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A novel tankyrase small-molecule inhibitor suppresses APC mutation-driven colorectal tumor growth.
Lau T, Chan E, Callow M, Waaler J, Boggs J, Blake RA, Magnuson S, Sambrone A, Schutten M, Firestein R, Machon O, Korinek V, Choo E, Diaz D, Merchant M, Polakis P, Holsworth DD, Krauss S, Costa M. Lau T, et al. Among authors: holsworth dd. Cancer Res. 2013 May 15;73(10):3132-44. doi: 10.1158/0008-5472.CAN-12-4562. Epub 2013 Mar 28. Cancer Res. 2013. PMID: 23539443
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ. Holsworth DD, et al. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3575-80. doi: 10.1016/j.bmcl.2007.04.052. Epub 2007 Apr 25. Bioorg Med Chem Lett. 2007. PMID: 17482464
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: holsworth dd. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
Ketopiperazine-based renin inhibitors: optimization of the "C" ring.
Holsworth DD, Cai C, Cheng XM, Cody WL, Downing DM, Erasga N, Lee C, Powell NA, Edmunds JJ, Stier M, Jalaie M, Zhang E, McConnell P, Ryan MJ, Bryant J, Li T, Kasani A, Hall E, Subedi R, Rahim M, Maiti S. Holsworth DD, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2500-4. doi: 10.1016/j.bmcl.2006.01.084. Epub 2006 Feb 15. Bioorg Med Chem Lett. 2006. PMID: 16480874
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Among authors: holsworth dd. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
22 results