Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors

Autor: Jürgen Brem, Tharindi Panduwawala, Jon Ulf Hansen, Joanne Hewitt, Edgars Liepins, Pawel Donets, Laura Espina, Alistair J. M. Farley, Kirill Shubin, Gonzalo Gomez Campillos, Paula Kiuru, Shifali Shishodia, Daniel Krahn, Robert K. Leśniak, Juliane Schmidt, Karina Calvopiña, María-Carmen Turrientes, Madeline E. Kavanagh, Dmitrijs Lubriks, Philip Hinchliffe, Gareth W. Langley, Ali F. Aboklaish, Anders Eneroth, Maria Backlund, Andrei G. Baran, Elisabet I. Nielsen, Michael Speake, Janis Kuka, John Robinson, Solveiga Grinberga, Lindsay Robinson, Michael A. McDonough, Anna M. Rydzik, Thomas M. Leissing, Juan Carlos Jimenez-Castellanos, Matthew B. Avison, Solange Da Silva Pinto, Andrew D. Pannifer, Marina Martjuga, Emma Widlake, Martins Priede, Iva Hopkins Navratilova, Marek Gniadkowski, Anna Karin Belfrage, Peter Brandt, Jari Yli-Kauhaluoma, Eric Bacque, Malcolm G. P. Page, Fredrik Björkling, Jonathan M. Tyrrell, James Spencer, Pauline A. Lang, Pawel Baranczewski, Rafael Cantón, Stuart P. McElroy, Philip S. Jones, Fernando Baquero, Edgars Suna, Angus Morrison, Timothy R. Walsh, Christopher J. Schofield

Publikováno v: Brem, J, Panduwawala, T, Hansen, J U, Hewitt, J, Liepins, E, Donets, P, Espina, L, Farley, A J M, Shubin, K, Campillos, G G, Kiuru, P, Shishodia, S, Krahn, D, Leśniak, R K, Schmidt Adrian, J, Calvopiña, K, Turrientes, M-C, Kavanagh, M E, Lubriks, D, Hinchliffe, P, Langley, G W, Aboklaish, A F, Eneroth, A, Backlund, M, Baran, A G, Nielsen, E I, Speake, M, Kuka, J, Robinson, J, Grinberga, S, Robinson, L, McDonough, M A, Rydzik, A M, Leissing, T M, Jimenez-Castellanos, J C, Avison, M B, Da Silva Pinto, S, Pannifer, A D, Martjuga, M, Widlake, E, Priede, M, Hopkins Navratilova, I, Gniadkowski, M, Belfrage, A K, Brandt, P, Yli-Kauhaluoma, J, Bacque, E, Page, M G P, Björkling, F, Tyrrell, J M, Spencer, J, Lang, P A, Baranczewski, P, Cantón, R, McElroy, S P, Jones, P S, Baquero, F, Suna, E, Morrison, A, Walsh, T R & Schofield, C J 2022, ' Imitation of β-lactam binding enables broad-spectrum metallo-β-lactamase inhibitors ', Nature Chemistry, vol. 14, pp. 15-24 . https://doi.org/10.1038/s41557-021-00831-x

Carbapenems are vital antibiotics, but their efficacy is increasingly compromised by metallo-beta-lactamases (MBLs). Here we report the discovery and optimization of potent broad-spectrum MBL inhibitors. A high-throughput screen for NDM-1 inhibitors

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3b4fafe7a19ff7ed314c37086b73a558
https://research-information.bris.ac.uk/ws/files/323318874/IC_MBLinh_NatChem_accepted.pdf

Identification of A Novel Class of Benzofuran Oxoacetic Acid-Derived Ligands that Selectively Activate Cellular EPAC1

Autor: John Robinson, Stuart P. McElroy, Philip S. Jones, Graeme Barker, Euan Parnell, Helma Rutjes, Lindsay Robinson, Angus Morrison, Elizabeth M. Beck, Andrew D. Pannifer, Martin Timmerman, Angela Cowley, Jolanta Wiejak, Veronique Hamon, Holger Rehmann, Urszula Luchowska-Stańska, Jonathan Gillespie, David Morgan, Stephen J. Yarwood, Alison Porter, Pravin Mahajan

Publikováno v: Cells
Volume 8
Issue 11

Cyclic AMP promotes EPAC1 and EPAC2 activation through direct binding to a specific cyclic nucleotide-binding domain (CNBD) within each protein, leading to activation of Rap GTPases, which control multiple cell responses, including cell proliferation

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::677a116fcb1675edbcc36ca4fb30482f
https://pubmed.ncbi.nlm.nih.gov/31726720

The Joint European Compound Library: boosting precompetitive research

Autor: Andrew L. Hopkins, Jérémy Besnard, Philip S. Jones, Andrew D. Pannifer

Publikováno v: Drug Discovery Today. 20:181-186

The Joint European Compound Library (JECL) is a new high-throughput screening collection aimed at driving precompetitive drug discovery and target validation. The JECL has been established with a core of over 321,000 compounds from the proprietary co

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5c89f680feb25478e7dee555678b1300
https://doi.org/10.1016/j.drudis.2014.08.014

IMI European Lead Factory — democratizing access to high-throughput screening

Autor: Philip S. Jones, Sylviane Boucharens, Stuart P. McElroy, Angus Morrison, Saman Honarnejad, Stan van Boeckel, Helma van den Hurk, Daniel Basting, Jörg Hüser, Stefan Jaroch, Eckhard Ottow, Jorg Benningshof, Rutger H. A. Folmer, Frank Leemhuis, Patricia M. Kramer-Verhulst, Vera J. M. Nies, Kristina M. Orrling, Ton Rijnders, Claudia Pfander, Ola Engkvist, Garry Pairaudeau, Peter B. Simpson, Jean-Yves Ortholand, Didier Roche, Alexander Dömling, Sven M. Kühnert, Peter W. M. Roevens, Herman van Vlijmen, Eva J. A. van Wanrooij, Christophe Verbruggen, Peter Nussbaumer, Huib Ovaa, Mario van der Stelt, Klaus Baek Simonsen, Lena Tagmose, Herbert Waldmann, James Duffy, Dirk Finsinger, Mirek Jurzak, Nicola A. Burgess-Brown, Wen H. Lee, Floris P. J. T. Rutjes, Hubert Haag, Christopher Kallus, Hartmut Mors, Thierry Dorval, Brigitte Lesur, Fernando Ramon Olayo, Daniel Hamza, Geraint Jones, Christopher Pearce, Alexander Piechot, Dimitrios Tzalis, Mads H. Clausen, Jeremy Davis, Daphné Derouane, Céline Vermeiren, Markus Kaiser, Robert A. Stockman, Denise V. Barrault, Andrew D. Pannifer, Jason R. Swedlow, Adam S. Nelson, Romano V. A. Orru, Eelco Ruijter, Steven P. van Helden, Volkhart M. Li, Ton Vries, Jon S. B. de Vlieger

Publikováno v: Nature Reviews Drug Discovery
Nature Reviews. Drug Discovery, 21, 245-246
Nature Reviews. Drug Discovery, 21, 4, pp. 245-246

Contains fulltext : 252474.pdf (Publisher’s version ) (Open Access)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3d851dc3fb96708a39839a80c7c53a40