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Page 1
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Thomas MG, McGonagle K, Rowland P, Robinson DA, Dodd PG, Camino-Díaz I, Campbell L, Cantizani J, Castañeda P, Conn D, Craggs PD, Edwards D, Ferguson L, Fosberry A, Frame L, Goswami P, Hu X, Korczynska J, MacLean L, Martin J, Mutter N, Osuna-Cabello M, Paterson C, Peña I, Pinto EG, Pont C, Riley J, Shishikura Y, Simeons FRC, Stojanovski L, Thomas J, Wrobel K, Young RJ, Zmuda F, Zuccotto F, Read KD, Gilbert IH, Marco M, Miles TJ, Manzano P, De Rycker M. Thomas MG, et al. Among authors: young rj. J Med Chem. 2023 Aug 10;66(15):10413-10431. doi: 10.1021/acs.jmedchem.3c00582. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37506194 Free PMC article.
Targeting the Regulatory Site of ER Aminopeptidase 1 Leads to the Discovery of a Natural Product Modulator of Antigen Presentation.
Liddle J, Hutchinson JP, Kitchen S, Rowland P, Neu M, Cecconie T, Holmes DS, Jones E, Korczynska J, Koumantou D, Lea JD, Nickels L, Pemberton M, Phillipou A, Schneck JL, Sheehan H, Tinworth CP, Uings I, Wojno-Picon J, Young RJ, Stratikos E. Liddle J, et al. Among authors: young rj. J Med Chem. 2020 Mar 26;63(6):3348-3358. doi: 10.1021/acs.jmedchem.9b02123. Epub 2020 Mar 9. J Med Chem. 2020. PMID: 32109056
Mycobacterium tuberculosis Decaprenylphosphoryl-β-d-ribose Oxidase Inhibitors: Expeditious Reconstruction of Suboptimal Hits into a Series with Potent in Vivo Activity.
Borthwick JA, Alemparte C, Wall I, Whitehurst BC, Argyrou A, Burley G, de Dios-Anton P, Guijarro L, Monteiro MC, Ortega F, Suckling CJ, Pichel JC, Cacho M, Young RJ. Borthwick JA, et al. Among authors: young rj. J Med Chem. 2020 Mar 12;63(5):2557-2576. doi: 10.1021/acs.jmedchem.9b01561. Epub 2020 Jan 22. J Med Chem. 2020. PMID: 31922409 Free article.
Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies.
Simpson GL, Bertrand SM, Borthwick JA, Campobasso N, Chabanet J, Chen S, Coggins J, Cottom J, Christensen SB, Dawson HC, Evans HL, Hobbs AN, Hong X, Mangatt B, Munoz-Muriedas J, Oliff A, Qin D, Scott-Stevens P, Ward P, Washio Y, Yang J, Young RJ. Simpson GL, et al. Among authors: young rj. J Med Chem. 2019 Feb 28;62(4):2154-2171. doi: 10.1021/acs.jmedchem.8b01872. Epub 2019 Feb 11. J Med Chem. 2019. PMID: 30689376
New direct inhibitors of InhA with antimycobacterial activity based on a tetrahydropyran scaffold.
Pajk S, Živec M, Šink R, Sosič I, Neu M, Chung CW, Martínez-Hoyos M, Pérez-Herrán E, Álvarez-Gómez D, Álvarez-Ruíz E, Mendoza-Losana A, Castro-Pichel J, Barros D, Ballell-Pages L, Young RJ, Convery MA, Encinas L, Gobec S. Pajk S, et al. Among authors: young rj. Eur J Med Chem. 2016 Apr 13;112:252-257. doi: 10.1016/j.ejmech.2016.02.008. Epub 2016 Feb 8. Eur J Med Chem. 2016. PMID: 26900657
The Mechanism of Acetyl Transfer Catalyzed by Mycobacterium tuberculosis GlmU.
Craggs PD, Mouilleron S, Rejzek M, de Chiara C, Young RJ, Field RA, Argyrou A, de Carvalho LPS. Craggs PD, et al. Among authors: young rj. Biochemistry. 2018 Jun 19;57(24):3387-3401. doi: 10.1021/acs.biochem.8b00121. Epub 2018 May 2. Biochemistry. 2018. PMID: 29684272 Free PMC article.
Structure guided drug design to develop kallikrein 5 inhibitors to treat Netherton syndrome.
Walker AL, Bingham RP, Edgar EV, Ferrie A, Holmes DS, Liddle J, Polyakova O, Rella M, Smith KJ, Thorpe JH, Wang Y, White GV, Young RJ, Hovnanian A. Walker AL, et al. Among authors: young rj. Bioorg Med Chem Lett. 2019 Jun 15;29(12):1454-1458. doi: 10.1016/j.bmcl.2019.04.022. Epub 2019 Apr 12. Bioorg Med Chem Lett. 2019. PMID: 31005442
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.
Chan C, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chung CW, Convery MA, Hamblin JN, Johnstone L, Kelly HA, Kleanthous S, Patikis A, Patel C, Pateman AJ, Senger S, Shah GP, Toomey JR, Watson NS, Weston HE, Whitworth C, Young RJ, Zhou P. Chan C, et al. Among authors: young rj. J Med Chem. 2007 Apr 5;50(7):1546-57. doi: 10.1021/jm060870c. Epub 2007 Mar 6. J Med Chem. 2007. PMID: 17338508
The Discovery of in Vivo Active Mitochondrial Branched-Chain Aminotransferase (BCATm) Inhibitors by Hybridizing Fragment and HTS Hits.
Bertrand SM, Ancellin N, Beaufils B, Bingham RP, Borthwick JA, Boullay AB, Boursier E, Carter PS, Chung CW, Churcher I, Dodic N, Fouchet MH, Fournier C, Francis PL, Gummer LA, Herry K, Hobbs A, Hobbs CI, Homes P, Jamieson C, Nicodeme E, Pickett SD, Reid IH, Simpson GL, Sloan LA, Smith SE, Somers DO, Spitzfaden C, Suckling CJ, Valko K, Washio Y, Young RJ. Bertrand SM, et al. Among authors: young rj. J Med Chem. 2015 Sep 24;58(18):7140-63. doi: 10.1021/acs.jmedchem.5b00313. Epub 2015 Jul 2. J Med Chem. 2015. PMID: 26090771
726 results