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Emerging peptide antibiotics with therapeutic potential
Gregory Upert1, Anatol Luther2, Daniel Obrecht1
1Polyphor Ltd, Hegenheimermattweg 125, 4123 Allschwil, Switzerland.
Medicine in Drug Discovery
|January 5, 2021
Abstract:
This review covers some of the recent progress in the field of peptide antibiotics with a focus on compounds with novel or established mode of action and with demonstrated efficacy in animal infection models. Novel drug discovery approaches, linear and macrocyclic peptide antibiotics, lipopeptides like the polymyxins as well as peptides addressing targets located in the plasma membrane or in the outer membrane of bacterial cells are discussed.
Keywords:
ADMET, absorption, distribution, metabolism and excretion – toxicity in pharmacokineticsAMP, antimicrobial peptideAMR, antimicrobial resistanceATCC, ATCC cell collectionAntibioticBAM, β-barrel assembly machineryCC50, cytotoxic concentration to kill 50% of cellsCD, circular dichroismCFU, colony forming unitCLSI, clinical and laboratory standards instituteCMS, colistin methane sulfonateDMPC, 1,2-dimyristoyl-sn-glycero-3-phosphocholineESKAPE, acronym encompassing six bacterial pathogens (often carrying antibiotic resistance): Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter sppFDA, U. S. Food and Drug AdministrationHABP, hospital acquired bacterial pneumoniaHDP, host-defense peptideHEK293, human embryonic kidney 293 cellsHK-2, human kidney 2 cells (proximal tubular cell line)HepG2, human hepatocellular carcinoma cell lineHpg, 4-hydroxy-phenyl glycineITC, isothermal titration calorimetryKPC, Klebsiella pneumoniae metallo-β-lactamase C resistantLPS, lipopolysaccharideLptA, lipopolysaccharide transport protein ALptC, lipopolysaccharide transport protein CLptD, lipopolysaccharide transport protein DMDR, multidrug-resistantMH-I, Müller-Hinton broth IMH-II, Müller-Hinton broth II (cation adjusted)MIC, minimal inhibitory concentrationMRSA, methicilline-resistant S. aureusMSSA, methicilline-sensitive S. aureusMoA, mechanism (mode) of actionNDM-1, New Delhi metallo-β-lactamase resistantNOAEL, no adverse effect levelODL, odilorhabdinOMPTA (outer membrane targeting antibiotic)OMPTA, outer membrane targeting antibioticOmp, outer membrane proteinPBMC, peripheral mononuclear blood cellPBP, penicillin-binding proteinPBS, phosphate-buffered salinePK, pharmacokineticsPOPC, 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholinePOPG, 2-oleoyl-1-palmitoyl-sn-glycero-3-phospho-(1-glycerol)PrAMPs, polyproline antimicrobial peptidesRBC, red blood cellSAR, structure-activity relationshipSPR, surface plasmon resonanceSPase I, signal peptidase IVABP, ventilator associated bacterial pneumoniaVIM-1, beta-lactamase 2 (K. pneumoniae)VISA, vancomycin-intermediate S. aureusVRE, vancomycin-resistant enterococcusWHO, World Health OrganizationWT, wild typeWTA, wall teichoic acidXDR, extremely drug-resistantantimicrobial peptideantimicrobial resistancebid, bis in die (two times a day)i.p., intraperitoneali.v., intravenouslipopeptidemITT population, minimal intend-to-treat populationpeptide antibiotics.c., subcutaneous
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