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https://www.readbyqxmd.com/read/29775284/multifunctional-tumor-targeting-cathepsin-b-sensitive-gemcitabine-prodrug-covalently-targets-albumin-in-situ-and-improves-cancer-therapy
#1
Huicong Zhang, Zhisu Sun, Kuanglei Wang, Na Li, Hongxiang Chen, Xiao Tan, Lingxiao Li, Zhonggui He, Jin Sun
We report a new type of amide bond-bearing cathepsin B-sensitive gemcitabine (GEM) prodrugs, capable of in situ covalently targeting circulating albumin and then making a hitchhike to the tumor. Specially, less plasma-enzyme deactivation, long plasma half-life, independence on nucleoside transporters, outstanding tumor targeting and site-specific drug release are achieved and such these multifunctional advantages contribute to the dramatically increased in vivo antitumor efficacy.
May 18, 2018: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/29774608/virion-like-membrane-breaking-nanoparticles-with-tumor-activated-cell-and-tissue-dual-penetration-conquer-impermeable-cancer
#2
Xiao Zhang, Xianghui Xu, Yachao Li, Cheng Hu, Zhijun Zhang, Zhongwei Gu
Poor drug penetration into tumor cells and tissues is a worldwide difficulty in cancer therapy. A strategy is developed for virion-like membrane-breaking nanoparticles (MBNs) to smoothly accomplish tumor-activated cell-and-tissue dual-penetration for surmounting impermeable drug-resistant cancer. Tailor-made dendritic arginine-rich peptide prodrugs are designed to mimic viral protein transduction domains and globular protein architectures. Attractively, these protein mimics self-assemble into virion-like nanoparticles in aqueous solution, having highly ordered secondary structure...
May 17, 2018: Advanced Materials
https://www.readbyqxmd.com/read/29774078/targeting-intracellular-mmps-efficiently-inhibits-tumor-metastasis-and-angiogenesis
#3
Yaqi Lv, Xiangmei Zhao, Lidan Zhu, Sijia Li, Qingqing Xiao, Wei He, Lifang Yin
Treatment for metastatic cancer is a great challenge throughout the world. Commonly, directed inhibition of extracellular matrix metalloproteinases (MMPs) secreted by cancer cells can reduce metastasis. Here, a novel nanoplatform (HPMC NPs) assembled from hyaluronic acid (HA)-paclitaxel (PTX) prodrug and marimastat (MATT)/β-casein (CN) complexes was established to cure a 4T1 metastatic cancer model via targeting CD44 and intracellular, rather than extracellular, MMPs. Methods: HPMC NPs were prepared by assembling the complexes and prodrug under ultrasonic treatment, which the interaction between them was evaluated by förster resonance energy transfer, circular dichroism and fluorescence spectra...
2018: Theranostics
https://www.readbyqxmd.com/read/29773381/cd44-targeted-hyaluronic-acid-curcumin-prodrug-protects-renal-tubular-epithelial-cell-survival-from-oxidative-stress-damage
#4
Jing-Bo Hu, Shu-Juan Li, Xu-Qi Kang, Jing Qi, Jia-Hui Wu, Xiao-Juan Wang, Xiao-Ling Xu, Xiao-Ying Ying, Sai-Ping Jiang, Jian You, Yong-Zhong Du
Based on the abnormally increased expression of CD44 receptors on renal tubule epithelial cells during ischemia/reperfusion-induced acute kidney injury (AKI), we developed a hyaluronic acid-curcumin (HA-CUR) polymeric prodrug targeting to epithelial cells and then relieving oxidative stress damages. The water solubility of HA-CUR was significantly enhanced and approximately 27-fold higher than that of CUR. Cellular uptake test showed HA-CUR was preferably internalized by H2 O2 -pretreated tubular epithelial (HK-2) cells compared with free CUR benefiting from the specific binding between HA and CD44 receptors...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29773367/reduction-active-polymeric-prodrug-micelles-based-on-%C3%AE-cyclodextrin-polyrotaxanes-for-triggered-drug-release-and-enhanced-cancer-therapy
#5
Shuang Bai, Meili Hou, Xiaoxiao Shi, Jiucun Chen, Xiaoqian Ma, Yong-E Gao, Yajun Wang, Peng Xue, Yuejun Kang, Zhigang Xu
As one of the medical polymers approved by US Food and Drug Administration (FDA), poly(ethylene glycol) has low toxicity, high stability, good biocompatibility, unique physical and chemical properties. Cyclodextrin is an ideal candidate as a drug carrier due to its special structures and characteristics. These two materials were successfully assembled through chemosynthesis in combination with the hydrophilic poly(ethylene glycol) methyl ether methacrylate (OEGMA) chain and hydrophobic polymeric camptothecin (CPT) chain by atom transfer radical polymerization (ATRP)...
