Zobrazeno 1 - 5
of 5
pro vyhledávání: '"Kevin J. Gillen"'
Autor:
Timothée Constantin, Bartosz Górski, Michael J. Tilby, Saloua Chelli, Fabio Juliá, Josep Llaveria, Kevin J. Gillen, Hendrik Zipse, Sami Lakhdar, Daniele Leonori
Publikováno v:
Constantin, T, Górski, B, Tilby, M J, Chelli, S, Julia Hernandez, F, Llaveria, J, Gillen, K J, Zipse, H, Lakhdar, S & Leonori, D 2022, ' Halogen-atom and group transfer reactivity enabled by hydrogen tunneling ', Science, vol. 377, no. 6612, pp. 1323-1328 . https://doi.org/10.1126/science.abq8663
The generation of carbon radicals by halogen-atom and group transfer reactions is generally achieved using tin and silicon reagents that maximize the interplay of enthalpic (thermodynamic) and polar (kinetic) effects. In this work, we demonstrate a d
Autor:
Elizabeth A. Love, Seema Patel, Andy Merritt, Kevin J. Gillen, Hannah Cook, Jonathan M. Large, David Matthews, Afrah Sattikar
Publikováno v:
Chembiochem
Antibody–drug conjugates (ADCs) are a growing class of therapeutics that harness the specificity of antibodies and the cell‐killing potency of small‐molecule drugs. Beyond cytotoxics, there are few examples of the application of an ADC approach
Autor:
Janet Brownlees, David W. Melton, Timothy M. Chapman, Puneet Khurana, Emilie A. Bureau, Simon Fox, Claire Wallace, Preeti Bakrania, P.J. Coombs, Kevin J. Gillen, Barbara Saxty
Publikováno v:
Chapman, T M, Wallace, C, Gillen, K J, Bakrania, P, Khurana, P, Coombs, P J, Fox, S, Bureau, E A, Brownlees, J, Melton, D & Saxty, B 2015, ' N-Hydroxyimides and hydroxypyrimidinones as inhibitors of the DNA repair complex ERCC1-XPF ', Bioorganic & Medicinal Chemistry Letters, vol. 25, no. 19 . https://doi.org/doi:10.1016/j.bmcl.2015.08.024
A high throughput screen allowed the identification of N-hydroxyimide inhibitors of ERCC1-XPF endonuclease activity with micromolar potency, but they showed undesirable selectivity profiles against FEN-1. A scaffold hop to a hydroxypyrimidinone templ
Autor:
Barbara Saxty, Simon Fox, Timothy M. Chapman, Maximillian T. W. Lee, David W. Melton, Emilie A. Bureau, Preeti Bakrania, Janet Brownlees, Kevin J. Gillen, P.J. Coombs, Claire Wallace, Laura Stennett, Puneet Khurana
Publikováno v:
Chapman, T M, Gillen, K J, Wallace, C, Lee, M T, Bakrania, P, Khurana, P, Coombs, P J, Stennett, L, Fox, S, Bureau, E A, Brownlees, J, Melton, D & Saxty, B 2015, ' Catechols and 3-hydroxypyridones as inhibitors of the DNA repair complex ERCC1-XPF ', Bioorganic & Medicinal Chemistry Letters . https://doi.org/doi:10.1016/j.bmcl.2015.08.031
Catechol-based inhibitors of ERCC1-XPF endonuclease activity were identified from a high-throughput screen. Exploration of the structure-activity relationships within this series yielded compound 13, which displayed an ERCC1-XPF IC50 of 0.6 μM, high
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11a4dad0c8c4ff0e532853e549f314dc
https://www.pure.ed.ac.uk/ws/files/21295310/Chapman_submission_1_main_R1.pdf
https://www.pure.ed.ac.uk/ws/files/21295310/Chapman_submission_1_main_R1.pdf
Autor:
Alison Levy, Michelle Newman, Chido Mpamhanga, Debra L. Taylor, Denise J. Harding, Gareth Hall, Ed Mclver, Kevin J. Gillen, Andy Merritt, Joanne Osborne, Stephen John Lewis, Janet Brownlees
Publikováno v:
Molecular Neurodegeneration
The four MARK (microtubule affinity regulating kinase) kinases (MARKs 1-4) are an evolutionary conserved group of proteins, which belong to the AMPK-related protein kinase family and are involved in the regulation of cell polarity. MARKs are highly e