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Drug Design, Development and Therapy

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https://www.readbyqxmd.com/read/29785090/semen-brassicae-ameliorates-hepatic-fibrosis-by-regulating-transforming-growth-factor-%C3%AE-1-smad-nuclear-factor-%C3%AE%C2%BAb-and-akt-signaling-pathways-in-rats
#1
Si Cao, Baoping Zheng, Tao Chen, Xinfeng Chang, Bao Yin, Zhihua Huang, Ping Shuai, Limin Han
Purpose: There is no effective treatment for liver fibrosis, which is a common phase during the progression of many chronic liver diseases to cirrhosis. Previous studies found that Semen Brassicae therapy can effectively improve the clinical symptoms of patients with asthma, allergic rhinitis, and chronic lung diseases; however, its effects on liver fibrosis in rats and its possible mechanisms of action remain unclear. Methods: Rats were injected intraperitoneally with 4% thioacetamide aqueous solution (5 mL·kg-1 ) at a dose of 200 mg·kg-1 twice a week for 8 consecutive weeks to establish the liver fibrosis model and were then treated with different concentrations of Semen Brassicae extract...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29785089/schisandrin-b-ameliorated-chondrocytes-inflammation-and-osteoarthritis-via-suppression-of-nf-%C3%AE%C2%BAb-and-mapk-signal-pathways
#2
Jisheng Ran, Chiyuan Ma, Kai Xu, Langhai Xu, Yuzhe He, Safwat Adel Abdo Moqbel, Pengfei Hu, Lifeng Jiang, Weiping Chen, Jiapeng Bao, Yan Xiong, Lidong Wu
Introduction: Osteoarthritis (OA) is the most prevalent joint disorder in the elderly population, and inflammatory mediators like IL-1β were thought to play central roles in its development. Schisandrin B, the main active component derived from Schisandra chinensis , exhibited anti-oxidative and antiinflammatory properties. Methods: In the present study, the protective effect and the underlying mechanism of Schisan-drin B on OA was investigated in vivo and in vitro...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29785088/insight-into-resistance-mechanism-of-anaplastic-lymphoma-kinase-to-alectinib-and-jh-viii-157-02-caused-by-g1202r-solvent-front-mutation
#3
Han Wang, Yao Wang, Wentao Guo, Bin Du, Xiaobing Huang, Riping Wu, Baoyu Yang, Xiaoyan Lin, Yilan Wu
Background: Mutated anaplastic lymphoma kinase (ALK) drives the development of advanced non-small cell lung cancer (NSCLC). Most reported small-molecule inhibitors targeting the ALK domain do not display good inhibition of the G1202R solvent front mutation. The solvent front mutation was assumed to hinder drug binding. However, a different fact could be uncovered by the simulations reported in this study through a structural analog of alectinib (JH-VIII-157-02), which demonstrated potent effects against the G1202R mutation...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29780238/update-on-new-biologics-for-intractable-eosinophilic-asthma-impact-of-reslizumab
#4
REVIEW
Jagdeep Sahota, Douglas S Robinson
A small percentage of patients with asthma have uncontrolled symptoms and frequent exacerbations, despite treatment with inhaled corticosteroids and other agents. It has become clear that different subtypes of this severe, treatment-resistant group exist due to different mechanisms of the disease. All such patients require detailed assessment in specialist centers to characterize the disease and assess treatment adherence. Recently, monoclonal antibodies have become available, which target specific pathways that may contribute to persistent inflammation and asthma exacerbations...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29780237/traditional-chinese-herbal-formula-relieves-snoring-by-modulating-activities-of-upper-airway-related-nerves-in-aged-rats
#5
Kou-Toung Chung, Chih-Hsiang Hsu, Ching-Lung Lin, Sheue-Er Wang, Chung-Hsin Wu
Aim: The present study investigated whether intraperitoneal treatment with the herbal formula B210 ([B210]; a herbal composition of Gastrodia elata and Cinnamomum cassia ) can reduce snoring in aged rats. Also, we studied possible neural mechanisms involved in B210 treatment and subsequent reduced snoring in rats. Methods and result: We compared pressure and frequency of snoring, activities of phrenic nerve (PNA), activities of recurrent laryngeal nerve (RLNA) and activities of hypoglossal nerve (HNA), inspiratory time (TI ) and expiratory time (TE ) of PNA, and pre-inspiratory time (Pre-TI ) of HNA in aged rats between sham and B210 treatment groups (30 mg/mL dissolved in DMSO)...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29780236/pharmacokinetic-comparison-of-a-fixed-dose-combination-versus-concomitant-administration-of-fimasartan-amlodipine-and-rosuvastatin-using-partial-replicated-design-in-healthy-adult-subjects