August 1, 2018: Carbohydrate Polymers
https://www.readbyqxmd.com/read/29772747/involvement-of-cyp4f2-in-the-metabolism-of-a-novel-monophosphate-ester-prodrug-of-gemcitabine-and-its-interaction-potential-in-vitro
#6
Yedong Wang, Yuan Li, Jia Lu, Huixin Qi, Isabel Cheng, Hongjian Zhang
Compound- 3 is an oral monophosphate prodrug of gemcitabine. Previous data showed that Compound- 3 was more potent than gemcitabine and it was orally active in a tumor xenograft model. In the present study, the metabolism of Compound- 3 was investigated in several well-known in vitro matrices. While relatively stable in human and rat plasma, Compound- 3 demonstrated noticeable metabolism in liver and intestinal microsomes in the presence of NADPH and human hepatocytes. Compound- 3 could also be hydrolyzed by alkaline phosphatase, leading to gemcitabine formation...
May 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29772538/targeting-fibroblast-activation-protein-in-cancer-prospects-and-caveats
#7
Petr Busek, Rosana Mateu, Michal Zubal, Lenka Kotackova, Aleksi Sedo
Fibroblast activation protein (FAP, seprase) is a serine protease with post-proline dipeptidyl peptidase and endopeptidase enzymatic activity. FAP is upregulated in several tumor types, while its expression in healthy adult tissues is scarce. FAP molecule itself and FAP+ stromal cells play an important although probably context-dependent and tumor type-specific pathogenetic role in tumor progression. We provide an overview of FAP expression under both physiological and pathological conditions with focus on human malignancies...
June 1, 2018: Frontiers in Bioscience (Landmark Edition)
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
#8
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
https://www.readbyqxmd.com/read/29770812/reduction-photo-dual-responsive-polymeric-prodrug-nanoparticles-for-programmed-sirna-and-doxorubicin-delivery
#9
Ming Wu, Jiong Li, Xinyi Lin, Zuwu Wei, Da Zhang, Bixing Zhao, Xiaolong Liu, Jingfeng Liu
Dual and multi-stimuli responsive polymeric nanoparticles that respond to two or more signals can further improve drug release performance compared with nanoparticles that respond to a single stimulus. However, usage of such nanoparticles to deliver siRNA and chemotherapeutic drugs in a sequential manner are currently very rare; meanwhile, this technology is vital to optimize the efficacy of chemotherapy towards cancer cells with multidrug resistance. By loading o-nitrobenzyl ester derivative caged DOX (DOC) into the inner poly(lactic-co-glycolic acid) (PLGA) core and adsorbing siRNA of P-gp protein onto the cationic polymeric shell derived from a disulfide-containing alkyl modified polyethylenimine (C16-S-S-PEI), here, a reduction/photo dual responsive device (RPDRD) is successfully designed for programmed P-gp siRNA and doxorubicin delivery...
May 17, 2018: Biomaterials Science
https://www.readbyqxmd.com/read/29768881/lipophilic-prodrug-of-floxuridine-loaded-into-solid-lipid-nanoparticles-in-vitro-cytotoxicity-studies-on-different-human-cancer-cell-lines
#10
Daniela Chirio, Elena Peira, Luigi Battaglia, Benedetta Ferrara, Alessandro Barge, Simona Sapino, Susanna Giordano, Chiara Dianzani, Marina Gallarate
Floxuridine is a very effective drug with high potency in the treatment of various tumors but its utility is limited by its low efficiency of cellular uptake. In order to improve the floxuridine efficiency of cellular uptake, lipophilic prodrug of floxuridine (3',5'-distearoyl-5-fluoro-2'-deoxyuridine) was synthetized and loaded into behenic acid nanoparticles produced by fatty acid coacervation technique. Generally, spherical shaped SLN with mean diameters below 300 nm were obtained. Distearoyl-floxuridine was loaded in SLN with high entrapment efficiency (from 70...
January 1, 2018: Journal of Nanoscience and Nanotechnology
https://www.readbyqxmd.com/read/29768713/clinical-drug-drug-interaction-potential-of-bfe1224-prodrug-of-antifungal-ravuconazole-using-two-types-of-cocktails-in-healthy-subjects
#11
Yasuyuki Ishii, Yuko Ito, Shunji Matsuki, Kasumi Sanpei, Osamu Ogawa, Kenji Takeda, Edgar L Schuck, Naoto Uemura
BFE1224, prodrug of ravuconazole, is a novel, once-daily, oral, triazole antifungal drug, and currently in development for the treatment of onychomycosis. The clinical drug-drug interaction (DDI) potential of BFE1224 with cytochrome P450 (CYP) and transporter was assessed by using two types of cocktails in healthy subjects in separate clinical studies. The CYP and transporter cocktails consisted of caffeine/tolbutamide/omeprazole/dextromethorphan/midazolam used in study 1 and digoxin/rosuvastatin used in study 2...
