Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta

Autor:	Martin L. Stockley, Amanda Ferdinand, Giovanni Benedetti, Peter Blencowe, Susan M. Boyd, Mat Calder, Mark D. Charles, Lucy V. Edwardes, Tennyson Ekwuru, Harry Finch, Alessandro Galbiati, Lerin Geo, Diego Grande, Vera Grinkevich, Nicholas D. Holliday, Wojciech W. Krajewski, Ellen MacDonald, Jayesh B. Majithiya, Hollie McCarron, Claire L. McWhirter, Viral Patel, Chris Pedder, Eeson Rajendra, Marco Ranzani, Laurent J. M. Rigoreau, Helen M. R. Robinson, Theresia Schaedler, Julija Sirina, Graeme C. M. Smith, Martin E. Swarbrick, Andrew P. Turnbull, Simon Willis, Robert A. Heald
Rok vydání:	2022
Předmět:	DNA End-Joining Repair Drug Discovery Humans Molecular Medicine DNA Poly(ADP-ribose) Polymerase Inhibitors Ligands
Zdroj:	Journal of Medicinal Chemistry. 65:13879-13891
ISSN:	1520-4804 0022-2623
DOI:	10.1021/acs.jmedchem.2c01142
Popis:	Human DNA polymerase theta (Polθ), which is essential for microhomology-mediated DNA double strand break repair, has been proposed as an attractive target for the treatment of BRCA deficient and other DNA repair pathway defective cancers. As previously reported, we recently identified the first selective small molecule Polθ in vitro probe
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a3234589eaa7f5350d23a2af196b12e https://doi.org/10.1021/acs.jmedchem.2c01142 Zobrazit plný text záznamu