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https://www.readbyqxmd.com/read/27904057/potential-of-ravuconazole-and-its-prodrugs-as-the-new-oraltherapeutics-for-onychomycosis
#1
Hideyo Yamaguchi
Onychomycosis is a fungal infection of the nail apparatus caused by dermatophytes, Candida and non-dermatophytic molds. It is highly prevalent in the general population worldwide and also responsible for significant morbidity and complications and does not usually cure itself. Thus, the condition needs to be treated in view of physical and psychological problems produced. Currently, oral medications using terbinafine are the most effective therapy, but it has relatively limited therapeutic success, particularly for long-term management...
2016: Medical Mycology Journal
https://www.readbyqxmd.com/read/27899985/possible-role-of-thymidine-phosphorylase-in-gynecological-tumors-as-an-individualized-treatment-strategy
#2
Masako Shida, Masanori Yasuda, Mariko Fujita, Masaki Miyazawa, Hiroshi Kajiwara, Takeshi Hirasawa, Masae Ikeda, Naruaki Matsui, Toshinari Muramatsu, Mikio Mikami
Thymidine phosphorylase (TP) is structurally similar to platelet-derived endothelial cell growth factor, and it activates 5-fluorouracil (5-FU) prodrugs and also promotes angiogenesis. In the present study, the possibility of using TP expression as a biomarker for 5-FU prodrugs, and the significance of TP as an angiogenic factor, were investigated in patients with gynecological tumors. The subjects enrolled in the study were 188 patients with gynecological tumors who provided informed consent and underwent tumor resection at the Department of Obstetrics and Gynecology of Tokai University Hospital between February 2002 and January 2010...
November 2016: Oncology Letters
https://www.readbyqxmd.com/read/27898344/may-glutamine-addiction-drive-the-delivery-of-antitumor-cisplatin-based-pt-iv-prodrugs
#3
Mauro Ravera, Elisabetta Gabano, Stefano Tinello, Ilaria Zanellato, Domenico Osella
A small series of Pt(IV) prodrugs containing Gln-like (Gln=glutamine) axial ligands has been designed with the aim to take advantage of the increased demand of Gln showed by some cancer cells (glutamine addiction). In complex 4 the Gln, linked through the α-carboxylic group is recognized by the Gln transporters, in particular by the solute carrier transporter SLC1A5. All compounds showed cellular accumulation, as well as antiproliferative activity, related to their lipophilicity, as already demonstrated for the majority of Pt(IV) prodrugs, that enter cells mainly by passive diffusion...
November 17, 2016: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/27898328/fate-of-new-three-anti-influenza-drugs-and-one-prodrug-in-the-water-environment
#4
Takashi Azuma, Mao Ishida, Kanae Hisamatsu, Ayami Yunoki, Kana Otomo, Mari Kunitou, Mai Shimizu, Kaori Hosomaru, Shiori Mikata, Yoshiki Mino
We evaluated the environmental fate of new three anti-influenza drugs, favipiravir (FAV), peramivir (PER), and laninamivir (LAN), and an active prodrug of LAN, laninamivir octanoate (LANO), in comparison with four conventional drugs, oseltamivir (OS), oseltamivir carboxylate (OC), amantadine (AMN), and zanamivir (ZAN) by photodegradation, biodegradation, and sorption to river sediments. In addition, we conducted 9-month survey of urban rivers in the Yodo River basin from 2015 to 2016 (including the influenza season) to investigate the current status of occurrence of these drugs in the river environment...
November 26, 2016: Chemosphere
https://www.readbyqxmd.com/read/27895114/in-vitro-and-clinical-evaluations-of-the-drug-drug-interaction-potential-of-a-metabotropic-glutamate-2-3-receptor-agonist-prodrug-at-pept1
#5
Y Anne Pak, Amanda J Long, William F Annes, Jennifer W Witcher, Mary Pat Knadler, Mosun A Ayan-Oshodi, Malcolm I Mitchell, Phillip Leese, Kathleen M Hillgren
Despite PEPT1 being responsible for the bioavailability for a variety of drugs, there has been little study of its potential involvement in drug-drug interactions. Pomaglumetad methionil, a metabotropic glutamate 2/3 receptor agonist prodrug, utilizes PEPT1 to enhance absorption and bioavailability. In vitro studies were conducted to guide the decision to conduct a clinical drug interaction study and to inform the clinical study design. In vitro investigations determined the prodrug (LY2140023 monohydrate) is a substrate of PEPT1 with Km value of approximately 30 μM, while the active moiety (LY404039) is not a PEPT1 substrate...