May 16, 2018: Clinical and Translational Science
https://www.readbyqxmd.com/read/29768008/striking-a-balance-between-carbonate-carbamate-linkage-bond-and-reduction-sensitive-disulfide-bond-bearing-linker-for-tailored-controlled-release-in-situ-covalently-albumin-binding-gemcitabine-prodrugs-promote-bioavailability-and-tumor-accumulation
#12
Huicong Zhang, Kuanglei Wang, Kexin Na, Dan Li, Zhenbao Li, Dongyang Zhao, Lu Zhong, Menglin Wang, Longfa Kou, Cong Luo, Haotian Zhang, Qiming Kan, Huaiwei Ding, Zhonggui He, Jin Sun
To address the challenge of rapid enzyme inactivation, poor tumor targeting, acquired drug resistance in gemcitabine (GEM) application, we report two groups of maleimide-functionalised GEM prodrugs conjugating covalently in situ with cys-34 of blood-circulating albumin, resulting in macromolecular prodrugs after intravenous administration. Specially, tailored and accurate controlled release was achieved through different combinations of linkage bonds relatively stable and labile (carbamate and carbonate, respectively) and linkers with or without insertion of a disulfide bond...
May 16, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29767448/development-and-validation-of-a-fast-and-sensitive-uhplc-esi-ms-method-for-the-simultaneous-quantification-of-spironolactone-and-its-metabolites-in-ocular-tissues
#13
Naoual Dahmana, Doris Gabriel, Robert Gurny, Yogeshvar N Kalia
Glucocorticoids are a mainstay for the treatment of immune-mediated conditions and inflammatory diseases. However, their chronic use causes numerous side-effects including delays in corneal and cutaneous wound healing. This is attributed to off-target agonism of the mineralocorticoid receptor, which can be reduced by co-administration of a mineralocorticoid receptor antagonist such as spironolactone. The aim of this study was to develop a fast, selective and sensitive UHPLC-ESI-MS method for the simultaneous quantification of spironolactone, its active metabolites - 7α-thiomethylspironolactone and canrenone, the latter's water-soluble prodrug potassium canrenoate, and the synthetic glucocorticoid, dexamethasone, in corneal samples (17α-methyltestosterone served as an internal standard)...
May 16, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29766157/dual-acting-antitumor-pt-iv-prodrugs-of-kiteplatin-with-dichloroacetate-axial-ligands
#14
Salvatore Savino, Valentina Gandin, James D Hoeschele, Cristina Marzano, Giovanni Natile, Nicola Margiotta
With the aim to obtain dual acting drugs able to target both nuclear DNA and mitochondria, Pt(iv) kiteplatin derivatives having dichloroacetate (DCA) ligands in axial positions have been synthesized. The rather fast hydrolysis (t1/2 of ca. 1 h) and reduction (by ascorbic acid) of these Pt(iv) derivatives did not impede a potent pharmacological effect on tumor cells. Moreover, similarly to kiteplatin, also the Pt(iv)-DCA compounds proved to be capable of overcoming oxaliplatin-resistance, which is particularly important in view of the fact that metastatic colorectal cancer is the third most common cancer in males and the second in females...
May 16, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29765659/self-assembly-behaviours-of-peptide-drug-conjugates-influence-of-multiple-factors-on-aggregate-morphology-and-potential-self-assembly-mechanism
#15
Qin Fan, Yujie Ji, Jingjing Wang, Li Wu, Weidong Li, Rui Chen, Zhipeng Chen
Peptide-drug conjugates (PDCs) as self-assembly prodrugs have the unique and specific features to build one-component nanomedicines. Supramolecular structure based on PDCs could form various morphologies ranging from nanotube, nanofibre, nanobelt to hydrogel. However, the assembly process of PDCs is too complex to predict or control. Herein, we investigated the effects of extrinsic factors on assembly morphology and the possible formation of nanostructures based on PDCs. To this end, we designed a PDC consisting of hydrophobic drug ( S )-ketoprofen (Ket) and valine-glutamic acid dimeric repeats peptide (L-VEVE) to study their assembly behaviour...
