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Table representation of search results timeline featuring number of search results per year.

Year Number of Results
2001 1
2002 1
2003 3
2004 1
2005 3
2006 1
2007 1
2008 1
2009 1
2012 1
2013 1
2014 1
2016 2
2017 1
2021 1
2022 2
2023 2
2024 1

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23 results

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Page 1
Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.
Hanan EJ, Braun MG, Heald RA, MacLeod C, Chan C, Clausen S, Edgar KA, Eigenbrot C, Elliott R, Endres N, Friedman LS, Gogol E, Gu XH, Thibodeau RH, Jackson PS, Kiefer JR, Knight JD, Nannini M, Narukulla R, Pace A, Pang J, Purkey HE, Salphati L, Sampath D, Schmidt S, Sideris S, Song K, Sujatha-Bhaskar S, Ultsch M, Wallweber H, Xin J, Yeap S, Young A, Zhong Y, Staben ST. Hanan EJ, et al. Among authors: heald ra. J Med Chem. 2022 Dec 22;65(24):16589-16621. doi: 10.1021/acs.jmedchem.2c01422. Epub 2022 Dec 1. J Med Chem. 2022. PMID: 36455032
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.
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.
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, 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
Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.
Safina BS, Elliott RL, Forrest AK, Heald RA, Murray JM, Nonomiya J, Pang J, Salphati L, Seward EM, Staben ST, Ultsch M, Wei B, Yang W, Sutherlin DP. Safina BS, et al. Among authors: heald ra. ACS Med Chem Lett. 2017 Aug 25;8(9):936-940. doi: 10.1021/acsmedchemlett.7b00170. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947940 Free PMC article.
Recognition and Stabilization of Quadruplex DNA by a Potent New Telomerase Inhibitor: NMR Studies of the 2:1 Complex of a Pentacyclic Methylacridinium Cation with d(TTAGGGT)(4) We thank the EPSRC of the UK and AstraZeneca for financial support to E.G. M.F.G.S. and R.A.H. are supported by the Cancer Research Campaign of the UK.
Gavathiotis E, Heald RA, Stevens MF, Searle MS. Gavathiotis E, et al. Among authors: heald ra. Angew Chem Int Ed Engl. 2001 Dec 17;40(24):4749-4751. doi: 10.1002/1521-3773(20011217)40:24<4749::aid-anie4749>3.0.co;2-i. Angew Chem Int Ed Engl. 2001. PMID: 12404405 No abstract available.
5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
Morley AD, Kenny PW, Burton B, Heald RA, Macfaul PA, Mullett J, Page K, Porres SS, Ribeiro LR, Smith P, Ward S, Wilkinson TJ. Morley AD, et al. Among authors: heald ra. Bioorg Med Chem Lett. 2009 Mar 15;19(6):1658-61. doi: 10.1016/j.bmcl.2009.01.110. Epub 2009 Feb 6. Bioorg Med Chem Lett. 2009. PMID: 19231183
23 results