Colistin kills bacteria by targeting lipopolysaccharide in the cytoplasmic membrane

Autor: Akshay Sabnis, Katheryn LH Hagart, Anna Klöckner, Michele Becce, Lindsay E Evans, R Christopher D Furniss, Despoina AI Mavridou, Ronan Murphy, Molly M Stevens, Jane C Davies, Gérald J Larrouy-Maumus, Thomas B Clarke, Andrew M Edwards

Publikováno v: eLife, Vol 10 (2021)

Colistin is an antibiotic of last resort, but has poor efficacy and resistance is a growing problem. Whilst it is well established that colistin disrupts the bacterial outer membrane (OM) by selectively targeting lipopolysaccharide (LPS), it was uncl

Externí odkaz: https://doaj.org/article/f64d8e9c4ae644fe8acd8e4ffd54da30

Exploitation of Antibiotic Resistance as a Novel Drug Target: Development of a β-Lactamase-Activated Antibacterial Prodrug

Autor: Thomas B. Clarke, Alan Armstrong, Thomas Webb, James Spencer, Lindsay E. Evans, Aishwarya Krishna, Dominic C Marshall, Yajing Ma, Catherine L. Tooke, Andrew M. Edwards

Publikováno v: Evans, L E, Krishna, A, Ma, Y, Webb, T E, Marshall, D C, Tooke, C L, Spencer, J, Clarke, T B, Armstrong, A & Edwards, A M 2019, ' Exploitation of Antibiotic Resistance as a Novel Drug Target : Development of a β-Lactamase-Activated Antibacterial Prodrug ', Journal of Medicinal Chemistry, vol. 62, no. 9, pp. 4411-4425 . https://doi.org/10.1021/acs.jmedchem.8b01923

[Image: see text] Expression of β-lactamase is the single most prevalent determinant of antibiotic resistance, rendering bacteria resistant to β-lactam antibiotics. In this article, we describe the development of an antibiotic prodrug that combines

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eae01767dd46807d26293699a66e1d99
https://doi.org/10.1021/acs.jmedchem.8b01923

Author response: Colistin kills bacteria by targeting lipopolysaccharide in the cytoplasmic membrane

Autor: R.A. Murphy, Lindsay E. Evans, Jane C. Davies, Michele Becce, Thomas B. Clarke, Gerald Larrouy-Maumus, Andrew M. Edwards, Katheryn Lh Hagart, Anna Klöckner, Molly M. Stevens, R. Christopher D. Furniss, Despoina A. I. Mavridou, Akshay Sabnis

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6bf2e3107d2ee9d9755099d3b60d20ad
https://doi.org/10.7554/elife.65836.sa2

N–N Bond-Forming Cyclization for the One-Pot Synthesis of N-Aryl[3,4-d]pyrazolopyrimidines

Autor: Lindsay E. Evans, Keith Jones, Matthew D. Cheeseman

Publikováno v: Organic Letters

An efficient one-pot synthesis of N-aryl[3,4-d]pyrazolopyrimidines in good yield and under mild reaction conditions is described. By exploiting electron-deficient hydroxylamines, the substituted oxime products were formed with very high E-diastereose

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a98c29e473b878ae151df0dac35331e
https://doi.org/10.1021/ol301561a

Abstract LB-304: Discovery of chemical probe CCT251236: An orally bioavailable efficacious pirin ligand from an HSF1 phenotypic screen

Autor: Keith Jones, Nicola E. A. Chessum, Elisa A. Pasqua, Matthew D. Cheeseman, Susan Lepri, Lisa O’Fee, Lindsay E. Evans, Emmanuel de Billy, Birgit Wilding, Robert te Poele, Carl S. Rye, Asadh Miah, Paul Workman, Alan T. Henley, Rosemary Burke, Michael J. Tucker, Loredana Pellegrino, Salyha Ali, Martin G. Rowlands, Suzanne A. Eccles, Meirion Richards, Swee Y. Sharp, Rob L. M. van Montfort, Florence I. Raynaud, Angela Hayes, Marissa V. Powers

Publikováno v: Cancer Research. 77:LB-304

Heat shock factor 1 (HSF1) was originally identified as a master regulator of the classical ‘cytoprotective’ heat shock response. However, a large body of evidence has now verified the importance of HSF1 to tumorigenesis and cancer progression. H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8c3da42013b9b61dceaf0f6da284c950
https://doi.org/10.1158/1538-7445.am2017-lb-304