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N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Huang W, Zheng W, Urban DJ, Inglese J, Sidransky E, Austin CP, Thomas CJ. Huang W, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5783-9. doi: 10.1016/j.bmcl.2007.08.050. Epub 2007 Aug 28. Bioorg Med Chem Lett. 2007. PMID: 17827006 Free PMC article.
Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease.
Zheng W, Padia J, Urban DJ, Jadhav A, Goker-Alpan O, Simeonov A, Goldin E, Auld D, LaMarca ME, Inglese J, Austin CP, Sidransky E. Zheng W, et al. Among authors: austin cp. Proc Natl Acad Sci U S A. 2007 Aug 7;104(32):13192-7. doi: 10.1073/pnas.0705637104. Epub 2007 Aug 1. Proc Natl Acad Sci U S A. 2007. PMID: 17670938 Free PMC article.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Skoumbourdis AP, Huang R, Southall N, Leister W, Guo V, Cho MH, Inglese J, Nirenberg M, Austin CP, Xia M, Thomas CJ. Skoumbourdis AP, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2008 Feb 15;18(4):1297-303. doi: 10.1016/j.bmcl.2008.01.028. Epub 2008 Jan 11. Bioorg Med Chem Lett. 2008. PMID: 18243697 Free PMC article.
Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors.
Skoumbourdis AP, Leclair CA, Stefan E, Turjanski AG, Maguire W, Titus SA, Huang R, Auld DS, Inglese J, Austin CP, Michnick SW, Xia M, Thomas CJ. Skoumbourdis AP, et al. Among authors: austin cp. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3686-92. doi: 10.1016/j.bmcl.2009.01.057. Epub 2009 Jan 23. Bioorg Med Chem Lett. 2009. PMID: 19464886 Free PMC article.
Structure mechanism insights and the role of nitric oxide donation guide the development of oxadiazole-2-oxides as therapeutic agents against schistosomiasis.
Rai G, Sayed AA, Lea WA, Luecke HF, Chakrapani H, Prast-Nielsen S, Jadhav A, Leister W, Shen M, Inglese J, Austin CP, Keefer L, Arnér ES, Simeonov A, Maloney DJ, Williams DL, Thomas CJ. Rai G, et al. Among authors: austin cp. J Med Chem. 2009 Oct 22;52(20):6474-83. doi: 10.1021/jm901021k. J Med Chem. 2009. PMID: 19761212 Free PMC article.
267 results