November 28, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27892656/cytochrome-p450-bioconjugate-as-a-nanovehicle-for-improved-chemotherapy-treatment
#6
Katrin Quester, Karla Juarez-Moreno, Isamel Secundino, Yvonne Roseinstein, Karla P Alejo, Alejandro Huerta-Saquero, Rafael Vazquez-Duhalt
Cancer is still a growing public health problem, especially breast cancer that is one of the most important cancers in women. Chemotherapy, even though a successful treatment, is accompanied by severe side effects. Moreover, most of the drugs used for chemotherapy are administered as prodrugs and need to be transformed to the active form by cytochromes P450 (CYPs). In addition, increasing numbers of cancer tissues show lower CYP activity than the surrounding healthy tissues in which prodrugs are preferentially activated causing cytotoxicity...
November 28, 2016: Macromolecular Bioscience
https://www.readbyqxmd.com/read/27892461/liver-specific-atp-citrate-lyase-inhibition-by-bempedoic-acid-decreases-ldl-c-and-attenuates-atherosclerosis
#7
Stephen L Pinkosky, Roger S Newton, Emily A Day, Rebecca J Ford, Sarka Lhotak, Richard C Austin, Carolyn M Birch, Brennan K Smith, Sergey Filippov, Pieter H E Groot, Gregory R Steinberg, Narendra D Lalwani
Despite widespread use of statins to reduce low-density lipoprotein cholesterol (LDL-C) and associated atherosclerotic cardiovascular risk, many patients do not achieve sufficient LDL-C lowering due to muscle-related side effects, indicating novel treatment strategies are required. Bempedoic acid (ETC-1002) is a small molecule intended to lower LDL-C in hypercholesterolemic patients, and has been previously shown to modulate both ATP-citrate lyase (ACL) and AMP-activated protein kinase (AMPK) activity in rodents...
November 28, 2016: Nature Communications
https://www.readbyqxmd.com/read/27888572/adverse-effect-profile-of-topical-ocular-administration-of-fingolimod-for-treatment-of-dry-eye-disease
#8
Weibao Xiao, Li Sun, Nan Zhang, Wen Ye
Fingolimod is a promising prodrug in attenuating multiple sclerosis and prolonging survival of organ allograft, with many other protective effects. Its mechanism of action is related to the internalization of sphingosine 1-phosphate receptors (S1PRs). Our previous study indicated that fingolimod eyedrop was efficacious in inhibiting ocular inflammation in a dry eye disease (DED) model of Non-Obese Diabetic (NOD) mice. In the current study, we evaluated potential adverse effects of fingolimod eyedrop. Inbred 10-week-old BALB/C mice were randomly divided into four groups, fingolimod-treated groups at three different concentrations (0...
November 26, 2016: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/27886551/reconsidering-azobenzene-as-a-component-of-small-molecule-hypoxia-mediated-cancer-drugs-a-theranostic-case-study
#9
Peter Verwilst, Jiyou Han, Jiyeong Lee, Sora Mun, Hee-Gyoo Kang, Jong Seung Kim
An azobenzene scaffold serves as both a fluorescence quencher and nitrogen mustard deactivator in a mitochondrial targeting unit bearing theranostic drug delivery system (DDS). The DDS exhibited a tissue selectivity for tumors with aggressive phenotypes, and the efficient in vitro and in vivo azoreduction under hypoxia conditions resulted in bright fluorescence at the tumor site as well as the in situ activation of the prodrug. In vivo therapeutic experiments demonstrated a significant reduction in tumor growth versus number of controls and ex vivo tissue analysis confirmed tissue normalization with strongly reduced angiogenic markers and suppressed cell proliferation...
November 16, 2016: Biomaterials
https://www.readbyqxmd.com/read/27886301/palladium-mediated-in-situ-synthesis-of-an-anticancer-agent
#10
Eugenio Indrigo, Jessica Clavadetscher, Sunay V Chankeshwara, Annamaria Lilienkampf, Mark Bradley
As a novel prodrug activation strategy Pd(0) nanoparticles, entrapped within a modular polymeric support, were used in cell culture, to synthesise the anticancer agent PP-121 from two non-toxic precursors, thereby inducing cell death in the first example of in situ mediated drug synthesis.
