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Page 1
Tricyclic covalent inhibitors selectively target Jak3 through an active site thiol.
Goedken ER, Argiriadi MA, Banach DL, Fiamengo BA, Foley SE, Frank KE, George JS, Harris CM, Hobson AD, Ihle DC, Marcotte D, Merta PJ, Michalak ME, Murdock SE, Tomlinson MJ, Voss JW. Goedken ER, et al. Among authors: harris cm. J Biol Chem. 2015 Feb 20;290(8):4573-4589. doi: 10.1074/jbc.M114.595181. Epub 2014 Dec 31. J Biol Chem. 2015. PMID: 25552479 Free PMC article.
2,4-Diaminopyrimidine MK2 inhibitors. Part I: Observation of an unexpected inhibitor binding mode.
Argiriadi MA, Ericsson AM, Harris CM, Banach DL, Borhani DW, Calderwood DJ, Demers MD, Dimauro J, Dixon RW, Hardman J, Kwak S, Li B, Mankovich JA, Marcotte D, Mullen KD, Ni B, Pietras M, Sadhukhan R, Sousa S, Tomlinson MJ, Wang L, Xiang T, Talanian RV. Argiriadi MA, et al. Among authors: harris cm. Bioorg Med Chem Lett. 2010 Jan 1;20(1):330-3. doi: 10.1016/j.bmcl.2009.10.102. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2010. PMID: 19919896
2,4-Diaminopyrimidine MK2 inhibitors. Part II: Structure-based inhibitor optimization.
Harris CM, Ericsson AM, Argiriadi MA, Barberis C, Borhani DW, Burchat A, Calderwood DJ, Cunha GA, Dixon RW, Frank KE, Johnson EF, Kamens J, Kwak S, Li B, Mullen KD, Perron DC, Wang L, Wishart N, Wu X, Zhang X, Zmetra TR, Talanian RV. Harris CM, et al. Bioorg Med Chem Lett. 2010 Jan 1;20(1):334-7. doi: 10.1016/j.bmcl.2009.10.103. Epub 2009 Oct 29. Bioorg Med Chem Lett. 2010. PMID: 19926477
Minimum significant ratio of selectivity ratios (MSRSR) and confidence in ratio of selectivity ratios (CRSR): quantitative measures for selectivity ratios obtained by screening assays.
Goedken ER, Devanarayan V, Harris CM, Dowding LA, Jakway JP, Voss JW, Wishart N, Jordan DC, Talanian RV. Goedken ER, et al. Among authors: harris cm. J Biomol Screen. 2012 Aug;17(7):857-67. doi: 10.1177/1087057112447108. Epub 2012 May 14. J Biomol Screen. 2012. PMID: 22584786
Discovery of A-971432, An Orally Bioavailable Selective Sphingosine-1-Phosphate Receptor 5 (S1P5) Agonist for the Potential Treatment of Neurodegenerative Disorders.
Hobson AD, Harris CM, van der Kam EL, Turner SC, Abibi A, Aguirre AL, Bousquet P, Kebede T, Konopacki DB, Gintant G, Kim Y, Larson K, Maull JW, Moore NS, Shi D, Shrestha A, Tang X, Zhang P, Sarris KK. Hobson AD, et al. Among authors: harris cm. J Med Chem. 2015 Dec 10;58(23):9154-70. doi: 10.1021/acs.jmedchem.5b00928. Epub 2015 Nov 23. J Med Chem. 2015. PMID: 26509640
Creation of a S1P Lyase bacterial surrogate for structure-based drug design.
Argiriadi MA, Banach D, Radziejewska E, Marchie S, DiMauro J, Dinges J, Dominguez E, Hutchins C, Judge RA, Queeney K, Wallace G, Harris CM. Argiriadi MA, et al. Among authors: harris cm. Bioorg Med Chem Lett. 2016 May 1;26(9):2293-6. doi: 10.1016/j.bmcl.2016.02.084. Epub 2016 Mar 3. Bioorg Med Chem Lett. 2016. PMID: 27013389
Hit-to-lead evaluation of a novel class of sphingosine 1-phosphate lyase inhibitors.
Dinges J, Harris CM, Wallace GA, Argiriadi MA, Queeney KL, Perron DC, Dominguez E, Kebede T, Desino KE, Patel H, Vasudevan A. Dinges J, et al. Among authors: harris cm. Bioorg Med Chem Lett. 2016 May 1;26(9):2297-302. doi: 10.1016/j.bmcl.2016.03.043. Epub 2016 Mar 14. Bioorg Med Chem Lett. 2016. PMID: 27020302
469 results