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ethambutol AND mechanism of action

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https://www.readbyqxmd.com/read/26887318/screening-of-antitubercular-compound-library-identifies-novel-shikimate-kinase-inhibitors-of-mycobacterium-tuberculosis
#1
Vikrant S Rajput, Rukmankesh Mehra, Sanjay Kumar, Amit Nargotra, Parvinder Pal Singh, Inshad Ali Khan
Shikimate kinase of Mycobacterium tuberculosis is involved in the biosynthesis of aromatic amino acids through shikimate pathway. The enzyme is essential for the survival of M. tuberculosis and is absent from mammals, thus providing an excellent opportunity for identifying new chemical entities to combat tuberculosis with a novel mechanism of action. In this study, an antitubercular library of 1000 compounds was screened against M. tuberculosis shikimate kinase (MtSK). This effort led to the identification of 20 inhibitors, among which five promising leads exhibited half maximal inhibitory concentration (IC50) values below 10 μM...
June 2016: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/26204816/new-treatment-strategies-for-pulmonary-sarcoidosis-antimetabolites-biological-drugs-and-other-treatment-approaches
#2
REVIEW
Robert P Baughman, Jan C Grutters
About half of patients with sarcoidosis will need systemic therapy for their disease. Oral glucocorticoids are the standard first-line treatment for sarcoidosis. With time, patients might develop substantial morbidity from long-term use of high doses of these drugs. We propose a step-wise approach to the management of pulmonary disease in sarcoidosis and provide details about how and when to use alternatives to glucocorticoids. The antimetabolites, such as methotrexate, azathioprine, leflunomide, and mycophenolate, are often used as alternatives to steroids...
October 2015: Lancet Respiratory Medicine
https://www.readbyqxmd.com/read/25877396/tuberculosis-drug-development-history-and-evolution-of-the-mechanism-based-paradigm
#3
REVIEW
Sumit Chakraborty, Kyu Y Rhee
Modern tuberculosis (TB) chemotherapy is widely viewed as a crowning triumph of anti-infectives research. However, only one new TB drug has entered clinical practice in the past 40 years while drug resistance threatens to further destabilize the pandemic. Here, we review a brief history of TB drug development, focusing on the evolution of mechanism(s)-of-action studies and key conceptual barriers to rational, mechanism-based drugs.
August 2015: Cold Spring Harbor Perspectives in Medicine
https://www.readbyqxmd.com/read/24965038/afm-resolves-effects-of-ethambutol-on-nanomechanics-and-nanostructures-of-single-dividing-mycobacteria-in-real-time
#4
Yangzhe Wu, Ronald C Sims, Anhong Zhou
Dynamic nanomechanics and nanostructures of dividing and anti-mycobacterial drug treated mycobacterium remain to be fully elucidated. Atomic force microscopy (AFM) is a promising nanotechnology tool for characterization of these dynamic alterations, especially at the single cell level. In this work, single dividing mycobacterium JLS (M.JLS) before and after anti-mycobacterial drug (ethambutol, EMB) treatment was in situ quantitatively analyzed, suggesting that nanomechanics would be referred as a sensitive indicator for evaluating efficacy of anti-mycobacterial drugs...
September 28, 2014: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/24268596/antimycobacterial-activity-of-nitrogen-heterocycles-derivatives-bipyridine-derivatives-part-iii
#5
Ramona Danac, Ionel I Mangalagiu
Three classes of fused bipyridine heterocycles were designed, synthesized and evaluated for their antimycobacterial activities. The method for preparation of fused bipyridine derivatives is straight and efficient. The primary antimycobacterial screening reveals that mono-indolizine mono-salts are displaying potency superior to the second-line antitubercular drugs Cycloserine and Pyrimethamine and, equal as the first line anti-TB Ethambutol. The data from Cycle-2 screening assay (MIC, MBC, LORA, intracellular (macrophage) drug screening, and MTT cell proliferation) confirm the promising anti-TB results from Cycle-1 for mono-indolizine mono-salts...
