Crystal Structure of DIM-1, an Acquired Subclass B1 Metallo-β-Lactamase from Pseudomonas stutzeri.

Autor: Michael P S Booth, Magda Kosmopoulou, Laurent Poirel, Patrice Nordmann, James Spencer

Publikováno v: PLoS ONE, Vol 10, Iss 10, p e0140059 (2015)

Metallo-β-lactamases (MBLs) hydrolyze almost all classes of β-lactam antibiotic, including carbapenems-currently first choice drugs for opportunistic infections by Gram-negative bacterial pathogens. MBL inhibitor development is complicated by the d

Externí odkaz: https://doaj.org/article/c7d49f50ac984e71beff242169a141ed

Bisthiazolidines: A Substrate-Mimicking Scaffold as an Inhibitor of the NDM-1 Carbapenemase

Autor: Valerie Castillo, Jürgen Brem, Maria F. Mojica, Alejandro J. Vila, Robert A. Bonomo, Leticia I. Llarrull, James Spencer, Magda Kosmopoulou, Ilaria Pettinati, Graciela Mahler, Philip Hinchliffe, Christopher J. Schofield, Mariano M. González

Publikováno v: CONICET Digital (CONICET)
Consejo Nacional de Investigaciones Científicas y Técnicas
instacron:CONICET

Pathogenic Gram-negative bacteria resistant to almost all β-lactam antibiotics are a major public health threat. Zn(II)-dependent or metallo-β-lactamases (MBLs) produced by these bacteria inactivate most β-lactam antibiotics, including the carbape

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::903a1f448d1ec5683530479343fb7c8a
https://doi.org/10.1021/acsinfecdis.5b00046

Cross-class metallo-β-lactamase inhibition by bisthiazolidines reveals multiple binding modes

Autor: Valerie Castillo, Alejandro J. Vila, Graciela Mahler, Javier M. González, Maria F. Mojica, Cecilia Saiz, Magda Kosmopoulou, Mariano M. González, James Spencer, Catherine L. Tooke, Philip Hinchliffe, Robert A. Bonomo, Leticia I. Llarrull

Publikováno v: Hinchliffe, P, Gonzalez, M M, Mojica, M F, Gonzalez, J M, Castillo, V, Saiz, C, Kosmopoulou, M, Tooke, C, Llarrull, L, Mahler, G, Bonomo, R A, Villa, A J & Spencer, J 2016, ' Cross-class metallo-β-lactamase inhibition by bisthiazolidines reveals multiple binding modes ', Proceedings of the National Academy of Sciences of the United States of America, vol. 113, no. 26, pp. E3745-E3754 . https://doi.org/10.1073/pnas.1601368113
CONICET Digital (CONICET)
Consejo Nacional de Investigaciones Científicas y Técnicas
instacron:CONICET

Metallo-β-lactamases (MBLs) hydrolyze almost all β-lactam antibiotics and are unaffected by clinically available β-lactamase inhibitors (βLIs). Active-site architecture divides MBLs into three classes (B1, B2, and B3), complicating development of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::68799a23a5f1b0de2ff1b3625c35706a
https://research-information.bris.ac.uk/en/publications/e66e5c86-fd98-4326-9bee-15426e11504f

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells

Autor: Nathan J. Brown, Edward McDonald, Jonathan M. Large, Jóhannes Reynisson, Spiros Linardopoulos, Mizio Matteucci, Butrus Atrash, Amir Faisal, Richard Bayliss, Magda Kosmopoulou, Vassilios Bavetsias, Chongbo Sun, Julian Blagg, Nathalie Bouloc

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:5988-5993

Co-crystallisation of the imidazo[1,2-a]pyrazine derivative 15 (3-chloro-N-(4-morpholinophenyl)-6-(pyridin-3-yl)imidazo[1,2-a]pyrazin-8-amine) with Aurora-A provided an insight into the interactions of this class of compound with Aurora kinases. This

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9963adc586e8f8225af6c581b5b4603f
https://doi.org/10.1016/j.bmcl.2010.08.091

In the Search of Glycogen Phosphorylase Inhibitors: Synthesis of C-D-Glycopyranosylbenzo(hydro)quinones – Inhibition of and Binding to Glycogen Phosphorylase in the Crystal

Autor: Evangelia D. Chrysina, Magda Kosmopoulou, C. Tiraidis, Guo-Rong Chen, Li He, Nikos G. Oikonomakos, Jean-Pierre Praly, Marcelle Tanoh, Demetres D. Leonidas, Yun Zhi Zhang

Publikováno v: European Journal of Organic Chemistry. 2007:596-606

Penta-O-acetyl-β-D-glycopyranoses and 1,4-dimethoxybenzene led selectively by electrophilic substitution to C-β-D-glycopyranosyl-1,4-dimethoxybenzenes which were converted by simple and efficient reactions (oxidation, reduction and deacetylation) t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::07315abd3d7356dad39bc04b5d6c403e
https://doi.org/10.1002/ejoc.200600548