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Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).
Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ. Rai G, et al. Among authors: sulikowski g. J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9. J Med Chem. 2017. PMID: 29120638 Free PMC article.
Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α.
Thorne CA, Hanson AJ, Schneider J, Tahinci E, Orton D, Cselenyi CS, Jernigan KK, Meyers KC, Hang BI, Waterson AG, Kim K, Melancon B, Ghidu VP, Sulikowski GA, LaFleur B, Salic A, Lee LA, Miller DM 3rd, Lee E. Thorne CA, et al. Among authors: sulikowski ga. Nat Chem Biol. 2010 Nov;6(11):829-36. doi: 10.1038/nchembio.453. Epub 2010 Oct 3. Nat Chem Biol. 2010. PMID: 20890287 Free PMC article.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Melancon BJ, Lamers AP, Bridges TM, Sulikowski GA, Utley TJ, Sheffler DJ, Noetzel MJ, Morrison RD, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Wood MR. Melancon BJ, et al. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1044-8. doi: 10.1016/j.bmcl.2011.11.110. Epub 2011 Dec 6. Bioorg Med Chem Lett. 2012. PMID: 22197142 Free PMC article.
Allosteric antagonism of insect odorant receptor ion channels.
Jones PL, Pask GM, Romaine IM, Taylor RW, Reid PR, Waterson AG, Sulikowski GA, Zwiebel LJ. Jones PL, et al. Among authors: sulikowski ga. PLoS One. 2012;7(1):e30304. doi: 10.1371/journal.pone.0030304. Epub 2012 Jan 17. PLoS One. 2012. PMID: 22272331 Free PMC article.
Discovery and SAR of a novel series of GIRK1/2 and GIRK1/4 activators.
Ramos-Hunter SJ, Engers DW, Kaufmann K, Du Y, Lindsley CW, Weaver CD, Sulikowski GA. Ramos-Hunter SJ, et al. Bioorg Med Chem Lett. 2013 Sep 15;23(18):5195-8. doi: 10.1016/j.bmcl.2013.07.002. Epub 2013 Jul 18. Bioorg Med Chem Lett. 2013. PMID: 23916258 Free PMC article.
Narrow SAR in odorant sensing Orco receptor agonists.
Romaine IM, Taylor RW, Saidu SP, Kim K, Sulikowski GA, Zwiebel LJ, Waterson AG. Romaine IM, et al. Among authors: sulikowski ga. Bioorg Med Chem Lett. 2014 Jun 15;24(12):2613-6. doi: 10.1016/j.bmcl.2014.04.081. Epub 2014 Apr 29. Bioorg Med Chem Lett. 2014. PMID: 24813736 Free PMC article.
Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes.
Dumas ME, Chen GY, Kendrick ND, Xu G, Larsen SD, Jana S, Waterson AG, Bauer JA, Hancock W, Sulikowski GA, Ohi R. Dumas ME, et al. Among authors: sulikowski ga. Bioorg Med Chem Lett. 2019 Jan 15;29(2):148-154. doi: 10.1016/j.bmcl.2018.12.008. Epub 2018 Dec 4. Bioorg Med Chem Lett. 2019. PMID: 30528696 Free PMC article.
Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
Rai G, Urban DJ, Mott BT, Hu X, Yang SM, Benavides GA, Johnson MS, Squadrito GL, Brimacombe KR, Lee TD, Cheff DM, Zhu H, Henderson MJ, Pohida K, Sulikowski GA, Dranow DM, Kabir M, Shah P, Padilha E, Tao D, Fang Y, Christov PP, Kim K, Jana S, Muttil P, Anderson T, Kunda NK, Hathaway HJ, Kusewitt DF, Oshima N, Cherukuri M, Davies DR, Norenberg JP, Sklar LA, Moore WJ, Dang CV, Stott GM, Neckers L, Flint AJ, Darley-Usmar VM, Simeonov A, Waterson AG, Jadhav A, Hall MD, Maloney DJ. Rai G, et al. Among authors: sulikowski ga. J Med Chem. 2020 Oct 8;63(19):10984-11011. doi: 10.1021/acs.jmedchem.0c00916. Epub 2020 Sep 27. J Med Chem. 2020. PMID: 32902275 Free PMC article.
98 results