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Drug repurposing

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https://www.readbyqxmd.com/read/28218840/drug-repurposing-of-histone-deacetylase-inhibitors-that-alleviate-neutrophilic-inflammation-in-acute-lung-injury-and-idiopathic-pulmonary-fibrosis-via-inhibiting-leukotriene-a4-hydrolase-and-blocking-ltb4-biosynthesis
#1
Weiqiang Lu, Xue Yao, Ping Ouyang, Ningning Dong, Dang Wu, Xingwu Jiang, Zengrui Wu, Chen Zhang, Zhongyu Xu, Yun Tang, Shien Zou, Mingyao Liu, Jian Li, Ming-Hua Zeng, Ping Lin, Feixiong Cheng, Jin Huang
Acute lung injury (ALI) and idiopathic pulmonary fibrosis (IPF) are both serious public health problems with high incidence and mortality rate in adults, and with few drugs available for the efficient treatment in clinic. In this study, we identified that two known histone deacetylase (HDAC) inhibitors, suberanilohydroxamic acid (SAHA, 1) and its analog 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide (2), are effective inhibitors of Leukotriene A4 hydrolase (LTA4H), a key enzyme in the biosynthesis of leukotriene B4 (LTB4), across a panel of 18 HDAC inhibitors, using enzymatic assay, thermofluor assay, and X-ray Crystallographic investigation...
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28215999/rat-animal-models-for-screening-medications-to-treat-alcohol-use-disorders
#2
REVIEW
Richard L Bell, Sheketha R Hauser, Tiebing Liang, Youssef Sari, Antoinette Maldonado-Devincci, Zachary A Rodd
The purpose of this review is to present animal research models that can be used to screen and/or repurpose medications for the treatment of alcohol abuse and dependence. The focus will be on rats and in particular selectively bred rats. Brief introductions discuss various aspects of the clinical picture, which provide characteristics of individuals with alcohol use disorders (AUDs) to model in animals. Following this, multiple selectively bred rat lines will be described and evaluated in the context of animal models used to screen medications to treat AUDs...
February 16, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28212175/advances-in-epilepsy-gene-discovery-and-implications-for-epilepsy-diagnosis-and-treatment
#3
Joseph D Symonds, Sameer M Zuberi, Michael R Johnson
PURPOSE OF REVIEW: Epilepsy genetics is shifting from the academic pursuit of gene discovery to a clinical discipline based on molecular diagnosis and stratified medicine. We consider the latest developments in epilepsy genetics and review how gene discovery in epilepsy is influencing the clinical classification of epilepsy and informing new therapeutic approaches and drug discovery. RECENT FINDINGS: Recent studies highlighting the importance of mutation in GABA receptors, NMDA receptors, potassium channels, G-protein coupled receptors, mammalian target of rapamycin pathway and chromatin remodeling are discussed...
February 15, 2017: Current Opinion in Neurology
https://www.readbyqxmd.com/read/28203090/exploring-targeted-therapy-of-osteosarcoma-using-proteomics-data
#4
Parunya Chaiyawat, Jongkolnee Settakorn, Apiruk Sangsin, Pimpisa Teeyakasem, Jeerawan Klangjorhor, Aungsumalee Soongkhaw, Dumnoensun Pruksakorn
Despite multimodal therapeutic treatments of osteosarcoma (OS), some patients develop resistance to currently available regimens and eventually end up with recurrent or metastatic outcomes. Many attempts have been made to discover effective drugs for improving outcome; however, due to the heterogeneity of the disease, new therapeutic options have not yet been identified. This study aims to explore potential targeted therapy related to protein profiles of OS. In this review of proteomics studies, we extracted data on differentially expressed proteins (DEPs) from archived literature in PubMed and our in-house repository...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28199182/one-reporter-for-in-cell-activity-profiling-of-majority-of-protein-kinase-oncogenes
#5
Iva Gudernova, Silvie Foldynova-Trantirkova, Barbora El Ghannamova, Bohumil Fafilek, Miroslav Varecha, Lukas Balek, Eva Hruba, Lucie Jonatova, Iva Jelinkova, Michaela Kunova Bosakova, Lukas Trantirek, Jiri Mayer, Pavel Krejci
In-cell profiling enables the evaluation of receptor tyrosine activity in a complex environment of regulatory networks that affect signal initiation, propagation and feedback. We used FGF-receptor signaling to identify EGR1 as a locus that strongly responds to the activation of a majority of the recognized protein kinase oncogenes, including 30 receptor tyrosine kinases and 154 of their disease-associated mutants. The EGR1 promoter was engineered to enhance trans-activation capacity and optimized for simple screening assays with luciferase or fluorescent reporters...
