, Patrice Dubreuil
Masitinib, a highly selective protein kinase inhibitor, can sensitise gemcitabine-refractory cancer cell lines when used in combination with gemcitabine. Here we report a reverse proteomic approach that identifies the target responsible for this sensitisation: the deoxycytidine kinase (dCK). Masitinib, as well as other protein kinase inhibitors, such as imatinib, interact with dCK and provoke an unforeseen conformational-dependent activation of this nucleoside kinase, modulating phosphorylation of nucleoside analogue drugs...
November 10, 2017: Nature Communications
https://www.readbyqxmd.com/read/29127031/sulfur-mustard-induced-mast-cell-degranulation-in-mouse-skin-is-inhibited-by-a-novel-anti-inflammatory-and-anticholinergic-bifunctional-prodrug
#20
Laurie B Joseph, Gabriella M Composto, Roberto M Perez, Hong-Duck Kim, Robert P Casillas, Ned D Heindel, Sherri C Young, Carl J Lacey, Jaya Saxena, Christophe D Guillon, Claire R Croutch, Jeffrey D Laskin, Diane E Heck
Sulfur mustard (SM, bis(2-chloroethyl sulfide) is a potent vesicating agent known to cause skin inflammation, necrosis and blistering. Evidence suggests that inflammatory cells and mediators that they generate are important in the pathogenic responses to SM. In the present studies we investigated the role of mast cells in SM-induced skin injury using a murine vapor cup exposure model. Mast cells, identified by toluidine blue staining, were localized in the dermis, adjacent to dermal appendages and at the dermal/epidermal junction...
November 7, 2017: Toxicology Letters
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