March 3, 2014: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/23127864/aorto-enteric-fistula-development-secondary-to-mycotic-abdominal-aortic-aneurysm-following-intravesical-bacillus-calmette-guerin-bcg-treatment-for-transitional-cell-carcinoma-of-the-bladder
#6
Anthony Roylance, John Mosley, Mohideen Jameel, Axel Sylvan, Virginie Walker
INTRODUCTION: Intravesical BCG-instillation for bladder cancer is considered safe but is not without risk. While most side-effects are localised and self-limiting, the development of secondary vascular pathology is a rare but significant complication. PRESENTATION OF CASE: A 77-year-old male presented with a mycotic abdominal aortic aneurysm and associated aorto-enteric fistula 18 months after receiving intravesical BCG-instillations for early stage transitional cell carcinoma...
2013: International Journal of Surgery Case Reports
https://www.readbyqxmd.com/read/20467231/development-of-new-anti-tuberculosis-drug-candidates
#7
REVIEW
Ruiru Shi, Isamu Sugawara
Mycobacterium tuberculosis, the causative agent of tuberculosis, is a tenacious and remarkably successful pathogen that has latently infected one third of the world's population, according to the World Health Organization (WHO) statistics. It is anticipated that 10% of these infected individuals will develop active tuberculosis at some point in their lifetime. The long-term use of the current drug regimen, the emergence of drug-resistant strains, and HIV co-infection have resulted in a resurgence of research efforts to address the urgent need for new anti-tuberculosis drugs...
June 2010: Tohoku Journal of Experimental Medicine
https://www.readbyqxmd.com/read/20133807/a-truncated-lipoglycan-from-mycobacteria-with-altered-immunological-properties
#8
Helen L Birch, Luke J Alderwick, Ben J Appelmelk, Janneke Maaskant, Apoorva Bhatt, Albel Singh, Jerome Nigou, Lothar Eggeling, Jeroen Geurtsen, Gurdyal S Besra
Maintenance of cell-wall integrity in Mycobacterium tuberculosis is essential and is the target of several antitubercular drugs. For example, ethambutol targets arabinogalactan and lipoarabinomannan (LAM) biosynthesis through the inhibition of several arabinofuranosyltransferases. Apart from their role in cell-wall integrity, mycobacterial LAMs also exhibit important immunomodulatory activities. Here we report the isolation and detailed structural characterization of a unique LAM molecule derived from Mycobacterium smegmatis deficient in the arabinofuranosyltransferase AftC (AftC-LAM)...
February 9, 2010: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/19492969/mycobacterium-tuberculosis-drug-resistance-and-future-perspectives
#9
REVIEW
Giovanna Riccardi, Maria Rosalia Pasca, Silvia Buroni
TB is still a global health problem. The selection and spread of multidrug-resistant and extensively drug-resistant Mycobacterium tuberculosis strains represents a threat for global TB control. The reappearance of TB has driven an increased interest in understanding the mechanisms of drug action and drug resistance, which could provide a significant contribution in the development of new antimicrobials. In this article, the authors describe the mode of action and the resistance mechanisms of the principal first- and second-line antitubercular agents, namely isoniazid, ethionamide, ethambutol, D-cycloserine, rifamycins, fluoroquinolones, streptomycin, linezolid and pyrazinamide...
June 2009: Future Microbiology
https://www.readbyqxmd.com/read/18647459/ethambutol-induced-optical-neuropathy-risk-of-overdosing-in-obese-subjects
#10
R E Hasenbosch, J W C Alffenaar, S A Koopmans, J G W Kosterink, T S van der Werf, R van Altena
BACKGROUND: Ethambutol (EMB) is one of the first-line drugs in the treatment against tuberculosis (TB). Side-effects are infrequent, but its main adverse effect, optical neuropathy, has long been recognised. The mechanisms of action and predisposing factors have not yet been fully understood. METHOD: We conducted a retrospective study (1992--2007) in an attempt to find predisposing factors for optical neuropathy. RESULTS: Visual disturbance was reported in 1...
August 2008: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/18631118/tuberculosis-a-balanced-diet-of-lipids-and-carbohydrates
#11
REVIEW
Veemal Bhowruth, Luke J Alderwick, Alistair K Brown, Apoorva Bhatt, Gurdyal S Besra
In spite of effective antibiotics to treat TB (tuberculosis) since the early 1960s, we enter the new millennium with TB currently the leading cause of death from a single infectious agent, killing more than 3 million people worldwide each year. Thus an understanding of drug-resistance mechanisms, the immunobiology of cell wall components to elucidate host-pathogen interactions and the discovery of new drug targets are now required for the treatment of TB. Above the plasma membrane is a classical chemotype IV peptidoglycan to which is attached the macromolecular structure, mycolyl-arabinogalactan via a unique diglycosylphosphoryl bridge...
