Selected Literature

Apramycin overcomes the inherent lack of antimicrobial bactericidal activity in Mycobacterium abscessus
Selchow P, Ordway DJ, Verma D, Whittel N, Petrig A, Hobbie SN, Böttger EC, Sander P (2022)
Antimicrob Agents Chemother 66: e015021

Short synthesis of (+)-actinobolin: simple entry to complex small-molecule inhibitors of protein synthesis
Tharra PR, Mikhaylov AA, Svejkar J, Gysin M, Hobbie SN, Svenda J (2022)
Angew Chem Int Ed Engl: Online ahead of print

Genotypic and phenotypic analyses of aac(3) aminoglycoside-resistance gene diversity point to three distinct phenotypes of contemporary clinical relevance
Plattner M, Goyet C, Haldimann K, Gysin M, Juhas M, Becker K, Hobbie SN (2021)

J Glob Antimicrob Resist: Online ahead of print

Antibacterial activity of apramycin at acidic pH warrants wide therapeutic window in the treatment of complicated urinary tract infections and acute pyelonephritis
Becker K, Cao S, Nilsson A, Erlandsson M, Hotop SK, Kuka J, Hansen J, Haldimann K, Grinberga S, Berruga-Fernandéz T, Huseby DL, Shariatgorji R, Lindmark E, Pltazack B, Böttger EC, Crich D, Friberg LE, Vingsbo Lundberg C, Hughes D, Brönstrup M, Andrén PE, Liepinsh E, Hobbie SN (2021)

EBioMedicine 73: 103652

Antimicrobial susceptibility patterns of respiratory Gram-negative bacterial isolates from COVID-19 patients in Switzerland
Gysin M, Acevedo CT, Haldimann K, Bodendoerfer E, Imkamp F, Bulut K, Buehler PK, Brugger SD, Becker K, Hobbie SN
Ann Clin Microbiol Antimicrob 20: 64

Synthesis and antibacterial activity of propylamycinderivatives functionalized at the 5′′- and other positions with a view to overcoming resistance due to aminoglycoside modifying enzymes
Lubriks D, Zogota R, Sarpe VA, Matsushita T, Sati GC, Haldimann K, Gysin M, Böttger EC, Vasella A, Suna E, Hobbie SN, Crich D (2021)

ACS Infect Dis 7: 2413-2424

Modelinformed drug development for antimicrobials: translational PK and PK/PD modeling to predict an efficacious human dose for apramycin
Sou T, Hansen J, Liepinsh E, Backlund M, Ercan O, Grinberga S, Cao S, Giachou P, Petersson A, Tomczak M, Urbas M, Zabicka D, Vingsbo-Lundberg C, Hughes D, Hobbie SN, Friberg LE
Clin Pharmacol Ther 109:1063-1073

An advanced apralog with increased in-vitro and in-vivo activity toward Gram-negative pathogens and reduced ex-vivo cochleotoxicity
Sonousi A, Quirke J, Waduge P, Janusic T, Gysin M, Haldimann K, Hobbie SN, Sha S, Schacht J, Chow Ch, Vasella A, Böttger EC, Xu S, Crich D (2021)
ChemMedChem 16: 335-339

Efficacy of EBL-1003 (apramycin) against Acinetobacter baumannii lung infections in mice
Becker K, Aranzana-Climent V, Cao S, Nilsson A, Shariatgorji R, Haldimann K, Platzack B, Hughes D, Andrén P, Böttger EC, Friberg L, Hobbie SN (2021)
Clin Microbiol Infect 27: 1315-1321

Epidemiologic, phenotypic, and structural characterization of aminoglycoside-resistance gene aac(3)-IV
Plattner M, Gysin M, Haldimann K, Becker K, Hobbie SN (2020)
Int J Mol Sci 21: 6133

Apralogs: apramycin 5-O-glycosides and ethers with improved antibacterial activity and ribosomal selectivity and reduced susceptibility to the aminoacyltranserferase (3)-IV resistance determinant
Quirke JCK, Rajasekaran P, Sarpe VA, Sonousi A, Osinnii I, Gysin M, Haldimann K, Fang QJ, Shcherbakov D, Hobbie SN, Sha SH, Schacht J, Vasella A, Böttger EC, Crich D (2020)
J Am Chem Soc 142: 530-544

Modification at the 2'-position of the 4,5-series of 2-deoxystreptamine aminoglycoside antibiotics to resist aminoglycoside modifying enzymes and increase ribosomal target selectivity
Sati GC, Sarpe VA, Furukawa T, Mondal S, Mantovani M, Hobbie SN, Vasella A, Böttger EC, Crich D (2019)
ACS Infect Dis 5: 1718-1730

Synthesis of saccharocin from apramycin and evaluation of its ribosomal selectivity
Sarpe VA, Pirrone MG, Haldimann K, Hobbie SN, Vasella A, Crich D (2019)
Medchemcomm 10: 554-558

Design, multigram synthesis, and in vitro and in vivo evaluation of propylamycin: a semisynthetic 4,5-deoxystreptamine class aminoglycoside for the treatment of drug-resistant Enterobacteriaceae and other Gram-negative pathogens
Matsushita T, Sati G, Kondasinghe N, Pirrone M, Kato T, Waduge P, Santhosh Kumar H, Cortes Sanchon A, Dobosz-Bartoszek M, Shcherbakov D, Juhas M, Hobbie S, Schrepfer T, Chow C, Polikanov Y, Schacht J, Vasella A, Böttger EC, Crich D (2019)
J Am Chem Soc 141: 5051-5061

In vitro activity of apramycin against multidrug-, carbapenem- and aminoglycoside-resistant Enterobacteriaceae and Acinetobacter baumannii
Juhas M, Widlake E, Teo J, Huseby DL, Tyrrell JM, Polikanov YS, Ercan O, Petersson A, Cao S, Aboklaish AF, Rominski A, Crich D, Böttger EC, Walsh TR, Hughes D, Hobbie SN (2019)

J Antimicrob Chemother 74: 944-952

Neutralization of antibody-enhanced dengue infection by VIS513, a pan serotype reactive monoclonal antibody targeting domain III of the dengue E protein
Budigi Y, Ong EZ, Robinson LN, Ong LC, Rowley KJ, Winnett A, Tan HC, Hobbie SN, Shriver Z, Babcock GJ, Alonso S, Ooi EE (2018)
PLoS Negl Trop Dis 12: e0006209

Structure-based design and synthesis of apramycin-paromomycin analogues. Importance of the configuration at the 6′-position and differences between the 6′-amino and hydroxy series
Mandhapati AR, Yang G, Kato T, Shcherbakov D, Hobbie SN, Vasella A, Böttger EC, Crich D (2017)
J Am Chem Soc 139: 14611-14619