#6
Minkyung Oh, Jong-Lyul Ghim, Sung-Eun Park, Eun-Young Kim, Jae-Gook Shin
Objective: The aim of this study was to compare the pharmacokinetics (PK) and safety profiles of a fixed-dose combination (FDC) formulation of fimasartan, amlodipine, and rosuvastatin with the co-administration of the two products by using a replicated crossover study design in healthy male subjects. Results: This was an open-label, randomized, three-sequence, three-period replicated crossover study in healthy male subjects. The replicated crossover design was done because of high coefficient of variation of PK parameter for fimasartan, that is, >30%...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29780235/the-cytochrome-p450-isoenzyme-and-some-new-opportunities-for-the-prediction-of-negative-drug-interaction-in-vivo
#7
REVIEW
Dmitrij A Sychev, Ghulam Md Ashraf, Andrey A Svistunov, Maksim L Maksimov, Vadim V Tarasov, Vladimir N Chubarev, Vitalij A Otdelenov, Natal'ja P Denisenko, George E Barreto, Gjumrakch Aliev
Cytochrome (CYP) 450 isoenzymes are the basic enzymes involved in Phase I biotransformation. The most important role in biotransformation belongs to CYP3A4, CYP2D6, CYP2C9, CYP2C19 and CYP1A2. Inhibition and induction of CYP isoenzymes caused by drugs are important and clinically relevant pharmacokinetic mechanisms of drug interaction. Investigation of the activity of CYP isoenzymes by using phenotyping methods (such as the determination of the concentration of specific substrates and metabolites in biological fluids) during drug administration provides the prediction of negative side effects caused by drug interaction...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29765203/identification-of-novel-drug-targets-in-bovine-respiratory-disease-an-essential-step-in-applying-biotechnologic-techniques-to-develop-more-effective-therapeutic-treatments
#8
Meena Kishore Sakharkar, Karthic Rajamanickam, Ramesh Chandra, Haseeb A Khan, Abdullah S Alhomida, Jian Yang
Background: Bovine Respiratory Disease (BRD) is a major problem in cattle production which causes substantial economic loss. BRD has multifactorial aetiologies, is multi-microbial, and several of the causative pathogens are unknown. Consequently, primary management practices such as metaphylactic antimicrobial injections for BRD prevention are used to reduce the incidence of BRD in feedlot cattle. However, this poses a serious threat in the form of development of antimicrobial resistance and demands an urgent need to find novel interventions that could reduce the effects of BRD drastically and also delay/prevent bacterial resistance...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29765202/inhibition-of-human-prostate-cancer-pc-3-cells-and-targeting-of-pc-3-derived-prostate-cancer-stem-cells-with-koenimbin-a-natural-dietary-compound-from-murraya-koenigii-l-spreng
#9
Behnam Kamalidehghan, Soudeh Ghafouri-Fard, Elahe Motevaseli, Fatemeh Ahmadipour
Background: Inhibition of prostate cancer stem cells (PCSCs) is an efficient curative maintenance protocol for the prevention of prostate cancer. The objectives of this study were to assess the efficiency of koenimbin, a major biologically active component of Murraya koenigii (L) Spreng, in the suppression of PC-3 cells and to target PC-3-derived cancer stem cells (CSCs) through apoptotic and CSC signaling pathways in vitro. Materials and methods: The antiproliferative activity of koenimbin was examined using MTT, and the apoptotic detection was carried out by acridine orange/propidium iodide (AO/PI) double-staining and multiparametric high-content screening (HCS) assays...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29765201/deposition-and-transport-of-linezolid-mediated-by-a-synthetic-surfactant-synsurf-%C3%A2-within-a-pressurized-metered-dose-inhaler-a-calu-3-model
#10
Lyné van Rensburg, Johann M van Zyl, Johan Smith