November 25, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27886300/a-three-dimensional-graphene-oxide-supramolecular-hydrogel-for-infrared-light-responsive-cascade-release-of-two-anticancer-drugs
#11
Wei Ha, Xiao-Bo Zhao, Kan Jiang, Yang Kang, Juan Chen, Bang-Jing Li, Yan-Ping Shi
A three dimensional supramolecular hydrogel consisting of prodrug-modified graphene oxide and α-cyclodextrin was developed. This hydrogel with a well-ordered interior microstructure integrated hydrophobic and hydrophilic anticancer drugs into a single multifunctional platform, and underwent a gel-sol transition leading to cascade release of two drugs in an on-demand fashion upon NIR light irradiation.
November 25, 2016: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/27884641/nanoparticle-delivery-of-chemotherapy-combination-regimen-improves-the-therapeutic-efficacy-in-mouse-models-of-lung-cancer
#12
Jing Tian, Zachary Rodgers, Yuanzeng Min, Xiaomeng Wan, Hui Qiu, Yu Mi, Xi Tian, Kyle T Wagner, Joseph M Caster, Yanfei Qi, Kyle Roche, Tian Zhang, Jianjun Cheng, Andrew Z Wang
The combination chemotherapy regimen of cisplatin (CP) and docetaxel (DTX) is effective against a variety of cancers. However, combination therapies present unique challenges that can complicate clinical application, such as increases in toxicity and imprecise exposure of tumors to specific drug ratios that can produce treatment resistance. Drug co-encapsulation within a single nanoparticle (NP) formulation can overcome these challenges and further improve combinations' therapeutic index. In this report, we employ a CP prodrug (CPP) strategy to formulate poly(lactic-co-glycolic acid)-poly(ethylene glycol) (PLGA-PEG) NPs carrying both CPP and DTX...
November 21, 2016: Nanomedicine: Nanotechnology, Biology, and Medicine
https://www.readbyqxmd.com/read/27883931/disassembly-of-amphiphilic-small-molecular-prodrug-with-fluorescence-switch-induced-by-ph-and-folic-acid-receptors-for-targeted-delivery-and-controlled-release
#13
Zhigang Xu, Xiaoxiao Shi, Meili Hou, Peng Xue, Yong-E Gao, Shiying Liu, Yuejun Kang
We develop a new type of pH-responsive amphiphilic small molecular prodrug by conjugating folic acid with anti-tumour doxorubicin via a hydrazone bond. This prodrug is featured by high and precise drug loading (55.4wt%), which can self-assemble into micellar nanoparticles in neutral environment while disassemble in the presence of tumour cells expressing folic acid receptors or the acidic tumoral endosomal environment. The prodrug nanoparticles can effectively improve anticancer efficacy due to the features of pH-triggered drug release and targeted delivery...
November 17, 2016: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/27883129/platinum-complexes-as-light-promoted-anticancer-agents-a-redefined-strategy-for-controlled-activation
#14
Koushambi Mitra
Site-specific delivery and amenable activation of prodrugs are indispensible criteria for designing novel anticancer agents. Platinum based drugs vanguard the chemotherapeutic regimes and over the years significant attention has been paid to achieve more efficacious drugs with fewer adverse effects. The switch from platinum(ii) drugs to the inert platinum(iv) analogues proved advantageous but the new prodrugs still suffered from unspecific cytotoxic actions. Thus the photoactivation of an inert platinum prodrug specifically within neoplastic cells provided the desired spatio-temporal control over drug activation by means of illumination, thereby limiting the cytotoxic events to only at the targeted tumors...
November 24, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/27882656/targeting-cancer-with-pcpa-drug-conjugates-lsd1-inhibition-triggered-release-of-4-hydroxytamoxifen
#15
Yosuke Ota, Yukihiro Itoh, Asako Kaise, Kiminori Ohta, Yasuyuki Endo, Mitsuharu Masuda, Yoshihiro Sowa, Toshiyuki Sakai, Takayoshi Suzuki
Targeting cancer with small molecule prodrugs should help overcome problems associated with conventional cancer-targeting methods. Herein, we focused on lysine-specific demethylase 1 (LSD1) to trigger the controlled release of anticancer drugs in cancer cells, where LSD1 is highly expressed. Conjugates of the LSD1 inhibitor trans-2-phenylcyclopropylamine (PCPA) were used as novel prodrugs to selectively release anticancer drugs by LSD1 inhibition. As PCPA-drug conjugate (PDC) prototypes, we designed PCPA-tamoxifen conjugates 1 a and 1 b, which released 4-hydroxytamoxifen in the presence of LSD1 in vitro...