August 2008: Biochemical Society Transactions
https://www.readbyqxmd.com/read/18556206/halicyclamine-a-a-marine-spongean-alkaloid-as-a-lead-for-anti-tuberculosis-agent
#12
Masayoshi Arai, Mari Sobou, Catherine Vilchéze, Anthony Baughn, Hiroyuki Hashizume, Patamaporn Pruksakorn, Shunsuke Ishida, Makoto Matsumoto, William R Jacobs, Motomasa Kobayashi
In the course of our search for anti-microbial agents against dormant Mycobacterium tuberculosis, halicyclamine A was re-discovered as a lead for anti-tuberculosis agent from a marine sponge of Haliclona sp. on the guidance of the constructed bioassay. Halicyclamine A showed growth inhibition against Mycobacterium smegmatis, Mycobacterium bovis BCG, and M. tuberculosis H37Ra with MICs in the range of 1.0-5.0microg/ml under both aerobic condition and hypoxic condition inducing dormant state. The growth-inhibitory activity of halicyclamine A was bactericidal, and halicyclamine A did not exhibit cross-resistance with the currently used anti-tuberculosis drugs of isoniazid, ethambutol, rifampicin, and streptomycin...
July 15, 2008: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/18217789/drug-induced-ocular-disorders
#13
REVIEW
Junping Li, Ramesh C Tripathi, Brenda J Tripathi
While beneficial therapeutically, almost all medications have untoward effects on various body tissues and functions, including the eye in which organ toxic reactions are readily detectable. Every part of the eye and all ocular functions could be affected adversely. In this review, we describe the most commonly recognized drug-induced ocular disorders, their specific clinical features, the medications that can cause the problem, the differential diagnosis and possible mechanisms of action, as well as guidelines for the management of the adverse reactions...
2008: Drug Safety: An International Journal of Medical Toxicology and Drug Experience
https://www.readbyqxmd.com/read/18043940/organization-of-the-mycobacterial-cell-wall-a-nanoscale-view
#14
David Alsteens, Claire Verbelen, Etienne Dague, Dominique Raze, Alain R Baulard, Yves F Dufrêne
The biosynthesis of the Mycobacterium tuberculosis cell wall is targeted by some of the most powerful antituberculous drugs. To date, the molecular mechanisms by which these antibiotics affect the cell wall characteristics are not well understood. Here, we used atomic force microscopy - in three different modes - to probe the nanoscale surface properties of live mycobacteria and their modifications upon incubation with four antimycobacterial drugs: isoniazid, ethionamide, ethambutol, and streptomycine. Topographic imaging, combined with quantitative surface roughness analysis, demonstrated that all drugs induce a substantial increase of surface roughness to an extent that correlates with the localization of the target (i...
April 2008: Pflügers Archiv: European Journal of Physiology
https://www.readbyqxmd.com/read/17956343/structure-function-and-biosynthesis-of-the-mycobacterium-tuberculosis-cell-wall-arabinogalactan-and-lipoarabinomannan-assembly-with-a-view-to-discovering-new-drug-targets
#15
REVIEW
L J Alderwick, H L Birch, A K Mishra, L Eggeling, G S Besra
In spite of effective antibiotics to treat TB (tuberculosis) since the early 1960s, we enter the new millennium with TB, currently the leading cause of death from a single infectious agent, killing more than three million people worldwide each year. Thus an understanding of drug-resistance mechanisms, the immunobiology of cell wall components to elucidate host-pathogen interactions and the discovery of new drug targets are now required for the treatment of TB. Above the plasma membrane is a classical chemotype IV PG (peptidoglycan) to which is attached the macromolecular structure, mycolyl-arabinogalactan, via a unique diglycosylphosphoryl bridge...