Background: Previous studies in our laboratory demonstrated that a synthetic peptide containing lung surfactant enhances the permeability of chemical compounds through bronchial epithelium. The purpose of this study was to test two formulations of Synsurf® combined with linezolid as respirable compounds using a pressurized metered dose inhaler (pMDI). Methods: Aerosolization efficiency of the surfactant-drug microparticles onto Calu-3 monolayers as an air interface culture was analyzed using a Next Generation Impactor™...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29765200/efficacy-and-safety-of-the-crth2-antagonist-azd1981-as-add-on-therapy-to-inhaled-corticosteroids-and-long-acting-%C3%AE-2-agonists-in-patients-with-atopic-asthma
#11
Eric D Bateman, Christopher O'Brien, Paul Rugman, Sally Luke, Stefan Ivanov, Mohib Uddin
Objectives: To evaluate the efficacy and safety of AZD1981, a potent, specific antagonist of the CRTh2 receptor, as add-on therapy to inhaled corticosteroids (ICS) and long-acting β2 -agonists (LABA), in patients with persistent asthma with an allergic component. Patients and methods: In this placebo-controlled, parallel-group Phase IIb study, patients with persistent atopic asthma on ICS and LABA were randomized to receive 12 weeks of treatment with placebo or AZD1981 (80 mg daily, 200 mg daily, and 10 mg, 40 mg, 100 mg, or 400 mg twice daily [BID])...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29760547/comparison-of-the-effects-of-deferasirox-deferoxamine-and-combination-of-deferasirox-and-deferoxamine-on-an-aplastic-anemia-mouse-model-complicated-with-iron-overload
#12
Dijiong Wu, Xiaowen Wen, Wenbin Liu, Huijin Hu, Baodong Ye, Yuhong Zhou
Background and aim: Iron overload is commonly observed during the course of aplastic anemia (AA), which is believed to aggravate hematopoiesis, cause multiple organ dysfunction, lead to disease progression, and impair quality of life. Deferasirox (DFX) and deferoxamine (DFO) are among the most common iron chelation agents available in the clinical setting. The aim of this study was to investigate if the combination therapy with DFX and DFO is superior in hematopoietic recovery and iron chelation...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750019/identification-of-mycobacterium-tuberculosis-bioa-inhibitors-by-using-structure-based-virtual-screening
#13
Swati Singh, Garima Khare, Ritika Kar Bahal, Prahlad C Ghosh, Anil K Tyagi
Background: 7,8-Diaminopelargonic acid synthase (BioA), an enzyme of biotin biosynthesis pathway, is a well-known promising target for anti-tubercular drug development. Methods: In this study, structure-based virtual screening was employed against the active site of BioA to identify new chemical entities for BioA inhibition and top ranking compounds were evaluated for their ability to inhibit BioA enzymatic activity. Results: Seven compounds inhibited BioA enzymatic activity by greater than 60% at 100 μg/mL with most potent compounds being A36, A35 and A65, displaying IC50 values of 10...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750018/inactivation-of-nuclear-factor-%C3%AE%C2%BAb-by-mip-based-drug-combinations-augments-cell-death-of-breast-cancer-cells
#14
Menaga Subramaniam, Su Ki Liew, Lionel LA In, Khalijah Awang, Niyaz Ahmed, Noor Hasima Nagoor
Background: Drug combination therapy to treat cancer is a strategic approach to increase successful treatment rate. Optimizing combination regimens is vital to increase therapeutic efficacy with minimal side effects. Materials and methods: In the present study, we evaluated the in vitro cytotoxicity of double and triple combinations consisting of 1'S-1'-acetoxychavicol acetate (ACA), Mycobacterium indicus pranii (MIP) and cisplatin (CDDP) against 14 various human cancer cell lines to address the need for more effective therapy...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750017/pharmacokinetic-characteristics-of-telaprevir-in-healthy-korean-male-subjects-and-comparisons-with-japanese
#15
Yewon Choi, Seonghae Yoon, Kyoko Matsumoto, Yoshiyasu Ohta, SeungHwan Lee, Kyung-Sang Yu, In-Jin Jang
Introduction: Telaprevir, a reversible selective inhibitor of viral protease and a potential blocker of viral replication, is indicated for the treatment of hepatitis C virus genotype 1 infection. In this study, the pharmacokinetic profile, safety, and tolerability of telaprevir and the effect of food on telaprevir exposure were evaluated in healthy Korean subjects, and compared with data from a previous study in Japanese male subjects. Methods: The single ascending dose study was conducted in 3 dose-based groups (500, 750, and 1,250 mg, six subjects each) in a fasted state...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750016/spotlight-on-isavuconazole-in-the-treatment-of-invasive-aspergillosis-and-mucormycosis-design-development-and-place-in-therapy