November 24, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27879193/pharmacokinetic-comparison-of-two-formulations-of-talniflumate-370%C3%A2-mg-tablets-in-healthy-korean-volunteers%C3%A2
#16
Yun Kim, Sung- Yim, Bo-Hyung Kim, SeungHwan Lee
BACKGROUND: Talniflumate, a prodrug of niflumic acid, is a potent analgesic and anti-inflammatory drug that has been widely used for the treatment of rheumatoid diseases. OBJECTIVE: The aim of this study was to compare the pharmacokinetics and to evaluate the bioequivalence of two formulations of talniflumate 370 mg tablets (test formulation: Flumagen® 370 mg tablet; reference formulation: Somalgen® 370 mg tablet). METHODS: A randomized, open-label, single dose, two-sequence, two-period crossover clinical study was conducted...
November 23, 2016: International Journal of Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27879021/click-and-release-a-chemical-strategy-toward-developing-gasotransmitter-prodrugs-by-using-an-intramolecular-diels-alder-reaction
#17
Xingyue Ji, Cheng Zhou, Kaili Ji, Robert E Aghoghovbia, Zhixiang Pan, Vayou Chittavong, Bowen Ke, Binghe Wang
Prodrug strategies have been proven to be a very effective way of addressing delivery problems. Much of the chemistry in prodrug development relies on the ability to mask an appropriate functional group, which can be removed under appropriate conditions. However, developing organic prodrugs of gasotransmitters represent unique challenges. This is especially true with carbon monoxide, which does not have an easy "handle" for bioreversible derivatization. By taking advantage of an intramolecular Diels-Alder reaction, we have developed a prodrug strategy for preparations of organic CO prodrugs that are stable during synthesis and storage, and yet readily release CO with tunable release rates under near physiological conditions...
November 23, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27876476/studies-relating-to-the-synthesis-enzymatic-reduction-and-cytotoxicity-of-a-series-of-nitroaromatic-prodrugs
#18
Philip J Burke, Lai Chun Wong, Terence C Jenkins, Richard J Knox, Ian T Meikle, Stephen P Stanforth
A series of N-nitroarylated-3-chloromethyl-1,2,3,4-tetrahydroisoquinoline derivatives, several of which also possessed a trifluoromethyl substituent, were prepared and assessed as potential nitroaromatic prodrugs. The enzymatic reduction of these compounds and their cytotoxicities were studied. The compounds were cytotoxic, but this is probably not related to their enzymatic reduction.
December 15, 2016: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/27873205/protein-protein-interaction-inhibitors-of-brca1-discovered-using-small-molecule-microarrays
#19
Zhenkun Na, Sijun Pan, Mahesh Uttamchandani, Shao Q Yao
Microarray screening technology has transformed the life sciences arena over the last decade. The platform is widely used in the area of mapping interaction networks, to molecular fingerprinting and small molecular inhibitor discovery. The technique has significantly impacted both basic and applied research. The microarray platform can likewise enable high-throughput screening and discovery of protein-protein interaction (PPI) inhibitors. Herein we demonstrate the application of microarray-guided PPI inhibitor discovery, using human BRCA1 as an example...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27872191/structural-and-biochemical-analyses-reveal-the-mechanism-of-glutathione-s-transferase-pi-1-inhibition-by-the-anti-cancer-compound-piperlongumine
#20
Wayne Harshbarger, Sudershan Gondi, Scott B Ficarro, John Hunter, Durga Udayakumar, Deepak Gurbani, William Singer, Yan Liu, Lianbo Li, Jarrod A Marto, Kenneth D Westover
Glutathione S-transferase pi 1 (GSTP1), is frequently overexpressed in cancerous tumors and is a putative target of the plant compound piperlongumine (PL), which contains two reactive olefins and inhibits proliferation in cancer cells but not normal cells. PL exposure of cancer cells results in increased reactive oxygen species and decreased glutathione (GSH). This data in tandem with other information led to the conclusion that PL inhibits GSTP1, which forms covalent bonds between GSH and various electrophilic compounds, through covalent adduct formation at PLs C7-C8 olefin, while PLs C2-C3 olefin was postulated to react with GSH...
November 21, 2016: Journal of Biological Chemistry
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