February 15, 2017: ELife
https://www.readbyqxmd.com/read/28198666/design-connecting-gene-expression-with-therapeutics-for-drug-repurposing-and-development
#6
Bernard Kok Bang Lee, Kai Hung Tiong, Jit Kang Chang, Chee Sun Liew, Zainal Ariff Abdul Rahman, Aik Choon Tan, Tsung Fei Khang, Sok Ching Cheong
BACKGROUND: The drug discovery and development pipeline is a long and arduous process that inevitably hampers rapid drug development. Therefore, strategies to improve the efficiency of drug development are urgently needed to enable effective drugs to enter the clinic. Precision medicine has demonstrated that genetic features of cancer cells can be used for predicting drug response, and emerging evidence suggest that gene-drug connections could be predicted more accurately by exploring the cumulative effects of many genes simultaneously...
January 25, 2017: BMC Genomics
https://www.readbyqxmd.com/read/28190396/in-vitro-screening-of-an-fda-approved-library-against-eskape-pathogens
#7
Waleed Younis, Ahmed AbdelKhalek, Abdelrahman S Mayhoub, Mohamed N Seleem
Bacterial resistance to conventional antibiotics is an increasingly serious threat to public health worldwide that requires immediate exploration and the development of novel antimicrobial compounds. Drug repurposing is an inexpensive and untapped source of new antimicrobial leads, and it holds many attractive features warranting further attention for antimicrobial drug discovery. In an effort to repurpose drugs and explore new leads in the field of antimicrobial drug discovery, we performed a whole-cell screening assay of 1,600 Food and Drug Administration (FDA) approved drugs against Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter cloacae (ESKAPE) pathogens...
February 9, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28185815/novel-antiviral-activity-and-mechanism-of-bromocriptine-as-a-zika-virus-ns2b-ns3-protease-inhibitor
#8
Jasper Fuk-Woo Chan, Kenn Ka-Heng Chik, Shuofeng Yuan, Cyril Chik-Yan Yip, Zheng Zhu, Kah-Meng Tee, Jessica Oi-Ling Tsang, Chris Chung-Sing Chan, Vincent Kwok-Man Poon, Gang Lu, Anna Jinxia Zhang, Kin-Kui Lai, Kwok-Hung Chan, Richard Yi-Tsun Kao, Kwok-Yung Yuen
Zika virus (ZIKV) infection is associated with congenital malformations in infected fetuses and severe neurological and other systemic complications in adults. There are currently limited anti-ZIKV treatment options that are readily available and safe for use in pregnancy. In this drug repurposing study, bromocriptine was found to have inhibitory effects on ZIKV replication in cytopathic effect inhibition, virus yield reduction, and plaque reduction assays. Time-of-drug-addition assay showed that bromocriptine exerted anti-ZIKV activity between 0 and 12 h post-ZIKV inoculation, corroborating with post-entry events in the virus replication cycle prior to budding...
February 7, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28182168/drugs-in-development-for-toxoplasmosis-advances-challenges-and-current-status
#9
REVIEW
P Holland Alday, Joseph Stone Doggett
Toxoplasma gondii causes fatal and debilitating brain and eye diseases. Medicines that are currently used to treat toxoplasmosis commonly have toxic side effects and require prolonged courses that range from weeks to more than a year. The need for long treatment durations and the risk of relapsing disease are in part due to the lack of efficacy against T. gondii tissue cysts. The challenges for developing a more effective treatment for toxoplasmosis include decreasing toxicity, achieving therapeutic concentrations in the brain and eye, shortening duration, eliminating tissue cysts from the host, safety in pregnancy, and creating a formulation that is inexpensive and practical for use in resource-poor areas of the world...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28170199/concise-review-cell-surface-n-linked-glycoproteins-as-potential-stem-cell-markers-and-drug-targets
#10
Kenneth R Boheler, Rebekah L Gundry
Stem cells and their derivatives hold great promise to advance regenerative medicine. Critical to the progression of this field is the identification and utilization of antibody-accessible cell-surface proteins for immunophenotyping and cell sorting-techniques essential for assessment and isolation of defined cell populations with known functional and therapeutic properties. Beyond their utility for cell identification and selection, cell-surface proteins are also major targets for pharmacological intervention...
