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

Year Number of Results
1998 1
1999 1
2001 2
2002 1
2003 1
2004 3
2005 2
2007 2
2008 5
2009 3
2010 5
2011 10
2013 5
2014 3
2016 5
2017 3
2018 4
2019 2
2020 1
2021 4
2022 1
2024 0

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60 results

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Page 1
Selective inhibition of BET bromodomains.
Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I, Philpott M, Munro S, McKeown MR, Wang Y, Christie AL, West N, Cameron MJ, Schwartz B, Heightman TD, La Thangue N, French CA, Wiest O, Kung AL, Knapp S, Bradner JE. Filippakopoulos P, et al. Among authors: heightman td. Nature. 2010 Dec 23;468(7327):1067-73. doi: 10.1038/nature09504. Epub 2010 Sep 24. Nature. 2010. PMID: 20871596 Free PMC article.
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
Therapeutic prospects for epigenetic modulation.
Heightman TD. Heightman TD. Expert Opin Ther Targets. 2011 Jun;15(6):729-40. doi: 10.1517/14728222.2011.561786. Epub 2011 Mar 3. Expert Opin Ther Targets. 2011. PMID: 21366500 Review.
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
Tamanini E, Miyamura S, Buck IM, Cons BD, Dawson L, East C, Futamura T, Goto S, Griffiths-Jones C, Hashimoto T, Heightman TD, Ishikawa S, Ito H, Kaneko Y, Kawato T, Kondo K, Kurihara N, McCarthy JM, Mori Y, Nagase T, Nakaishi Y, Reeks J, Sato A, Schöpf P, Tai K, Tamai T, Tisi D, Woolford AJ. Tamanini E, et al. Among authors: heightman td. ACS Med Chem Lett. 2022 Sep 6;13(10):1591-1597. doi: 10.1021/acsmedchemlett.2c00272. eCollection 2022 Oct 13. ACS Med Chem Lett. 2022. PMID: 36262388 Free PMC article.
3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.
Hewings DS, Wang M, Philpott M, Fedorov O, Uttarkar S, Filippakopoulos P, Picaud S, Vuppusetty C, Marsden B, Knapp S, Conway SJ, Heightman TD. Hewings DS, et al. Among authors: heightman td. J Med Chem. 2011 Oct 13;54(19):6761-70. doi: 10.1021/jm200640v. Epub 2011 Sep 6. J Med Chem. 2011. PMID: 21851057 Free PMC article.
Nonenzymatic biotinylation of histone H2A.
Healy S, Heightman TD, Hohmann L, Schriemer D, Gravel RA. Healy S, et al. Among authors: heightman td. Protein Sci. 2009 Feb;18(2):314-28. doi: 10.1002/pro.37. Protein Sci. 2009. PMID: 19160459 Free PMC article.
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
60 results