Antibiotic Resistance themed issue
Welcome to the Antibiotic Resistance themed issue of MedChemComm.
Bacterial lipid membranes as promising targets to fight antimicrobial resistance, molecular foundations and illustration through the renewal of aminoglycoside antibiotics and emergence of amphiphilic aminoglycosides
Membrane anionic lipids as attractive targets in the design of amphiphilic antibacterial drugs active against resistant bacteria: molecular foundations and examples.
Drug-target networks in aminoglycoside resistance: hierarchy of priority in structural drug design
Drug-target network analysis for advancing next-generation aminoglycoside therapies that combat antibiotic resistant infections.
A review of patents (2011–2015) towards combating resistance to and toxicity of aminoglycosides
The information about synthesis, resistance, and toxicity of aminoglycosides in all patents from 2011–2015 is presented in details.
Mechanisms of resistance to membrane-disrupting antibiotics in Gram-positive and Gram-negative bacteria
A diverse repertoire of mechanisms has evolved to confer resistance to bacterial membrane disrupting antimicrobial cationic amphiphiles.
Targeting the trehalose utilization pathways of Mycobacterium tuberculosis
Tuberculosis (TB) is an epidemic disease and the growing burden of multidrug-resistant (MDR) TB world wide underlines the need to discover new drugs to treat the disease.
Endless resistance. Endless antibiotics?
The practice of medicine was profoundly transformed by the introduction of the antibiotics (compounds isolated from Nature) and the antibacterials (compounds prepared by synthesis) for the control of bacterial infection.
Molecular basis for resistance against phosphonate antibiotics and herbicides
Research studies in recent years have illuminated data on the mechanisms and targets of phosphonic acid antibiotics and herbicides, including fosfomycin, glyphosate, fosmidomycin and FR900098.
Mechanisms of resistance to aminoglycoside antibiotics: overview and perspectives
The newest information (2010-present) on the four main mechanisms of resistance to the broad-spectrum aminoglycoside antibiotics is presented in details.
Probing substrate binding to the metal binding sites in metallo-β-lactamase L1 during catalysis
RFQ-EXAFS studies were used to probe the metal centers in metallo-β-lactamase L1 during catalysis.
6-O-Nucleotidyltransferase: an aminoglycoside-modifying enzyme specific for streptomycin/streptidine
ANT(6) has a narrow tolerance to chemical variations in the aminoglycoside/nucleotide, making it very useful in the design of non-inactivable derivatives.
In vitro and in vivo activity of ML302F: a thioenolate inhibitor of VIM-subfamily metallo β-lactamases
The thioenol ML302F, recently identified as an inhibitor of class B metallo-β-lactamases (MBLs), restores antibiotic susceptibility to meropenem resistant strains in cells and the Galleria mellonella invertebrate model.
Identification of an inhibitor of the aminoglycoside 6′-N-acetyltransferase type Ib [AAC(6′)-Ib] by glide molecular docking
The aminoglycoside 6′-N-acetyltransferase type Ib, AAC(6′)-Ib, confers resistance to clinically relevant aminoglycosides and is the most widely distributed enzyme among AAC(6′)-I-producing Gram-negative pathogens.
Structural hybridization of three aminoglycoside antibiotics yields a potent broad-spectrum bactericide that eludes bacterial resistance enzymes
Systematically blending structural features from obsolete aminoglycosides gleaned from X-ray co-crystal models rendered a promising antibiotic inert to enzymatic modification.
Arginine-linked neomycin B dimers: synthesis, rRNA binding, and resistance enzyme activity
New dimeric aminoglycosides conjugated to arginine were synthesized and found to efficiently bind to human and bacterial RNA A-site and to evade the activity of resistance enzymes.
Patterns of biofilm structure and formation kinetics among Acinetobacter baumannii clinical isolates with different antibiotic resistance profiles
This study evaluates the rates of biofilm formation in light of the different characteristics of twelve A. baumannii clinical isolates.
Synergistic activity of a short lipidated antimicrobial peptide (lipoAMP) and colistin or tobramycin against Pseudomonas aeruginosa from cystic fibrosis patients
Synergistic effects between a lipoAMP and colistin against clinical P. aeruginosa strains isolated from cystic fibrosis patients are described.
Syntheses and biological evaluations of highly functionalized hydroxamate containing and N-methylthio monobactams as anti-tuberculosis and β-lactamase inhibitory agents
Described are the syntheses and evaluations of hydroxamate containing and N-methylthiolated monobactams as a class of potent β-lactamase inhibitors.
Potentiation of Francisella resistance to conventional antibiotics through small molecule adjuvants
A screen of 20 compounds identified small molecule adjuvants capable of potentiating antibiotic activity against Francisella philomiragia.
Design and synthesis of peptide inhibitor conjugates as probes of the Cytochrome P450s from glycopeptide antibiotic biosynthesis
The glycopeptide antibiotics are important clinical antibiotics that are currently employed against serious Gram-positive bacterial infections.
Phase II metabolic pathways of spectinamide antitubercular agents: a comparative study of the reactivity of 4-substituted pyridines to glutathione conjugation
Spectinamides are promising new semisynthetic anti-tubercular agents that are modified with a pyridyl side chain, which blocks native efflux from the tuberculosis cell.
Tabtoxinine-β-lactam is a “stealth” β-lactam antibiotic that evades β-lactamase-mediated antibiotic resistance
Tabtoxinine-β-lactam (TβL) is a phytotoxin produced by plant pathogenic strains of Pseudomonas syringae.
About this collection
This themed issue, guest edited by Professors Sylvie Garneau-Tsodikova and Gerard D. Wright, showcases some of the top research currently being carried out into the many facets of antibiotic resistance.