Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Aaron Keeley"'
Autor:
László Petri, Péter Ábrányi-Balogh, Noémi Csorba, Aaron Keeley, József Simon, Ivan Ranđelović, József Tóvári, Gitta Schlosser, Dániel Szabó, László Drahos, György M. Keserű
Publikováno v:
Molecules, Vol 28, Iss 7, p 3042 (2023)
SuFEx chemistry is based on the unique reactivity of the sulfonyl fluoride group with a range of nucleophiles. Accordingly, sulfonyl fluorides label multiple nucleophilic amino acid residues, making these reagents popular in both chemical biology and
Externí odkaz:
https://doaj.org/article/c77c5ffab3114b2793cf463335f0bda9
Autor:
Alice Douangamath, Daren Fearon, Paul Gehrtz, Tobias Krojer, Petra Lukacik, C. David Owen, Efrat Resnick, Claire Strain-Damerell, Anthony Aimon, Péter Ábrányi-Balogh, José Brandão-Neto, Anna Carbery, Gemma Davison, Alexandre Dias, Thomas D. Downes, Louise Dunnett, Michael Fairhead, James D. Firth, S. Paul Jones, Aaron Keeley, György M. Keserü, Hanna F. Klein, Mathew P. Martin, Martin E. M. Noble, Peter O’Brien, Ailsa Powell, Rambabu N. Reddi, Rachael Skyner, Matthew Snee, Michael J. Waring, Conor Wild, Nir London, Frank von Delft, Martin A. Walsh
Publikováno v:
Nature Communications, Vol 11, Iss 1, Pp 1-11 (2020)
The SARS-CoV-2 main protease is an important target for the development of COVID-19 therapeutics. Here, the authors combine X-ray crystallography and mass spectrometry and performed a large scale fragment screening campaign, which yielded 96 liganded
Externí odkaz:
https://doaj.org/article/d499338758524d99942f9963faf75661
Autor:
Péter Ábrányi-Balogh, Aaron Keeley, György G. Ferenczy, László Petri, Tímea Imre, Katarina Grabrijan, Martina Hrast, Damijan Knez, Janez Ilaš, Stanislav Gobec, György M. Keserű
Publikováno v:
Pharmaceuticals, Vol 15, Iss 12, p 1484 (2022)
Heterocyclic electrophiles as small covalent fragments showed promising inhibitory activity on the antibacterial target MurA (UDP-N-acetylglucosamine 1-carboxyvinyltransferase, EC:2.5.1.7). Here, we report the second generation of heterocyclic electr
Externí odkaz:
https://doaj.org/article/df22a37fca3f4388a828d755b3209126
Autor:
David J. Hamilton, Péter Ábrányi-Balogh, Aaron Keeley, László Petri, Martina Hrast, Tímea Imre, Maikel Wijtmans, Stanislav Gobec, Iwan J. P. de Esch, György Miklós Keserű
Publikováno v:
Pharmaceuticals, Vol 13, Iss 11, p 362 (2020)
Drug discovery programs against the antibacterial target UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) have already resulted in covalent inhibitors having small three- and five-membered heterocyclic rings. In the current study, the reactivit
Externí odkaz:
https://doaj.org/article/6dd80a358b834ae49f8f35767510ca13
Publikováno v:
MedChemComm
A fragment library of electrophilic small heterocycles was characterized through cysteine-reactivity and aqueous stability tests that suggested their potential as covalent warheads.
