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Book
Tuberculosis Drug Discovery and Development 2019
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ISBN: 3039432362 3039432370 Year: 2020 Publisher: MDPI - Multidisciplinary Digital Publishing Institute

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Keywords


Book
Tuberculosis Drug Discovery and Development 2019
Authors: ---
Year: 2020 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis and still represents one of the global health threats to mankind. The World Health Organization estimated more than 10 million new cases and reported more than 1.5 million deaths in 2019, thus ranking TB among the main causes of death due to a single pathogen. Standard anti-TB therapy includes four first-line antibiotics that should be administered for at least six months. However, in the case of multi- and extensively drug-resistant TB, second-line medications must be used and these frequently cause severe side effects resulting in poor compliance. Developing new anti-TB drug candidates is therefore of outmost importance. In this Special Issue dedicated to Tuberculosis Drug Discovery and Development, we present the main and latest achievements in the fields of drug and target discovery, host-directed therapy, anti-virulence drugs, and describe the development of two advanced compounds: macozinone and delpazolid. In addition, this Special Issue provides an historical perspective focused on Carlo Forlanini, the inventor of pneumothorax for TB treatment, and includes an overview of the state-of-the-art technologies which are being exploited nowadays in TB drug development. Finally, a summary of TB vaccines that are either approved or undergoing clinical trials concludes the Special Issue.

Keywords

Research & information: general --- Biology, life sciences --- mycobacteria --- tuberculosis --- multi-drug resistance --- drug discovery --- promiscuous targets --- Mycobacterium tuberculosis --- rifampin --- isoniazid --- mechanisms of resistance --- mutations --- granulomas --- caseum --- cell envelope --- dormancy --- delpazolid --- macozinone --- DprE1 inhibitor --- clinical studies --- discovery --- mode of action --- drug resistance --- toxicity --- target --- energy metabolism --- electron transport chain --- oxidative phosphorylation --- bedaquiline --- Q203 --- MID3 --- pharmacokinetics --- pharmacodynamics --- drug-drug interactions --- in vitro --- in vivo --- drug development --- tuberculosis treatment --- biomarkers --- drug combination --- clinical trial --- BCG --- tuberculosis vaccines --- TBVI --- EDCTP --- IAVI --- CTVD --- host-directed therapy --- anti-virulence compounds --- TB --- post-treatment sequelae --- surgery --- pulmonary rehabilitation --- Carlo Forlanini --- artificial pneumothorax --- n/a --- structure-based drug design --- target-based drug design --- PknB --- PknG --- DNA gyrase --- antibiotic --- mycobacterium --- genomics --- transcriptomics --- proteomics --- metabolomics --- lipidomics --- target identification --- mechanism of action --- antimicrobial drug resistance (AMR) --- target-based screening --- phenotypic screening --- antituberculosis agents --- antimycobacterial --- anti-TB drug pipeline --- privileged targets --- lead generation


Book
Tuberculosis Drug Discovery and Development 2019
Authors: ---
Year: 2020 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis and still represents one of the global health threats to mankind. The World Health Organization estimated more than 10 million new cases and reported more than 1.5 million deaths in 2019, thus ranking TB among the main causes of death due to a single pathogen. Standard anti-TB therapy includes four first-line antibiotics that should be administered for at least six months. However, in the case of multi- and extensively drug-resistant TB, second-line medications must be used and these frequently cause severe side effects resulting in poor compliance. Developing new anti-TB drug candidates is therefore of outmost importance. In this Special Issue dedicated to Tuberculosis Drug Discovery and Development, we present the main and latest achievements in the fields of drug and target discovery, host-directed therapy, anti-virulence drugs, and describe the development of two advanced compounds: macozinone and delpazolid. In addition, this Special Issue provides an historical perspective focused on Carlo Forlanini, the inventor of pneumothorax for TB treatment, and includes an overview of the state-of-the-art technologies which are being exploited nowadays in TB drug development. Finally, a summary of TB vaccines that are either approved or undergoing clinical trials concludes the Special Issue.


