Antibiotic Drug Discovery Targeting Bacterial Metabolism - read free eBook in online reader or directly download on the web page. Select files or add your book in reader. Download and read online ebook Antibiotic Drug Discovery Targeting Bacterial Metabolism write by Miranda J Wallace. This book was released on 2019. Antibiotic Drug Discovery Targeting Bacterial Metabolism available in PDF, EPUB and Kindle. Over the last century, the use of antibiotics has enabled many advances in modern medicine, making life as we know it possible. In recent years, however, emerging bacterial resistance to virtually all major antibiotic classes has resulted in a worldwide increase in morbidity, mortality, and financial burden associated with drug resistant infections. The antimicrobial resistance crisis presents an urgent need for new antimicrobials with distinct mechanisms of action from existing drugs. The current pharmaceutical pipeline of new antibiotics is limited due to three obstacles: a lack of understanding of resistance mechanisms, a dearth of novel mechanisms of action among new antibiotics, and drug discovery challenges unique to bacteria due to their cellular and physiological composition. My dissertation research addressed each of these challenges. The mechanisms of resistance to folate biosynthesis inhibitors in Staphylococcus aureus were explored from a genetic, biological, biochemical, and structural basis. Unexpected roles in resistance and fitness were attributed to various mutations in the sulfonamide target dihydropteroate synthase. This information currently guides the development of next-generation antifolates designed to avoid these characterized resistance strategies. In the subsequent chapter, a conditional metabolic screening approach was employed to discover inhibitors disrupting metabolic pathways related to folate biosynthesis. The testing conditions were optimized to measure the biological activity of antimetabolites, which is often masked by nutrients present in standard testing media. This screen yielded an inhibitor of cysteine synthase A in Escherichia coli, which was characterized in chapter four. Multiple experimental approaches yielded indications that the cysteine synthase A inhibitors have a false-product mechanism, resulting in a widespread impact on several key branches of metabolism beyond cysteine biosynthesis. The final research chapter describes the adaptation of the cellular thermal shift assay to explore target engagement in the Gram-negative cell system. Drug entry and accumulation are especially challenging to achieve in Gram-negative cells due to their unique dual membrane system and associated efflux machinery. This assay provided an early stage tool to quickly assess the ability of antimicrobial candidates to engage the intended target in the intact cell system and also measure efflux sensitivity. Taken together, this dissertation contributes to the fight against the antimicrobial resistance crisis from multiple angles, all within the context of bacterial metabolism which is a rich source of exciting new antibiotic targets.
Drug Discovery Targeting Drug-Resistant Bacteria
Drug Discovery Targeting Drug-Resistant Bacteria - read free eBook in online reader or directly download on the web page. Select files or add your book in reader. Download and read online ebook Drug Discovery Targeting Drug-Resistant Bacteria write by Prashant Kesharwani. This book was released on 2020-05-15. Drug Discovery Targeting Drug-Resistant Bacteria available in PDF, EPUB and Kindle. Drug Discovery Targeting Drug-Resistant Bacteria explores the status and possible future of developments in fighting drug-resistant bacteria. The book covers the majority of microbial diseases and the drugs targeting them. In addition, it discusses the potential targeting strategies and innovative approaches to address drug resistance. It brings together academic and industrial experts working on discovering and developing drugs targeting drug-resistant (DR) bacterial pathogens. New drugs active against drug-resistant pathogens are discussed, along with new strategies being used to discover molecules acting via new modes of action. In addition, alternative therapies such as peptides and phages are included. Pharmaceutical scientists, microbiologists, medical professionals, pathologists, researchers in the field of drug discovery, infectious diseases and microbial drug discovery both in academia and in industrial settings will find this book helpful. Written by scientists with extensive industrial experience in drug discovery Provides a balanced view of the field, including its challenges and future directions Includes a special chapter on the identification and development of drugs against pathogens which exhibit the potential to be used as weapons of war
Antibacterial Agents
Antibacterial Agents - read free eBook in online reader or directly download on the web page. Select files or add your book in reader. Download and read online ebook Antibacterial Agents write by Rosaleen Anderson. This book was released on 2012-07-23. Antibacterial Agents available in PDF, EPUB and Kindle. Antibacterial agents act against bacterial infection either by killing the bacterium or by arresting its growth. They do this by targeting bacterial DNA and its associated processes, attacking bacterial metabolic processes including protein synthesis, or interfering with bacterial cell wall synthesis and function. Antibacterial Agents is an essential guide to this important class of chemotherapeutic drugs. Compounds are organised according to their target, which helps the reader understand the mechanism of action of these drugs and how resistance can arise. The book uses an integrated “lab-to-clinic” approach which covers drug discovery, source or synthesis, mode of action, mechanisms of resistance, clinical aspects (including links to current guidelines, significant drug interactions, cautions and contraindications), prodrugs and future improvements. Agents covered include: agents targeting DNA - quinolone, rifamycin, and nitroimidazole antibacterial agents agents targeting metabolic processes - sulfonamide antibacterial agents and trimethoprim agents targeting protein synthesis - aminoglycoside, macrolide and tetracycline antibiotics, chloramphenicol, and oxazolidinones agents targeting cell wall synthesis - β-Lactam and glycopeptide antibiotics, cycloserine, isonaizid, and daptomycin Antibacterial Agents will find a place on the bookshelves of students of pharmacy, pharmacology, pharmaceutical sciences, drug design/discovery, and medicinal chemistry, and as a bench reference for pharmacists and pharmaceutical researchers in academia and industry.
Antibiotic Drug Discovery
Antibiotic Drug Discovery - read free eBook in online reader or directly download on the web page. Select files or add your book in reader. Download and read online ebook Antibiotic Drug Discovery write by Steven M Firestine. This book was released on 2017-05-19. Antibiotic Drug Discovery available in PDF, EPUB and Kindle. Recent years have seen a resurgence of antibiotic drug discovery. This book brings together the relevant information to assess the state-of-the-art. It identifies and elaborates the most recent and compelling strategies for antibiotic drug discovery with a primary focus on new targets, mechanisms and molecular entities. Addressing the need for continued investment in antibiotic drug development, the book provides a point of reference for the rapidly expanding infectious disease research community. In addition to its attention on new targets, the book focusses on the medicinal chemistry and chemistry of the targets. Within this framework, chapters from leading researchers in academia and industry address findings in important areas such as biofilm production, narrow spectrum antibiotics and novel antibacterials from previously uncultured soil bacteria. This book will be a useful resource for postgraduate students and researchers in medicinal chemistry wishing to understand the latest approaches to antibiotic drug discovery.
The Antibiotic Resistome
The Antibiotic Resistome - read free eBook in online reader or directly download on the web page. Select files or add your book in reader. Download and read online ebook The Antibiotic Resistome write by Gerry Wright. This book was released on 2016-08-22. The Antibiotic Resistome available in PDF, EPUB and Kindle.
