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Page 1
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: heightman td. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Discovery of ASTX029, A Clinical Candidate Which Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Bevan L, Buck IM, Carr MG, Courtin A, Coyle JE, Day JEH, East C, Fazal L, Griffiths-Jones CM, Howard S, Kucia-Tran J, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Peakman TM, Reader M, Rees DC, Rich SJ, Shah A, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Heightman TD, et al. J Med Chem. 2021 Aug 26;64(16):12286-12303. doi: 10.1021/acs.jmedchem.1c00905. Epub 2021 Aug 13. J Med Chem. 2021. PMID: 34387469
Monoacidic Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction with High Cell Potency Identified by Fragment-Based Discovery.
Davies TG, Wixted WE, Coyle JE, Griffiths-Jones C, Hearn K, McMenamin R, Norton D, Rich SJ, Richardson C, Saxty G, Willems HM, Woolford AJ, Cottom JE, Kou JP, Yonchuk JG, Feldser HG, Sanchez Y, Foley JP, Bolognese BJ, Logan G, Podolin PL, Yan H, Callahan JF, Heightman TD, Kerns JK. Davies TG, et al. Among authors: heightman td. J Med Chem. 2016 Apr 28;59(8):3991-4006. doi: 10.1021/acs.jmedchem.6b00228. Epub 2016 Apr 12. J Med Chem. 2016. PMID: 27031670
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP).
Tamanini E, Buck IM, Chessari G, Chiarparin E, Day JEH, Frederickson M, Griffiths-Jones CM, Hearn K, Heightman TD, Iqbal A, Johnson CN, Lewis EJ, Martins V, Peakman T, Reader M, Rich SJ, Ward GA, Williams PA, Wilsher NE. Tamanini E, et al. Among authors: heightman td. J Med Chem. 2017 Jun 8;60(11):4611-4625. doi: 10.1021/acs.jmedchem.6b01877. Epub 2017 May 24. J Med Chem. 2017. PMID: 28492317
Fragment-Based Discovery of a Potent, Orally Bioavailable Inhibitor That Modulates the Phosphorylation and Catalytic Activity of ERK1/2.
Heightman TD, Berdini V, Braithwaite H, Buck IM, Cassidy M, Castro J, Courtin A, Day JEH, East C, Fazal L, Graham B, Griffiths-Jones CM, Lyons JF, Martins V, Muench S, Munck JM, Norton D, O'Reilly M, Palmer N, Pathuri P, Reader M, Rees DC, Rich SJ, Richardson C, Saini H, Thompson NT, Wallis NG, Walton H, Wilsher NE, Woolford AJ, Cooke M, Cousin D, Onions S, Shannon J, Watts J, Murray CW. Heightman TD, et al. J Med Chem. 2018 Jun 14;61(11):4978-4992. doi: 10.1021/acs.jmedchem.8b00421. Epub 2018 May 31. J Med Chem. 2018. PMID: 29775310
Fragment-Guided Discovery of Pyrazole Carboxylic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1: Nuclear Factor Erythroid 2 Related Factor 2 (KEAP1:NRF2) Protein-Protein Interaction.
Norton D, Bonnette WG, Callahan JF, Carr MG, Griffiths-Jones CM, Heightman TD, Kerns JK, Nie H, Rich SJ, Richardson C, Rumsey W, Sanchez Y, Verdonk ML, Willems HMG, Wixted WE, Wolfe L 3rd, Woolford AJ, Wu Z, Davies TG. Norton D, et al. Among authors: heightman td. J Med Chem. 2021 Nov 11;64(21):15949-15972. doi: 10.1021/acs.jmedchem.1c01351. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34705450
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
Howard S, Amin N, Benowitz AB, Chiarparin E, Cui H, Deng X, Heightman TD, Holmes DJ, Hopkins A, Huang J, Jin Q, Kreatsoulas C, Martin AC, Massey F, McCloskey L, Mortenson PN, Pathuri P, Tisi D, Williams PA. Howard S, et al. Among authors: heightman td. ACS Med Chem Lett. 2013 Oct 18;4(12):1208-12. doi: 10.1021/ml4003277. eCollection 2013 Dec 12. ACS Med Chem Lett. 2013. PMID: 24900632 Free PMC article.
Structure-Activity and Structure-Conformation Relationships of Aryl Propionic Acid Inhibitors of the Kelch-like ECH-Associated Protein 1/Nuclear Factor Erythroid 2-Related Factor 2 (KEAP1/NRF2) Protein-Protein Interaction.
Heightman TD, Callahan JF, Chiarparin E, Coyle JE, Griffiths-Jones C, Lakdawala AS, McMenamin R, Mortenson PN, Norton D, Peakman TM, Rich SJ, Richardson C, Rumsey WL, Sanchez Y, Saxty G, Willems HMG, Wolfe L 3rd, Woolford AJ, Wu Z, Yan H, Kerns JK, Davies TG. Heightman TD, et al. J Med Chem. 2019 May 9;62(9):4683-4702. doi: 10.1021/acs.jmedchem.9b00279. Epub 2019 Apr 25. J Med Chem. 2019. PMID: 30973731
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. Among authors: heightman td. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
64 results