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Page 1
Structure-Guided Discovery of a Selective Mcl-1 Inhibitor with Cellular Activity.
Szlávik Z, Ondi L, Csékei M, Paczal A, Szabó ZB, Radics G, Murray J, Davidson J, Chen I, Davis B, Hubbard RE, Pedder C, Dokurno P, Surgenor A, Smith J, Robertson A, LeToumelin-Braizat G, Cauquil N, Zarka M, Demarles D, Perron-Sierra F, Claperon A, Colland F, Geneste O, Kotschy A. Szlávik Z, et al. Among authors: pedder c. J Med Chem. 2019 Aug 8;62(15):6913-6924. doi: 10.1021/acs.jmedchem.9b00134. Epub 2019 Jul 24. J Med Chem. 2019. PMID: 31339316
The MCL1 inhibitor S63845 is tolerable and effective in diverse cancer models.
Kotschy A, Szlavik Z, Murray J, Davidson J, Maragno AL, Le Toumelin-Braizat G, Chanrion M, Kelly GL, Gong JN, Moujalled DM, Bruno A, Csekei M, Paczal A, Szabo ZB, Sipos S, Radics G, Proszenyak A, Balint B, Ondi L, Blasko G, Robertson A, Surgenor A, Dokurno P, Chen I, Matassova N, Smith J, Pedder C, Graham C, Studeny A, Lysiak-Auvity G, Girard AM, Gravé F, Segal D, Riffkin CD, Pomilio G, Galbraith LC, Aubrey BJ, Brennan MS, Herold MJ, Chang C, Guasconi G, Cauquil N, Melchiore F, Guigal-Stephan N, Lockhart B, Colland F, Hickman JA, Roberts AW, Huang DC, Wei AH, Strasser A, Lessene G, Geneste O. Kotschy A, et al. Among authors: pedder c. Nature. 2016 Oct 27;538(7626):477-482. doi: 10.1038/nature19830. Epub 2016 Oct 19. Nature. 2016. PMID: 27760111
The Effect of Core Replacement on S64315, a Selective MCL-1 Inhibitor, and Its Analogues.
Sipos S, Bálint B, Szabó ZB, Ondi L, Csékei M, Szlávik Z, Proszenyák Á, Murray JB, Davidson J, Chen I, Dokurno P, Surgenor AE, Pedder C, Hubbard RE, Maragno AL, Chanrion M, Colland F, Geneste O, Kotschy A. Sipos S, et al. Among authors: pedder c. ACS Omega. 2021 Aug 18;6(34):22073-22102. doi: 10.1021/acsomega.1c02595. eCollection 2021 Aug 31. ACS Omega. 2021. PMID: 34497901 Free PMC article.
S55746 is a novel orally active BCL-2 selective and potent inhibitor that impairs hematological tumor growth.
Casara P, Davidson J, Claperon A, Le Toumelin-Braizat G, Vogler M, Bruno A, Chanrion M, Lysiak-Auvity G, Le Diguarher T, Starck JB, Chen I, Whitehead N, Graham C, Matassova N, Dokurno P, Pedder C, Wang Y, Qiu S, Girard AM, Schneider E, Gravé F, Studeny A, Guasconi G, Rocchetti F, Maïga S, Henlin JM, Colland F, Kraus-Berthier L, Le Gouill S, Dyer MJS, Hubbard R, Wood M, Amiot M, Cohen GM, Hickman JA, Morris E, Murray J, Geneste O. Casara P, et al. Among authors: pedder c. Oncotarget. 2018 Apr 13;9(28):20075-20088. doi: 10.18632/oncotarget.24744. eCollection 2018 Apr 13. Oncotarget. 2018. PMID: 29732004 Free PMC article.
Establishing Drug Discovery and Identification of Hit Series for the Anti-apoptotic Proteins, Bcl-2 and Mcl-1.
Murray JB, Davidson J, Chen I, Davis B, Dokurno P, Graham CJ, Harris R, Jordan A, Matassova N, Pedder C, Ray S, Roughley SD, Smith J, Walmsley C, Wang Y, Whitehead N, Williamson DS, Casara P, Le Diguarher T, Hickman J, Stark J, Kotschy A, Geneste O, Hubbard RE. Murray JB, et al. Among authors: pedder c. ACS Omega. 2019 May 23;4(5):8892-8906. doi: 10.1021/acsomega.9b00611. eCollection 2019 May 31. ACS Omega. 2019. PMID: 31459977 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: pedder c. 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
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: pedder c. Nat Commun. 2021 Jun 17;12(1):3636. doi: 10.1038/s41467-021-23463-8. Nat Commun. 2021. PMID: 34140467 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: pedder c. 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.
13 results