Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Jacob T. Bush"'
Autor:
Péter Ábrányi-Balogh, Dávid Bajusz, Zoltán Orgován, Aaron B. Keeley, László Petri, Nikolett Péczka, Tibor Viktor Szalai, Gyula Pálfy, Márton Gadanecz, Emma K. Grant, Tímea Imre, Tamás Takács, Ivan Ranđelović, Marcell Baranyi, András Marton, Gitta Schlosser, Qirat F. Ashraf, Elvin D. de Araujo, Tamás Karancsi, László Buday, József Tóvári, András Perczel, Jacob T. Bush, György M. Keserű
Publikováno v:
Communications Chemistry, Vol 7, Iss 1, Pp 1-13 (2024)
Abstract Fragment screening is a popular strategy of generating viable chemical starting points especially for challenging targets. Although fragments provide a better coverage of chemical space and they have typically higher chance of binding, their
Externí odkaz:
https://doaj.org/article/0a79f05dcd144d4ba343eaa1f806db99
Autor:
Ross P. Thomas, Emma K. Grant, Eleanor R. Dickinson, Francesca Zappacosta, Lee J. Edwards, Michael M. Hann, David House, Nicholas C. O. Tomkinson, Jacob T. Bush
Publikováno v:
RSC Medicinal Chemistry. 14:671-679
We present a carboxylate-targeting reactive fragment screening platform using 2-aryl-5-carboxytetrazole (ACT) as the photoreactive functionality. This work will provide a simple accessible method to rapidly discover tool molecules to interrogate impo
Autor:
Arron Aatkar, Aini Vuorinen, Oliver E. Longfield, Katharine Gilbert, Rachel Peltier-Heap, Craig D. Wagner, Francesca Zappacosta, Katrin Rittinger, Chun-wa Chung, David House, Nicholas C. O. Tomkinson, Jacob T. Bush
Publikováno v:
ACS Chemical Biology.
Sulfur(VI) fluorides (SFs) have emerged as valuable electrophiles for the design of 'beyond cysteine' covalent inhibitors, and offer potential for expansion of the liganded proteome. Since SFs target a broad range of nucleophilic amino acids, they de
Autor:
Rosa Cookson, Aini Vuorinen, Jonathan Pettinger, Cassandra R. Kennedy, Joanna M. Kirkpatrick, Rachel E. Peltier-Heap, Andrew Powell, Ambrosius P. Snijders, Mark Skehel, David House, Katrin Rittinger, Jacob T. Bush
SummaryChemoproteomics is a powerful method capable of detecting interactions between small molecules and the proteome, however its use as a high-throughput screening method for chemical libraries has so far been limited. To address this need, we hav
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9ff8aafd003a34329baeafd8d02f1023
https://doi.org/10.1101/2023.02.01.526632
https://doi.org/10.1101/2023.02.01.526632
Autor:
Katharine E. Gilbert, Aini Vuorinen, Arron Aatkar, Peter Pogány, Jonathan Pettinger, Emma K. Grant, Joanna M. Kirkpatrick, Katrin Rittinger, David House, Glenn A. Burley, Jacob T. Bush
A comprehensive profiling of sulfur(VI) fluoride reactivity is reported in the context of fragment binders and optimized probes. The reactivity profile of an SVI-F panel is demonstrated using live cell chemoproteomics. The studies provide an in-depth
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59458f436898af2b214b686cc11b1373
Autor:
Marcus Bantscheff, Christian Eberl, Chun-wa Chung, Nicholas C. O. Tomkinson, Stephanie Lehmann, Ken G. M. Fantom, Jacob T. Bush, Alex Phillipou, Christopher J. Schofield, Francesca Zappacosta, David J. Fallon, Vipulkumar Kantibhai Patel
Publikováno v:
Chemistry – A European Journal. 27:17880-17888
We present a one-step Ugi reaction protocol for the expedient synthesis of photoaffinity probes for live-cell MS-based proteomics. The reaction couples an amine affinity function with commonly used photoreactive groups, and a variety of handle functi
Autor:
Emma K. Grant, Francesca Zappacosta, Peter Pogány, Michael M. Hann, Nicholas C. O. Tomkinson, David House, Ross P. Thomas, Jacob T. Bush, David J. Fallon, Rachel E. Heap, Stephen Besley
Publikováno v:
Chemical Science
Methods for rapid identification of chemical tools are essential for the validation of emerging targets and to provide medicinal chemistry starting points for the development of new medicines. Here, we report a screening platform that combines ‘dir
Autor:
Jacob T Bush, Monique Wasunna, Fabiana Alves, Jorge Alvar, Piero L Olliaro, Michael Otieno, Carol Hopkins Sibley, Nathalie Strub Wourgaft, Philippe J Guerin
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 11, Iss 9, p e0005781 (2017)
There are an estimated 200,000 to 400,000 cases of visceral leishmaniasis (VL) annually. A variety of factors are taken into account when considering the best therapeutic options to cure a patient and reduce the risk of resistance, including geograph
Externí odkaz:
https://doaj.org/article/0c9877163c4a4391b8df04218b9eb8c7
Autor:
Emma Campbell, Andrea Taladriz-Sender, Olivia I. Paisley, Alan R. Kennedy, Jacob T. Bush, Glenn A. Burley
A modular approach to prepare tri- and tetracyclic carbazoles by a sequential [3 + 2]heteroannulation is described. First, optimization of Pd-catalyzed Buchwald-Hartwig amination followed by C/N-arylation in a one-pot process is established. Second,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc27d72c27da62134ba39f17bdda2a09
https://strathprints.strath.ac.uk/79949/1/Campbell_etal_JOC_2022_A_chemo_and_regioselective_tandem_heteroannulation_strategy_for_carbazole_synthesis.pdf
https://strathprints.strath.ac.uk/79949/1/Campbell_etal_JOC_2022_A_chemo_and_regioselective_tandem_heteroannulation_strategy_for_carbazole_synthesis.pdf
Autor:
Yoshiaki Washio, Alan Nadin, Mike Barker, Peter Pogány, Darren V. S. Green, Gemma V. White, Anthony W. J. Cooper, Stephen D. Pickett, Graham George Adam Inglis, Sebastien Andre Campos, Jacob T. Bush, Darren L Poole, John Pritchard, Vipulkumar Kantibhai Patel, Andrew Baxter, David Jonathan Hirst
Publikováno v:
Journal of Medicinal Chemistry. 63:11964-11971
Machine learning approaches promise to accelerate and improve success rates in medicinal chemistry programs by more effectively leveraging available data to guide a molecular design. A key step of an automated computational design algorithm is molecu