January 2017: Stem Cells Translational Medicine
https://www.readbyqxmd.com/read/28167256/turning-the-tide-against-tuberculosis
#11
Nesri Padayatchi, Naressa Naidu, Gerald Friedland, Kasavan Naidoo, Francesca Conradie, Kogieleum Naidoo, Max Roe O'Donnell
Despite affecting men, women, and children for millennia, tuberculosis (TB) is the most neglected disease. In contrast, the global response to HIV has reached a defining moment. By uniting efforts, promptly integrating major scientific findings for both treatment and prevention, and scaling up services, the once inconceivable end to the HIV epidemic may no longer be an illusion. "The world has made defeating AIDS a top priority. This is a blessing. But TB remains ignored" - Nelson Mandela. While there is no doubt that revolutionary diagnostics and new and repurposed drugs have provided some hope in the fight against TB, it is evident that scientific advances on their own are inadequate to achieve the World Health Organization's ambitious goal to end TB by 2035...
February 4, 2017: International Journal of Infectious Diseases: IJID
https://www.readbyqxmd.com/read/28166637/computational-multi-target-drug-design
#12
Weilin Zhang, Jianfeng Pei, Luhua Lai
Designing drugs that can simultaneously interact with multiple targets is a promising approach for treating complicated diseases. Compared to using combinations of single target drugs, multi-target drugs have advantages of higher efficacy, improved safety profile, and simpler administration. Many in silico methods have been developed to approach different aspects of this polypharmacology-guided drug design, particularly for drug repurposing and multi-target drug design. In this review, we summarize recent progress in computational multi-target drug design and discuss their advantages and limitations...
February 6, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28163699/a-systematic-review-of-in-vitro-and-in-vivo-activities-of-anti-toxoplasma-drugs-and-compounds-2006-2016
#13
REVIEW
Mahbobeh Montazeri, Mehdi Sharif, Shahabeddin Sarvi, Saeed Mehrzadi, Ehsan Ahmadpour, Ahmad Daryani
The currently available anti-Toxoplasma agents have serious limitations. This systematic review was performed to evaluate drugs and new compounds used for the treatment of toxoplasmosis. Data was systematically collected from published papers on the efficacy of drugs/compounds used against Toxoplasma gondii (T. gondii) globally during 2006-2016. The searched databases were PubMed, Google Scholar, Science Direct, ISI Web of Science, EBSCO, and Scopus. One hundred and eighteen papers were eligible for inclusion in this systematic review, which were both in vitro and in vivo studies...
2017: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28159655/screening-a-repurposing-library-for-potentiators-of-antibiotics-against-staphylococcus-aureus-biofilms
#14
Freija Van den Driessche, Gilles Brackman, Rosalie Swimberghe, Petra Rigole, Tom Coenye
Staphylococcus aureus biofilms are involved in a wide range of infections that are extremely difficult to treat with conventional antibiotic therapy. We aimed to identify potentiators of antibiotics against mature biofilms of S. aureus Mu50, a methicillin-resistant and vancomycin-intermediate-resistant strain. Over 700 off-patent drugs from a repurposing library were screened in combination with vancomycin in a microtitre plate (MTP)-based biofilm model system. This led to the identification of 25 hit compounds, including four phenothiazines among which thioridazine was the most potent...
January 31, 2017: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/28157711/the-repurposed-anthelmintic-mebendazole-in-combination-with-trametinib-suppresses-refractory-nrasq61k-melanoma
#15
Cynthia M Simbulan-Rosenthal, Sivanesan Dakshanamurthy, Anirudh Gaur, You-Shin Chen, Hong-Bin Fang, Maryam Abdussamad, Hengbo Zhou, John Zapas, Valerie Calvert, Emanuel F Petricoin, Michael B Atkins, Stephen W Byers, Dean S Rosenthal
Structure-based drug repositioning in addition to random chemical screening is now a viable route to rapid drug development. Proteochemometric computational methods coupled with kinase assays showed that mebendazole (MBZ) binds and inhibits kinases important in cancer, especially both BRAFWT and BRAFV600E. We find that MBZ synergizes with the MEK inhibitor trametinib to inhibit growth of BRAFWT-NRASQ61K melanoma cells in culture and in xenografts, and markedly decreased MEK and ERK phosphorylation. Reverse Phase Protein Array (RPPA) and immunoblot analyses show that both trametinib and MBZ inhibit the MAPK pathway, and cluster analysis revealed a protein cluster showing strong MBZ+trametinib - inhibited phosphorylation of MEK and ERK within 10 minutes, and its direct and indirect downstream targets related to stress response and translation, including ElK1 and RSKs within 30 minutes...
