Search Results - "CHIARELLI, Laurent R"
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Burkholderia cenocepacia Infections in Cystic Fibrosis Patients: Drug Resistance and Therapeutic Approaches
Published in Frontiers in microbiology (22-08-2017)“…is an opportunistic pathogen particularly dangerous for cystic fibrosis (CF) patients. It can cause a severe decline in CF lung function possibly developing…”
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Antibiotics' Sustainability: Another Issue in the Fight against Antimicrobial Resistance
Published in Current topics in medicinal chemistry (01-01-2022)“…The spread of antimicrobial resistance (AMR) is still a major threat to global health that is likely to worsen also as a consequence of the COVID-19 pandemic…”
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Quorum Sensing as Antivirulence Target in Cystic Fibrosis Pathogens
Published in International journal of molecular sciences (13-04-2019)“…Cystic fibrosis (CF) is an autosomal recessive genetic disorder which leads to the secretion of a viscous mucus layer on the respiratory epithelium that…”
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Mycobacterium abscessus Infections in Cystic Fibrosis Individuals: A Review on Therapeutic Options
Published in International journal of molecular sciences (27-02-2023)“…is an opportunistic pathogen that mainly colonizes and infects cystic fibrosis patients' lungs. is naturally resistant to many antibiotics such as rifamycin,…”
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Structural Study of a New MbtI-Inhibitor Complex: Towards an Optimized Model for Structure-Based Drug Discovery
Published in Pharmaceuticals (Basel, Switzerland) (01-11-2023)“…MbtI from Mycobacterium tuberculosis (Mtb) is a Mg2+-dependent salicylate synthase, belonging to the chorismate-utilizing enzyme (CUE) family. As a fundamental…”
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Synthesis, Characterization, and Biological Evaluation of New Derivatives Targeting MbtI as Antitubercular Agents
Published in Pharmaceuticals (Basel, Switzerland) (13-02-2021)“…Tuberculosis (TB) causes millions of deaths every year, ranking as one of the most dangerous infectious diseases worldwide. Because several pathogenic strains…”
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Improving Protection to Prevent Bacterial Infections: Preliminary Applications of Reverse Vaccinology against the Main Cystic Fibrosis Pathogens
Published in Vaccines (Basel) (01-07-2023)“…Reverse vaccinology is a powerful tool that was recently used to develop vaccines starting from a pathogen genome. Some bacterial infections have the necessity…”
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Engineering of Helicobacter pylori L-asparaginase: characterization of two functionally distinct groups of mutants
Published in PloS one (09-02-2015)“…Bacterial L-asparaginases have been used as anti-cancer drugs for over 4 decades though presenting, along with their therapeutic efficacy, several side effects…”
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Molecular insights on pathogenic effects of mutations causing phosphoglycerate kinase deficiency
Published in PloS one (14-02-2012)“…Phosphoglycerate kinase (PGK) catalyzes an important ATP-generating step in glycolysis. PGK1 deficiency is an uncommon X-linked inherited disorder, generally…”
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Expanding targets for a metabolic therapy of cancer: L-asparaginase
Published in Recent patents on anti-cancer drug discovery (01-01-2012)“…The antitumour enzyme L-asparaginase (L-asparagine amidohydrolase, EC 3.5.1.1, ASNase), which catalyses the deamidation of L-asparagine (Asn) to L-aspartic…”
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Editorial: Enzyme targeting for the development of novel antimicrobials
Published in Frontiers in molecular biosciences (19-08-2024)Get full text
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Synthesis and Assessment of the In Vitro and Ex Vivo Activity of Salicylate Synthase (Mbti) Inhibitors as New Candidates for the Treatment of Mycobacterial Infections
Published in Pharmaceuticals (Basel, Switzerland) (01-08-2022)“…Tuberculosis (TB) causes millions of deaths every year, ranking as one of the most dangerous infectious diseases worldwide. Because several pathogenic strains…”
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Targeting Siderophore-Mediated Iron Uptake in M. abscessus : A New Strategy to Limit the Virulence of Non-Tuberculous Mycobacteria
Published in Pharmaceutics (02-02-2023)“…Targeting pathogenic mechanisms, rather than essential processes, represents a very attractive approach for the development of new antimycobacterial drugs. In…”
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New insight into structure-activity of furan-based salicylate synthase (MbtI) inhibitors as potential antitubercular agents
Published in Journal of enzyme inhibition and medicinal chemistry (01-01-2019)“…Starting from the analysis of the hypothetical binding mode of our previous furan-based hit (I), we successfully achieved our objective to replace the nitro…”
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Structural and Energetic Basis of Protein Kinetic Destabilization in Human Phosphoglycerate Kinase 1 Deficiency
Published in Biochemistry (Easton) (19-02-2013)“…Protein kinetic destabilization is a common feature of many human genetic diseases. Human phosphoglycerate kinase 1 (PGK1) deficiency is a rare genetic disease…”
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Rv0579 Is Involved in the Resistance to the TP053 Antitubercular Prodrug
Published in Frontiers in microbiology (25-02-2020)“…Tuberculosis remains one of the leading causes of death from a single pathogen globally. It is estimated that 1/4 of the world's population harbors latent…”
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Chemical, Metabolic, and Cellular Characterization of a FtsZ Inhibitor Effective Against Burkholderia cenocepacia
Published in Frontiers in microbiology (07-04-2020)“…There is an urgent need for new antimicrobials to treat the opportunistic Gram-negative , which represents a problematic challenge for cystic fibrosis…”
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Investigating the Mechanism of Action of Diketopiperazines Inhibitors of the Burkholderia cenocepacia Quorum Sensing Synthase CepI: A Site-Directed Mutagenesis Study
Published in Frontiers in pharmacology (31-07-2018)“…Quorum sensing (QS) is a bacterial intercellular communication process which controls the production of major virulence factors, such as proteases,…”
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Crystal Structure, Hirshfeld Surface Analysis, In-Silico and Antimycotic Investigations of Methyl 6-methyl-4-(4-nitrophenyl)-2-oxo-1,2-dihydropyrimidine-5-carboxylate
Published in Crystals (Basel) (01-01-2023)“…Herein, we report the preparation of methyl 6-methyl-4-(4-nitrophenyl)-2-oxo-1,2-dihydropyrimidine-5-carboxylate 2, obtained by the regioselective oxidative…”
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Side Chain-Modified Benzothiazinone Derivatives with Anti-Mycobacterial Activity
Published in Biomedicines (01-07-2023)“…Tuberculosis (TB) is a leading infectious disease with serious antibiotic resistance. The benzothiazinone (BTZ) scaffold PBTZ169 kills (Mtb) through the…”
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