A fragment library of electrophilic small heterocycles was char
A fragment library of electrophilic small heterocycles was char
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53c3459695fe2c1722bdb90dcb7e56c3
https://doi.org/10.1039/c8md00327k
https://doi.org/10.1039/c8md00327k
Autor:
Peter O'Brien, C. David Owen, Alice Douangamath, Louise Dunnett, Efrat Resnick, Mathew P. Martin, P. Gehrtz, R. Skyner, José Brandão-Neto, Nir London, Martin A. Walsh, Petra Lukacik, S. Paul Jones, Péter Ábrányi-Balogh, James D. Firth, M. Snee, Rambabu N. Reddi, Anna Carbery, D. Fearon, Aaron Keeley, Hanna F. Klein, T. Krojer, Gemma Davison, Frank von Delft, Conor Wild, Michael J. Waring, A.J. Powell, Martin E.M. Noble, G.M. Keseru, Claire Strain-Damerell, A. Aimon, Thomas D. Downes, Alexandre Dias, Michael Fairhead
Publikováno v:
Nature Communications
Nature Communications, Vol 11, Iss 1, Pp 1-11 (2020)
Nature Communications, Vol 11, Iss 1, Pp 1-11 (2020)
COVID-19, caused by SARS-CoV-2, lacks effective therapeutics. Additionally, no antiviral drugs or vaccines were developed against the closely related coronavirus, SARS-CoV-1 or MERS-CoV, despite previous zoonotic outbreaks. To identify starting point
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0901607193d626009824417763fb3128
https://doi.org/10.1101/2020.05.27.118117
https://doi.org/10.1101/2020.05.27.118117
Publikováno v:
Drug Discovery Today
Targeted covalent inhibitors and chemical probes have become integral parts of drug discovery approaches. Given the advantages of fragment-based drug discovery, screening electrophilic fragments emerged as a promising alternative to discover and vali
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::efc9304c54f9bbffffe5254a22f71fcc
Publikováno v:
Tetrahedron. 72:2552-2559
The combination of ring closing, or enyne metathesis with oxidation in order to prepare N-sulfonyl pyrroles is described. Reasonable to good yields were obtained for a variety of substituents and the procedure may also be conducted in one-pot. 2-Brom
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::450b5881a33b040188c0752f2f20bf38
https://doi.org/10.1016/j.tet.2016.03.088
https://doi.org/10.1016/j.tet.2016.03.088
Autor:
Stanislav Gobec, Péter Ábrányi-Balogh, Iwan J. P. de Esch, László Petri, Martina Hrast, Aaron Keeley, David J. Hamilton, György M. Keserű, Maikel Wijtmans, Tímea Imre
Publikováno v:
Pharmaceuticals, vol. 13, no. 11, 362, 2020.
Pharmaceuticals, 13(11):362, 1-14. Multidisciplinary Digital Publishing Institute (MDPI)
Hamilton, D J, Ábrányi-Balogh, P, Keeley, A, Petri, L, Hrast, M, Imre, T, Wijtmans, M, Gobec, S, de Esch, I J P & Keserű, G M 2020, ' Bromo-cyclobutenaminones as new covalent udp-n-acetylglucosamine enolpyruvyl transferase (Mura) inhibitors ', Pharmaceuticals, vol. 13, no. 11, 362, pp. 1-14 . https://doi.org/10.3390/ph13110362
Pharmaceuticals, Vol 13, Iss 362, p 362 (2020)
Pharmaceuticals, 13(11):362, 1-14. Multidisciplinary Digital Publishing Institute (MDPI)
Hamilton, D J, Ábrányi-Balogh, P, Keeley, A, Petri, L, Hrast, M, Imre, T, Wijtmans, M, Gobec, S, de Esch, I J P & Keserű, G M 2020, ' Bromo-cyclobutenaminones as new covalent udp-n-acetylglucosamine enolpyruvyl transferase (Mura) inhibitors ', Pharmaceuticals, vol. 13, no. 11, 362, pp. 1-14 . https://doi.org/10.3390/ph13110362
Pharmaceuticals, Vol 13, Iss 362, p 362 (2020)
Drug discovery programs against the antibacterial target UDP-N-acetylglucosamine enolpyruvyl transferase (MurA) have already resulted in covalent inhibitors having small three- and five-membered heterocyclic rings. In the current study, the reactivit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4fd3ef395cfbf8d8b219e2d8e2f45204
https://doi.org/10.3390/ph13110362
https://doi.org/10.3390/ph13110362
Autor:
Janez Ilaš, Aaron Keeley, Péter Ábrányi-Balogh, Tímea Imre, Stanislav Gobec, György M. Keserű, Martina Hrast
Publikováno v:
Archiv der Pharmazie. 351(12)
An electrophilic fragment library of small heterocycles was developed and characterized in the surrogate GSH-reactivity assay and aqueous stability test that revealed their potential as covalent warheads. Screening the library against MurA from Staph
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::391915c803c15ef5535b9c479e3ea23c
https://pubmed.ncbi.nlm.nih.gov/30461051
https://pubmed.ncbi.nlm.nih.gov/30461051