April 2018: Royal Society Open Science
https://www.readbyqxmd.com/read/29764744/effective-gene-silencing-activity-of-prodrug-type-2-o-methyldithiomethyl-sirna-compared-with-non-prodrug-type-2-o-methyl-sirna
#16
Junsuke Hayashi, Misa Nishigaki, Yosuke Ochi, Shun-Ichi Wada, Fumito Wada, Osamu Nakagawa, Satoshi Obika, Mariko Harada-Shiba, Hidehito Urata
Small interfering RNAs (siRNAs) are an active agent to induce gene silencing and they have been studied for becoming a biological and therapeutic tool. Various 2'-O-modified RNAs have been extensively studied to improve the nuclease resistance. However, the 2'-O-modified siRNA activities were often decreased by modification, since the bulky 2'-O-modifications inhibit to form a RNA-induced silencing complex (RISC). We developed novel prodrug-type 2'-O-methyldithiomethyl (MDTM) siRNA, which is converted into natural siRNA in an intracellular reducing environment...
May 8, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29764490/efficacy-of-the-hypoxia-activated-prodrug-evofosfamide-th-302-in-nasopharyngeal-carcinoma-in-vitro-and-in-vivo
#17
Yan Huang, Ying Tian, Yuanyuan Zhao, Cong Xue, Jianhua Zhan, Lin Liu, Xiaobo He, Li Zhang
BACKGROUND: Tumor hypoxia is considered an important factor in metastasis and disease relapse. Evofosfamide is a hypoxia-activated prodrug that selectively targets the hypoxic regions of solid tumors. As hypoxia-inducible factor-1α (HIF-1α) is overexpressed in nasopharyngeal carcinoma (NPC) tissues, we performed the present study to evaluate the efficacy profile of evofosfamide in NPC. METHODS: We evaluated the efficacy of evofosfamide as a single agent or combined with cisplatin (DDP) in the NPC cell lines CNE-2, HONE-1 and HNE-1, and in nude mouse xenograft tumor models...
May 3, 2018: Cancer communications
https://www.readbyqxmd.com/read/29763687/therapeutic-efficacy-of-lipid-emulsions-of-docetaxel-linoleic-acid-conjugate-in-breast-cancer
#18
Tao Zhang, Meng Li, Ruyi Yang, Dong Zhang, Jibin Guan, Jiang Yu, Bin Yang, Huicong Zhang, Shenwu Zhang, Dan Liu, Yongjun Wang
Docetaxel (DTX) solution is among the most widely-used parenteral formulations used in advanced breast cancer therapy. However, severe side effects have been observed due to the use of ethanol and polysorbate 80. Herein, a novel DTX-based prodrug, docetaxel-linoleic acid conjugate (DTX-LA) was successfully synthesized. The high lipid solubility of DTX and DTX-LA resulted in a tendency for them to become entrapped in the oil core of the emulsions. As anticipated, nano-sized, sterically stabilized oil-in-water lipid emulsions (LMs) of DTX-LA LMs and DTX LMs were successfully constructed...
May 12, 2018: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/29762011/strategies-toward-organic-carbon-monoxide-prodrugs
#19
Xingyue Ji, Binghe Wang
Carbon monoxide is widely acknowledged as an important gasotransmitter in the mammalian system with importance on par with that of nitric oxide. It has also been firmly established as a potential therapeutic agent with a wide range of indications including organ transplantation, cancer, bacterial infection, and inflammation-related conditions such as colitis and sepsis. One major issue in developing CO based therapeutics is its delivery in a pharmaceutically acceptable form. Currently, there are generally five forms of deliveries: inhaled CO, photosensitive CO-releasing molecules, encapsulated CO, CO dissolved in drinks, and molecules that would release CO under physiological conditions without the need for light...
May 15, 2018: Accounts of Chemical Research
https://www.readbyqxmd.com/read/29761789/ph-and-redox-responsive-nanoparticles-composed-of-charge-reversible-pullulan-based-shells-and-disulfide-containing-poly-%C3%AE-amino-ester-cores-for-co-delivery-of-gene-and-chemotherapeutic-agent
#20
Sipei Zhang, Dan Wang, Yating Li, Ling Li, Hongli Chen, Qingqing Xiong, Yuan-Yuan Liu, Yingsong Wang
A novel pH- and redox-responsive nanoparticle system was designed based on charge-reversible pullulan derivative (CAPL) and disulfide-containing poly(β-amino ester) (ssPBAE) for the co-delivery of gene and chemotherapeutic agent targeting hepatoma. The end-alkene groups of ssPBAE were reacted with diethylenetriamine to form amino-modified ssPBAE (NH-ssPBAE). Methotrexate (MTX), a chemotherapy agent, was then conjugated to NH-ssPBAE via amide bond to obtain a polymeric prodrug ssPBAE-MTX. ssPBAE-MTX exhibited a good capability for condensing genes including plasmid DNA (pDNA) and tetramethyl rhodamine-labeled DNA (TAMRA-DNA), and almost completely condensed pDNA at the weight ratio of 5/1 to form spherical nanocomplexes with an uniform size...
May 15, 2018: Nanotechnology
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