#16
REVIEW
Jeffrey D Jenks, Helmut Jf Salzer, Juergen Prattes, Robert Krause, Dieter Buchheidt, Martin Hoenigl
In recent decades, important advances have been made in the diagnosis and treatment of invasive aspergillosis (IA) and mucormycosis. One of these advances has been the introduction of isavuconazole, a second-generation broad spectrum triazole with a favorable pharmacokinetic and safety profile and few drug-drug interactions. Phase III trials in patients with IA and mucormycosis demonstrated that isavuconazole has similar efficacy to voriconazole for the treatment of IA (SECURE trial) and liposomal amphotericin B for the treatment of mucormycosis (VITAL trial with subsequent case-control analysis) and a favorable safety profile with significantly fewer ocular, hepatobiliary, and skin and soft tissue adverse events compared to voriconazole...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750015/symmetric-dimeric-adamantanes-for-exploring-the-structure-of-two-viroporins-influenza-virus-m2-and-hepatitis-c-virus-p7
#17
Yasmine M Mandour, Ulrike Breitinger, Chunlong Ma, Jun Wang, Frank M Boeckler, Hans-Georg Breitinger, Darius P Zlotos
Background: Adamantane-based compounds have been identified to interfere with the ion-channel activity of viroporins and thereby inhibit viral infection. To better understand the difference in the inhibition mechanism of viroporins, we synthesized symmetric dimeric adamantane analogs of various alkyl-spacer lengths. Methods: Symmetric dimeric adamantane derivatives were synthesized where two amantadine or rimantadine molecules were linked by various alkyl-spacers...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29750014/advances-in-the-drug-therapies-of-acute-myeloid-leukemia-except-acute-wpromyelocytic-leukemia
#18
REVIEW
Min Lin, Baoan Chen
Acute myeloid leukemia (AML) is a heterogeneous hematologic malignancy, characterized by the clonal expansion of myeloid blasts in the peripheral blood, bone marrow, and/or other tissues. The new drugs used for treating AML are facing a big challenge, and the candidates include cytotoxic drugs, targeted small-molecule inhibitors, and monoclonal antibodies. In recent years, active research has focused on several new agents for including them in the large antileukemic drug family. This review aims to introduce some of these new drugs and highlights new advances made in the old drugs, mainly in the last 5 years...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29731607/4-amino-2-trifluoromethyl-phenyl-retinate-inhibits-proliferation-invasion-and-migration-of-breast-cancer-cells-by-independently-regulating-crabp2-and-fabp5
#19
Jing Ju, Nan Wang, Jiali Wang, Fanrong Wu, Jinfang Ge, Feihu Chen
Background: 4-Amino-2-trifluoromethyl-phenyl retinate (ATPR), a novel retinoid derivative, inhibits proliferation and induces differentiation in many cancer cells. In this study, the inhibitory effects of ATPR on the proliferation, invasion, and migration of breast cancer (BC) cells, and the relationship between ATPR and the expression of the intracellular lipid-binding proteins CRABP2 and FABP5 were investigated. Methods: CRABP2 and FABP5 expression was evaluated in infiltrating breast-infiltrating ductal carcinoma(BIDC) and benign breast fibroma (BBF) by immunohistochemistry and in MCF-7, MDA-MB-231, MDA-MB-435, and MDA-MB-453 cells by immunofluorescence...
2018: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29731606/clickable-prodrugs-bearing-potent-and-hydrolytically-cleavable-nicotinamide-phosphoribosyltransferase-inhibitors
#20
Keivan Sadrerafi, Emilia O Mason, Mark W Lee
Purpose: Our previous study indicated that carborane containing small-molecule 1-(hydroxymethyl)-7-(4'-( trans -3″-(3'″-pyridyl)acrylamido)butyl)-1,7-dicarbadodecaborane (hm-MC4-PPEA), was a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt). Nampt has been shown to be upregulated in most cancers and is a promising target for the treatment of many different types of cancers, including breast cancers. Patients and methods: To increase the selectivity of hm-MC4-PPEA toward cancer cells, three prodrugs were synthesized with different hydrolyzable linkers: ester, carbonate, and carbamate...
2018: Drug Design, Development and Therapy
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