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List of selected publications

Discovery and development of antibacterials

Influence of 4'-O-glycoside constitution and configuration on ribosomal selectivity of paromomycin. Matsushita. T, Chen W., Juskeviciene R., Teo Y., Shcherbakov D., Vasella A., Boettger EC., Crich D. J Am Chem Soc. 2015 Jun 24; 137(24):7706-17.

Identification and evaluation of improved 4'-O-(alkyl) 4,5-disubstituted 2-deoxystreptamines as next-generation aminoglycoside antibiotics. Duscha S, Boukari H, Shcherbakov D, Salian S, Silva S, Kendall A, Kato T, Akbergenov R, Perez-Fernandez D, Bernet B, Vaddi S, Thommes P, Schacht J, Crich D, Vasella A, Böttger EC. MBio. 2014 Sep 30;5(5):e01827-14

4'-O-Substitutions determine selectivity of aminoglycoside antibiotics. Perez-Fernandez D, Shcherbakov D, Matt T, Leong NC, Kudyba I, Duscha S, Boukari H, Patak R, Dubbaka SR, Lang K, Meyer M, Akbergenov R, Freihofer P, Vaddi S, Thommes P, Ramakrishnan V, Vasella A, Böttger EC. Nat Commun. 2014;5:3112. doi: 10.1038/ncomms4112

Synthesis, antiribosomal and antibacterial activity of 4’-O-glycopyranosyl paromomycin aminoglycoside antibiotics. Chen W, Matsushita T, Shcherbakov D, Boukari H, Vasella A, Böttger EC, Crich D. Med Chem Commun. 2014;5:1179-1187.

Importance of the 6'-hydroxy group and its configuration for apramycin activity. Mandhapati AR, Shcherbakov D, Duscha S, Vasella A, Böttger EC, Crich D. ChemMedChem. 2014 Sep;9(9):2074-83. doi: 10.1002/cmdc.201402146

Dissociation of antibacterial activity and aminoglycoside ototoxicity in the 4-monosubstituted 2-deoxystreptamine apramycin. Matt T, Ng CL, Lang K, Sha SH, Akbergenov R, Shcherbakov D, Meyer M, Duscha S, Xie J, Dubbaka SR, Perez-Fernandez D, Vasella A, Ramakrishnan V, Schacht J, Böttger EC. Proc Natl Acad Sci U S A. 2012 Jul 3;109(27):10984-9. doi: 10.1073/pnas.1204073109

Structure-activity relationships among the kanamycin aminoglycosides: role of ring I hydroxyl and amino groups. Salian S, Matt T, Akbergenov R, Harish S, Meyer M, Duscha S, Shcherbakov D, Bernet BB, Vasella A, Westhof E, Böttger EC. Antimicrob Agents Chemother. 2012 Dec; 56(12):6104-8. doi: 10.1128/AAC.01326-12

Aminoglycoside toxicity

Genetic analysis of interactions with eukaryotic rRNA identify the mitoribosome as target in aminoglycoside ototoxicity. Hobbie SN, Akshay S, Kalapala SK, Bruell CM, Shcherbakov D, Böttger EC. Proc Natl Acad Sci U S A. 2008 Dec 30;105(52):20888-93

Engineering the rRNA decoding site of eukaryotic cytosolic ribosomes in bacteria. Hobbie SN, Kalapala SK, Akshay S, Bruell C, Schmidt S, Dabow S, Vasella A, Sander P, Böttger EC. Nucleic Acids Res. 2007;35(18):6086-93

Structural basis for selectivity and toxicity of ribosomal antibiotics. Böttger EC, Springer B, Prammananan T, Kidan Y, Sander P. EMBO Rep. 2001 Apr;2(4):318-23

Mechanistic studies on antibacterials

In vivo efficacy of apramycin in murine infection models. Meyer M, Freihofer P, Scherman M, Teague J, Lenaerts A, Böttger EC. Antimicrob Agents Chemother. 2014 Nov; 58(11):6938-41. doi: 10.1128/AAC.03239-14

Molecular basis for the selectivity of antituberculosis compounds capreomycin and viomycin. Akbergenov R, Shcherbakov D, Matt T, Duscha S, Meyer M, Wilson DN, Böttger EC. Antimicrob Agents Chemother. 2011 Oct;55(10):4712-7. doi: 10.1128/AAC.00628-11

Binding of neomycin-class aminoglycoside antibiotics to mutant ribosomes with alterations in the A site of 16S rRNA. Hobbie SN, Pfister P, Bruell C, Sander P, François B, Westhof E, Böttger EC. Antimicrob Agents Chemother. 2006 Apr;50(4):1489-96

Analysis of the contribution of individual substituents in 4,6-aminoglycoside-ribosome interaction. Hobbie SN, Pfister P, Brüll C, Westhof E, Böttger EC. Antimicrob Agents Chemother. 2005 Dec;49(12):5112-8

Mutagenesis of 16S rRNA C1409-G1491 base-pair differentiates between 6'OH and 6'NH3+ aminoglycosides. Pfister P, Hobbie S, Brüll C, Corti N, Vasella A, Westhof E, Böttger EC. J Mol Biol. 2005 Feb 18;346(2):467-75

Role of 16S rRNA Helix 44 in Ribosomal Resistance to Hygromycin B. Pfister P, Risch M, Brodersen DE, Böttger EC. Antimicrob Agents Chemother. 2003 May;47(5):1496-502

The molecular basis for A-site mutations conferring aminoglycoside resistance: relationship between ribosomal susceptibility and X-ray crystal structures. Pfister P, Hobbie S, Vicens Q, Böttger EC, Westhof E. Chembiochem. 2003 Oct 6;4(10):1078-88

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