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Page 1
Polθ inhibitors elicit BRCA-gene synthetic lethality and target PARP inhibitor resistance.
Zatreanu D, Robinson HMR, Alkhatib O, Boursier M, Finch H, Geo L, Grande D, Grinkevich V, Heald RA, Langdon S, Majithiya J, McWhirter C, Martin NMB, Moore S, Neves J, Rajendra E, Ranzani M, Schaedler T, Stockley M, Wiggins K, Brough R, Sridhar S, Gulati A, Shao N, Badder LM, Novo D, Knight EG, Marlow R, Haider S, Callen E, Hewitt G, Schimmel J, Prevo R, Alli C, Ferdinand A, Bell C, Blencowe P, Bot C, Calder M, Charles M, Curry J, Ekwuru T, Ewings K, Krajewski W, MacDonald E, McCarron H, Pang L, Pedder C, Rigoreau L, Swarbrick M, Wheatley E, Willis S, Wong AC, Nussenzweig A, Tijsterman M, Tutt A, Boulton SJ, Higgins GS, Pettitt SJ, Smith GCM, Lord CJ. Zatreanu D, et al. Among authors: heald ra. Nat Commun. 2021 Jun 17;12(1):3636. doi: 10.1038/s41467-021-23463-8. Nat Commun. 2021. PMID: 34140467 Free PMC article.
Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta.
Stockley ML, Ferdinand A, Benedetti G, Blencowe P, Boyd SM, Calder M, Charles MD, Edwardes LV, Ekwuru T, Finch H, Galbiati A, Geo L, Grande D, Grinkevich V, Holliday ND, Krajewski WW, MacDonald E, Majithiya JB, McCarron H, McWhirter CL, Patel V, Pedder C, Rajendra E, Ranzani M, Rigoreau LJM, Robinson HMR, Schaedler T, Sirina J, Smith GCM, Swarbrick ME, Turnbull AP, Willis S, Heald RA. Stockley ML, et al. Among authors: heald ra. J Med Chem. 2022 Oct 27;65(20):13879-13891. doi: 10.1021/acs.jmedchem.2c01142. Epub 2022 Oct 6. J Med Chem. 2022. PMID: 36200480
Small-Molecule Polθ Inhibitors Provide Safe and Effective Tumor Radiosensitization in Preclinical Models.
Rodriguez-Berriguete G, Ranzani M, Prevo R, Puliyadi R, Machado N, Bolland HR, Millar V, Ebner D, Boursier M, Cerutti A, Cicconi A, Galbiati A, Grande D, Grinkevich V, Majithiya JB, Piscitello D, Rajendra E, Stockley ML, Boulton SJ, Hammond EM, Heald RA, Smith GCM, Robinson HMR, Higgins GS. Rodriguez-Berriguete G, et al. Among authors: heald ra. Clin Cancer Res. 2023 Apr 14;29(8):1631-1642. doi: 10.1158/1078-0432.CCR-22-2977. Clin Cancer Res. 2023. PMID: 36689546 Free PMC article.
Correction to "Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase Theta".
Stockley ML, Benedetti G, Blencowe P, Boulton SJ, Boyd SM, Calder M, Charles MD, Edwardes LV, Ekwuru T, Ferdinand A, Finch H, Galbiati A, Geo L, Grande D, Grinkevich V, Higgins GS, Holliday ND, Krajewski WW, MacDonald E, Majithiya JB, McCarron H, McWhirter CL, Patel V, Pedder C, Rajendra E, Ranzani M, Rigoreau LJM, Robinson HMR, Schaedler T, Sirina J, Smith GCM, Swarbrick ME, Turnbull AP, Willis S, Zemla A, Heald RA. Stockley ML, et al. Among authors: heald ra. J Med Chem. 2023 Feb 23. doi: 10.1021/acs.jmedchem.3c00204. Online ahead of print. J Med Chem. 2023. PMID: 36815444 No abstract available.
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers.
Hatzivassiliou G, Haling JR, Chen H, Song K, Price S, Heald R, Hewitt JF, Zak M, Peck A, Orr C, Merchant M, Hoeflich KP, Chan J, Luoh SM, Anderson DJ, Ludlam MJ, Wiesmann C, Ultsch M, Friedman LS, Malek S, Belvin M. Hatzivassiliou G, et al. Nature. 2013 Sep 12;501(7466):232-6. doi: 10.1038/nature12441. Epub 2013 Aug 11. Nature. 2013. PMID: 23934108
Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.
Chan BK, Hanan EJ, Bowman KK, Bryan MC, Burdick D, Chan E, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Shao L, Wang S, Yeap SK, Yen I, Yu C, Heffron TP. Chan BK, et al. Among authors: heald ra. J Med Chem. 2016 Oct 13;59(19):9080-9093. doi: 10.1021/acs.jmedchem.6b00995. Epub 2016 Sep 12. J Med Chem. 2016. PMID: 27564586
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoform.
Staben ST, Ndubaku C, Blaquiere N, Belvin M, Bull RJ, Dudley D, Edgar K, Gray D, Heald R, Heffron TP, Jones GE, Jones M, Kolesnikov A, Lee L, Lesnick J, Lewis C, Murray J, McLean NJ, Nonomiya J, Olivero AG, Ord R, Pang J, Price S, Prior WW, Rouge L, Salphati L, Sampath D, Wallin J, Wang L, Wei B, Weismann C, Wu P. Staben ST, et al. Bioorg Med Chem Lett. 2013 May 1;23(9):2606-13. doi: 10.1016/j.bmcl.2013.02.102. Epub 2013 Mar 7. Bioorg Med Chem Lett. 2013. PMID: 23540645
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Ndubaku CO, Heffron TP, Staben ST, Baumgardner M, Blaquiere N, Bradley E, Bull R, Do S, Dotson J, Dudley D, Edgar KA, Friedman LS, Goldsmith R, Heald RA, Kolesnikov A, Lee L, Lewis C, Nannini M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Wallin JJ, Wang L, Wei B, Sampath D, Olivero AG. Ndubaku CO, et al. Among authors: heald ra. J Med Chem. 2013 Jun 13;56(11):4597-610. doi: 10.1021/jm4003632. Epub 2013 Jun 3. J Med Chem. 2013. PMID: 23662903
Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.
Safina BS, Sweeney ZK, Li J, Chan BK, Bisconte A, Carrera D, Castanedo G, Flagella M, Heald R, Lewis C, Murray JM, Nonomiya J, Pang J, Price S, Reif K, Salphati L, Seward EM, Wei B, Sutherlin DP. Safina BS, et al. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4953-9. doi: 10.1016/j.bmcl.2013.06.052. Epub 2013 Jun 29. Bioorg Med Chem Lett. 2013. PMID: 23867164 Free article.
31 results