February 2, 2017: Oncotarget
https://www.readbyqxmd.com/read/28155912/repurposing-doxycycline-for-synucleinopathies-remodelling-of-%C3%AE-synuclein-oligomers-towards-non-toxic-parallel-beta-sheet-structured-species
#16
Florencia González-Lizárraga, Sergio B Socías, César L Ávila, Clarisa M Torres-Bugeau, Leandro R S Barbosa, Andres Binolfi, Julia E Sepúlveda-Díaz, Elaine Del-Bel, Claudio O Fernandez, Dulce Papy-Garcia, Rosangela Itri, Rita Raisman-Vozari, Rosana N Chehín
Synucleinophaties are progressive neurodegenerative disorders with no cure to date. An attractive strategy to tackle this problem is repurposing already tested safe drugs against novel targets. In this way, doxycycline prevents neurodegeneration in Parkinson models by modulating neuroinflammation. However, anti-inflammatory therapy per se is insufficient to account for neuroprotection. Herein we characterise novel targets of doxycycline describing the structural background supporting its effectiveness as a neuroprotector at subantibiotic doses...
February 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28155663/scmbyk-prediction-and-characterization-of-bacterial-tyrosine-kinases-based-on-propensity-scores-of-dipeptides
#17
Tamara Vasylenko, Yi-Fan Liou, Po-Chin Chiou, Hsiao-Wei Chu, Yung-Sung Lai, Yu-Ling Chou, Hui-Ling Huang, Shinn-Ying Ho
BACKGROUND: Bacterial tyrosine-kinases (BY-kinases), which play an important role in numerous cellular processes, are characterized as a separate class of enzymes and share no structural similarity with their eukaryotic counterparts. However, in silico methods for predicting BY-kinases have not been developed yet. Since these enzymes are involved in key regulatory processes, and are promising targets for anti-bacterial drug design, it is desirable to develop a simple and easily interpretable predictor to gain new insights into bacterial tyrosine phosphorylation...
December 22, 2016: BMC Bioinformatics
https://www.readbyqxmd.com/read/28150521/drug-repurposing-and-therapeutic-anti-microrna-predictions-for-inhibition-of-oxidized-low-density-lipoprotein-induced-vascular-smooth-muscle-cell-associated-diseases
#18
Shun-Tsung Chen, Chien-Hung Huang, Victor C Kok, Chi-Ying F Huang, Jin-Shuei Ciou, Jeffrey J P Tsai, Nilubon Kurubanjerdjit, Ka-Lok Ng
Drug repurposing is a new method for disease treatments, which accelerates the identification of new uses for existing drugs with minimal side effects for patients. MicroRNA-based therapeutics are a class of drugs that have been used in gene therapy following the FDA's approval of the first anti-sense therapy. This study examines the effects of oxLDL on vascular smooth muscle cells (VSMCs) and identifies potential drugs and antimiRs for treating VSMC-associated diseases. The Connectivity Map (cMap) database is utilized to identify potential new uses of existing drugs...
December 22, 2016: Journal of Bioinformatics and Computational Biology
https://www.readbyqxmd.com/read/28149831/repurposing-approach-identifies-auranofin-with-broad-spectrum-antifungal-activity-that-targets-mia40-erv1-pathway
#19
Shankar Thangamani, Matthew Maland, Haroon Mohammad, Pete E Pascuzzi, Larisa Avramova, Carla M Koehler, Tony R Hazbun, Mohamed N Seleem
Current antifungal therapies have limited effectiveness in treating invasive fungal infections. Furthermore, the development of new antifungal is currently unable to keep pace with the urgent demand for safe and effective new drugs. Auranofin, an FDA-approved drug for the treatment of rheumatoid arthritis, inhibits growth of a diverse array of clinical isolates of fungi and represents a new antifungal agent with a previously unexploited mechanism of action. In addition to auranofin's potent antifungal activity against planktonic fungi, this drug significantly reduces the metabolic activity of Candida cells encased in a biofilm...
2017: Frontiers in Cellular and Infection Microbiology
https://www.readbyqxmd.com/read/28137938/repurposing-an-old-drug-aztreonam-as-a-new-treatment-strategy-for-gonorrhoea
#20
Benjamin Davido, Aurelien Dinh, Olivia Senard, Ruxandra Calin, Sabrina Makhloufi, Jerome Salomon
OBJECTIVES: To determine whether aztreonam is still an effective drug for the treatment of gonorrhoea. METHODS: Observational study of patients with gonorrhoea diagnosed by urine multiplex PCR, with a past medical history of allergy to β-lactams or relapse after treatment with a third-generation cephalosporin. Patients received a single 1 g dose of aztreonam in accordance with the manufacturer's instructions. RESULTS: Five patients (four males, one female) were enrolled, comprising two who were allergic to β-lactams and three previously treated with cephalosporins who relapsed...
January 30, 2017: Journal of Antimicrobial Chemotherapy
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