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Page 1
Donated chemical probes for open science.
Müller S, Ackloo S, Arrowsmith CH, Bauser M, Baryza JL, Blagg J, Böttcher J, Bountra C, Brown PJ, Bunnage ME, Carter AJ, Damerell D, Dötsch V, Drewry DH, Edwards AM, Edwards J, Elkins JM, Fischer C, Frye SV, Gollner A, Grimshaw CE, IJzerman A, Hanke T, Hartung IV, Hitchcock S, Howe T, Hughes TV, Laufer S, Li VM, Liras S, Marsden BD, Matsui H, Mathias J, O'Hagan RC, Owen DR, Pande V, Rauh D, Rosenberg SH, Roth BL, Schneider NS, Scholten C, Singh Saikatendu K, Simeonov A, Takizawa M, Tse C, Thompson PR, Treiber DK, Viana AY, Wells CI, Willson TM, Zuercher WJ, Knapp S, Mueller-Fahrnow A. Müller S, et al. Among authors: tse c. Elife. 2018 Apr 20;7:e34311. doi: 10.7554/eLife.34311. Elife. 2018. PMID: 29676732 Free PMC article.
Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.
Bruncko M, Wang L, Sheppard GS, Phillips DC, Tahir SK, Xue J, Erickson S, Fidanze S, Fry E, Hasvold L, Jenkins GJ, Jin S, Judge RA, Kovar PJ, Madar D, Nimmer P, Park C, Petros AM, Rosenberg SH, Smith ML, Song X, Sun C, Tao ZF, Wang X, Xiao Y, Zhang H, Tse C, Leverson JD, Elmore SW, Souers AJ. Bruncko M, et al. Among authors: tse c. J Med Chem. 2015 Mar 12;58(5):2180-94. doi: 10.1021/jm501258m. Epub 2015 Feb 26. J Med Chem. 2015. PMID: 25679114
The Bcl-2/Bcl-X(L)/Bcl-w inhibitor, navitoclax, enhances the activity of chemotherapeutic agents in vitro and in vivo.
Chen J, Jin S, Abraham V, Huang X, Liu B, Mitten MJ, Nimmer P, Lin X, Smith M, Shen Y, Shoemaker AR, Tahir SK, Zhang H, Ackler SL, Rosenberg SH, Maecker H, Sampath D, Leverson JD, Tse C, Elmore SW. Chen J, et al. Among authors: tse c. Mol Cancer Ther. 2011 Dec;10(12):2340-9. doi: 10.1158/1535-7163.MCT-11-0415. Epub 2011 Sep 13. Mol Cancer Ther. 2011. PMID: 21914853
Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax).
Leverson JD, Zhang H, Chen J, Tahir SK, Phillips DC, Xue J, Nimmer P, Jin S, Smith M, Xiao Y, Kovar P, Tanaka A, Bruncko M, Sheppard GS, Wang L, Gierke S, Kategaya L, Anderson DJ, Wong C, Eastham-Anderson J, Ludlam MJ, Sampath D, Fairbrother WJ, Wertz I, Rosenberg SH, Tse C, Elmore SW, Souers AJ. Leverson JD, et al. Among authors: tse c. Cell Death Dis. 2015 Jan 15;6(1):e1590. doi: 10.1038/cddis.2014.561. Cell Death Dis. 2015. PMID: 25590800 Free PMC article.
Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Wilsbacher JL, Cheng M, Cheng D, Trammell SAJ, Shi Y, Guo J, Koeniger SL, Kovar PJ, He Y, Selvaraju S, Heyman HR, Sorensen BK, Clark RF, Hansen TM, Longenecker KL, Raich D, Korepanova AV, Cepa S, Towne DL, Abraham VC, Tang H, Richardson PL, McLoughlin SM, Badagnani I, Curtin ML, Michaelides MR, Maag D, Buchanan FG, Chiang GG, Gao W, Rosenberg SH, Brenner C, Tse C. Wilsbacher JL, et al. Among authors: tse c. Mol Cancer Ther. 2017 Jul;16(7):1236-1245. doi: 10.1158/1535-7163.MCT-16-0819. Epub 2017 May 3. Mol Cancer Ther. 2017. PMID: 28468779
ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.
Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ, Huang DC, Hymowitz SG, Jin S, Khaw SL, Kovar PJ, Lam LT, Lee J, Maecker HL, Marsh KC, Mason KD, Mitten MJ, Nimmer PM, Oleksijew A, Park CH, Park CM, Phillips DC, Roberts AW, Sampath D, Seymour JF, Smith ML, Sullivan GM, Tahir SK, Tse C, Wendt MD, Xiao Y, Xue JC, Zhang H, Humerickhouse RA, Rosenberg SH, Elmore SW. Souers AJ, et al. Among authors: tse c. Nat Med. 2013 Feb;19(2):202-8. doi: 10.1038/nm.3048. Epub 2013 Jan 6. Nat Med. 2013. PMID: 23291630
Pyrazole diaminopyrimidines as dual inhibitors of KDR and Aurora B kinases.
Curtin ML, Heyman HR, Frey RR, Marcotte PA, Glaser KB, Jankowski JR, Magoc TJ, Albert DH, Olson AM, Reuter DR, Bouska JJ, Montgomery DA, Palma JP, Donawho CK, Stewart KD, Tse C, Michaelides MR. Curtin ML, et al. Among authors: tse c. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4750-5. doi: 10.1016/j.bmcl.2012.05.067. Epub 2012 May 26. Bioorg Med Chem Lett. 2012. PMID: 22695126
858 results