November 2007: Biochemical Society Transactions
https://www.readbyqxmd.com/read/17691942/novel-agents-in-the-management-of-mycobacterium-tuberculosis-disease
#16
REVIEW
P J Barry, T M O'Connor
The goals of tuberculosis control are to cure active disease, prevent relapse, reduce transmission and avert the emergence of drug resistance. However, since the 1960s, there have been few developments in available therapies. Currently available agents are complicated by numerous side-effects, drug interactions and the need for a long duration of therapy. Rifampicin-containing regimes lead to hepatic enzyme induction which can complicate or preclude the use of protease inhibitors and non-nucleoside reverse transcriptase inhibitors in patients infected with the human immunodeficiency virus...
2007: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/17590082/transcriptional-regulation-of-multi-drug-tolerance-and-antibiotic-induced-responses-by-the-histone-like-protein-lsr2-in-m-tuberculosis
#17
Roberto Colangeli, Danica Helb, Catherine Vilchèze, Manzour Hernando Hazbón, Chee-Gun Lee, Hassan Safi, Brendan Sayers, Irene Sardone, Marcus B Jones, Robert D Fleischmann, Scott N Peterson, William R Jacobs, David Alland
Multi-drug tolerance is a key phenotypic property that complicates the sterilization of mammals infected with Mycobacterium tuberculosis. Previous studies have established that iniBAC, an operon that confers multi-drug tolerance to M. bovis BCG through an associated pump-like activity, is induced by the antibiotics isoniazid (INH) and ethambutol (EMB). An improved understanding of the functional role of antibiotic-induced genes and the regulation of drug tolerance may be gained by studying the factors that regulate antibiotic-mediated gene expression...
June 2007: PLoS Pathogens
https://www.readbyqxmd.com/read/16129320/-resistance-to-antituberculous-drugs
#18
REVIEW
N Veziris, E Cambau, W Sougakoff, J Robert, V Jarlier
Mycobacteria responsible for tuberculosis (M. tuberculosis, M. bovis, M. africanum) are susceptible to a very small number of antibiotics. As soon as these drugs were used in humans all gave rise to the selection of resistant mycobacteria. Study of the mechanisms of acquired resistance, with the help of the genetics of mycobacteria, led to a more accurate understanding of the mode of action of antituberculous drugs. The antibiotics isoniazid, pyrazinamide, ethionamide and ethambutol are mycobacteria-specific because they inhibit the synthesis of mycolic acids, which are specific constituants of the bacterial wall...
August 2005: Archives de Pédiatrie: Organe Officiel de la Sociéte Française de Pédiatrie
https://www.readbyqxmd.com/read/16085758/pharmacoproteomic-effects-of-isoniazid-ethambutol-and-n-geranyl-n-2-adamantyl-ethane-1-2-diamine-sq109-on-mycobacterium-tuberculosis-h37rv
#19
Lee Jia, Lori Coward, Gregory S Gorman, Patricia E Noker, Joseph E Tomaszewski
The present study was aimed at fingerprinting pharmacoproteomic alterations of the Mycobacterium tuberculosis H37Rv strain induced by antitubercular drugs isoniazid (INH), ethambutol (EMB), and SQ109 [N-geranyl-N'-(2-adamantyl)ethane-1,2-diamine, a novel 1,2-diamine-based EMB analog], providing new understanding of pharmacoproteomic mechanisms of each and exploring new drug targets. The three drugs produced significant down-regulation of 13 proteins, including immunogenic ModD, Mpt64, with proteins from the Pro-Glu family being inhibited the most...
November 2005: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/15247240/the-transcriptional-responses-of-mycobacterium-tuberculosis-to-inhibitors-of-metabolism-novel-insights-into-drug-mechanisms-of-action
#20
Helena I M Boshoff, Timothy G Myers, Brent R Copp, Michael R McNeil, Michael A Wilson, Clifton E Barry
The differential transcriptional response of Mycobacterium tuberculosis to drugs and growth-inhibitory conditions was monitored to generate a data set of 430 microarray profiles. Unbiased grouping of these profiles independently clustered agents of known mechanism of action accurately and was successful at predicting the mechanism of action of several unknown agents. These predictions were validated biochemically for two agents of previously uncategorized mechanism, pyridoacridones and phenothiazines. Analysis of this data set further revealed 150 underlying clusters of coordinately regulated genes offering the first glimpse at the full metabolic potential of this organism...
September 17, 2004: Journal of Biological Chemistry
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