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Biochemical assays for the discovery of TDP1 inhibitors.
Marchand C, Huang SY, Dexheimer TS, Lea WA, Mott BT, Chergui A, Naumova A, Stephen AG, Rosenthal AS, Rai G, Murai J, Gao R, Maloney DJ, Jadhav A, Jorgensen WL, Simeonov A, Pommier Y. Marchand C, et al. Among authors: rosenthal as. Mol Cancer Ther. 2014 Aug;13(8):2116-26. doi: 10.1158/1535-7163.MCT-13-0952. Epub 2014 Jul 14. Mol Cancer Ther. 2014. PMID: 25024006 Free PMC article.
Synthesis and structure-activity relationship studies of N-benzyl-2-phenylpyrimidin-4-amine derivatives as potent USP1/UAF1 deubiquitinase inhibitors with anticancer activity against nonsmall cell lung cancer.
Dexheimer TS, Rosenthal AS, Luci DK, Liang Q, Villamil MA, Chen J, Sun H, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ. Dexheimer TS, et al. Among authors: rosenthal as. J Med Chem. 2014 Oct 9;57(19):8099-110. doi: 10.1021/jm5010495. Epub 2014 Sep 17. J Med Chem. 2014. PMID: 25229643 Free PMC article.
A selective USP1-UAF1 inhibitor links deubiquitination to DNA damage responses.
Liang Q, Dexheimer TS, Zhang P, Rosenthal AS, Villamil MA, You C, Zhang Q, Chen J, Ott CA, Sun H, Luci DK, Yuan B, Simeonov A, Jadhav A, Xiao H, Wang Y, Maloney DJ, Zhuang Z. Liang Q, et al. Among authors: rosenthal as. Nat Chem Biol. 2014 Apr;10(4):298-304. doi: 10.1038/nchembio.1455. Epub 2014 Feb 16. Nat Chem Biol. 2014. PMID: 24531842 Free PMC article.
A small molecule inhibitor of the BLM helicase modulates chromosome stability in human cells.
Nguyen GH, Dexheimer TS, Rosenthal AS, Chu WK, Singh DK, Mosedale G, Bachrati CZ, Schultz L, Sakurai M, Savitsky P, Abu M, McHugh PJ, Bohr VA, Harris CC, Jadhav A, Gileadi O, Maloney DJ, Simeonov A, Hickson ID. Nguyen GH, et al. Among authors: rosenthal as. Chem Biol. 2013 Jan 24;20(1):55-62. doi: 10.1016/j.chembiol.2012.10.016. Chem Biol. 2013. PMID: 23352139 Free PMC article.
Discovery of ML323 as a Novel Inhibitor of the USP1/UAF1 Deubiquitinase Complex.
Dexheimer TS, Rosenthal AS, Liang Q, Chen J, Villamil MA, Kerns EH, Simeonov A, Jadhav A, Zhuang Z, Maloney DJ. Dexheimer TS, et al. Among authors: rosenthal as. 2012 Oct 23 [updated 2014 Sep 18]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. 2012 Oct 23 [updated 2014 Sep 18]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 25506968 Free Books & Documents. Review.
Discovery of ML216, a Small Molecule Inhibitor of Bloom (BLM) Helicase.
Rosenthal AS, Dexheimer TS, Nguyen G, Gileadi O, Vindigni A, Simeonov A, Jadhav A, Hickson I, Maloney DJ. Rosenthal AS, et al. 2011 Apr 15 [updated 2013 Feb 28]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. 2011 Apr 15 [updated 2013 Feb 28]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010–. PMID: 24027802 Free Books & Documents. Review.
119 results