Book
Tuberculosis Drug Discovery and Development 2019
Authors: ---
Year: 2020 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Bookmark

Abstract

Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis and still represents one of the global health threats to mankind. The World Health Organization estimated more than 10 million new cases and reported more than 1.5 million deaths in 2019, thus ranking TB among the main causes of death due to a single pathogen. Standard anti-TB therapy includes four first-line antibiotics that should be administered for at least six months. However, in the case of multi- and extensively drug-resistant TB, second-line medications must be used and these frequently cause severe side effects resulting in poor compliance. Developing new anti-TB drug candidates is therefore of outmost importance. In this Special Issue dedicated to Tuberculosis Drug Discovery and Development, we present the main and latest achievements in the fields of drug and target discovery, host-directed therapy, anti-virulence drugs, and describe the development of two advanced compounds: macozinone and delpazolid. In addition, this Special Issue provides an historical perspective focused on Carlo Forlanini, the inventor of pneumothorax for TB treatment, and includes an overview of the state-of-the-art technologies which are being exploited nowadays in TB drug development. Finally, a summary of TB vaccines that are either approved or undergoing clinical trials concludes the Special Issue.

Keywords

Research & information: general --- Biology, life sciences --- mycobacteria --- tuberculosis --- multi-drug resistance --- drug discovery --- promiscuous targets --- Mycobacterium tuberculosis --- rifampin --- isoniazid --- mechanisms of resistance --- mutations --- granulomas --- caseum --- cell envelope --- dormancy --- delpazolid --- macozinone --- DprE1 inhibitor --- clinical studies --- discovery --- mode of action --- drug resistance --- toxicity --- target --- energy metabolism --- electron transport chain --- oxidative phosphorylation --- bedaquiline --- Q203 --- MID3 --- pharmacokinetics --- pharmacodynamics --- drug-drug interactions --- in vitro --- in vivo --- drug development --- tuberculosis treatment --- biomarkers --- drug combination --- clinical trial --- BCG --- tuberculosis vaccines --- TBVI --- EDCTP --- IAVI --- CTVD --- host-directed therapy --- anti-virulence compounds --- TB --- post-treatment sequelae --- surgery --- pulmonary rehabilitation --- Carlo Forlanini --- artificial pneumothorax --- structure-based drug design --- target-based drug design --- PknB --- PknG --- DNA gyrase --- antibiotic --- mycobacterium --- genomics --- transcriptomics --- proteomics --- metabolomics --- lipidomics --- target identification --- mechanism of action --- antimicrobial drug resistance (AMR) --- target-based screening --- phenotypic screening --- antituberculosis agents --- antimycobacterial --- anti-TB drug pipeline --- privileged targets --- lead generation --- mycobacteria --- tuberculosis --- multi-drug resistance --- drug discovery --- promiscuous targets --- Mycobacterium tuberculosis --- rifampin --- isoniazid --- mechanisms of resistance --- mutations --- granulomas --- caseum --- cell envelope --- dormancy --- delpazolid --- macozinone --- DprE1 inhibitor --- clinical studies --- discovery --- mode of action --- drug resistance --- toxicity --- target --- energy metabolism --- electron transport chain --- oxidative phosphorylation --- bedaquiline --- Q203 --- MID3 --- pharmacokinetics --- pharmacodynamics --- drug-drug interactions --- in vitro --- in vivo --- drug development --- tuberculosis treatment --- biomarkers --- drug combination --- clinical trial --- BCG --- tuberculosis vaccines --- TBVI --- EDCTP --- IAVI --- CTVD --- host-directed therapy --- anti-virulence compounds --- TB --- post-treatment sequelae --- surgery --- pulmonary rehabilitation --- Carlo Forlanini --- artificial pneumothorax --- structure-based drug design --- target-based drug design --- PknB --- PknG --- DNA gyrase --- antibiotic --- mycobacterium --- genomics --- transcriptomics --- proteomics --- metabolomics --- lipidomics --- target identification --- mechanism of action --- antimicrobial drug resistance (AMR) --- target-based screening --- phenotypic screening --- antituberculosis agents --- antimycobacterial --- anti-TB drug pipeline --- privileged targets --- lead generation


Book
Fighting Against Resistant Strains : The Case of Benzothiazinones and Dinitrobenzamides
Authors: --- ---
Year: 2012 Publisher: London : InTechOpen,

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Abstract

In 1957, a Streptomyces strain, the ME/83 (S.mediterranei), was isolated in the Lepetit Research Laboratories from a soil sample collected at a pine arboretum near Saint Raphael, France. This drug was the base for the chemotherapy with Streptomicine. The euphoria generated by the success of this regimen lead to the idea that TB eradication would be possible by the year 2000. Thus, any further drug development against TB was stopped. Unfortunately, the lack of an accurate administration of these drugs originated the irruption of the drug resistance in Mycobacterium tuberculosis. Once the global emergency was declared in 1993, seeking out new drugs became urgent. In this book, diverse authors focus on the development and the activity of the new drug families.

Keywords

Tuberculosis.

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