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Page 1
Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery.
Coussens NP, Sittampalam GS, Guha R, Brimacombe K, Grossman A, Chung TDY, Weidner JR, Riss T, Trask OJ, Auld D, Dahlin JL, Devanaryan V, Foley TL, McGee J, Kahl SD, Kales SC, Arkin M, Baell J, Bejcek B, Gal-Edd N, Glicksman M, Haas JV, Iversen PW, Hoeppner M, Lathrop S, Sayers E, Liu H, Trawick B, McVey J, Lemmon VP, Li Z, McManus O, Minor L, Napper A, Wildey MJ, Pacifici R, Chin WW, Xia M, Xu X, Lal-Nag M, Hall MD, Michael S, Inglese J, Simeonov A, Austin CP. Coussens NP, et al. Among authors: kales sc. Clin Transl Sci. 2018 Sep;11(5):461-470. doi: 10.1111/cts.12570. Epub 2018 Jul 24. Clin Transl Sci. 2018. PMID: 29877628 Free PMC article. Review.
Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.
Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X. Horton JR, et al. Among authors: kales sc. J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23. J Med Chem. 2018. PMID: 29537847 Free PMC article.
High-throughput screening with nucleosome substrate identifies small-molecule inhibitors of the human histone lysine methyltransferase NSD2.
Coussens NP, Kales SC, Henderson MJ, Lee OW, Horiuchi KY, Wang Y, Chen Q, Kuznetsova E, Wu J, Chakka S, Cheff DM, Cheng KC, Shinn P, Brimacombe KR, Shen M, Simeonov A, Lal-Nag M, Ma H, Jadhav A, Hall MD. Coussens NP, et al. Among authors: kales sc. J Biol Chem. 2018 Aug 31;293(35):13750-13765. doi: 10.1074/jbc.RA118.004274. Epub 2018 Jun 26. J Biol Chem. 2018. PMID: 29945974 Free PMC article.
KDM5 histone demethylases repress immune response via suppression of STING.
Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q. Wu L, et al. Among authors: kales sc. PLoS Biol. 2018 Aug 6;16(8):e2006134. doi: 10.1371/journal.pbio.2006134. eCollection 2018 Aug. PLoS Biol. 2018. PMID: 30080846 Free PMC article.
Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X. Horton JR, et al. Among authors: kales sc. J Med Chem. 2018 Dec 13;61(23):10588-10601. doi: 10.1021/acs.jmedchem.8b01219. Epub 2018 Nov 15. J Med Chem. 2018. PMID: 30392349 Free PMC article.
KDM5B Promotes Drug Resistance by Regulating Melanoma-Propagating Cell Subpopulations.
Liu X, Zhang SM, McGeary MK, Krykbaeva I, Lai L, Jansen DJ, Kales SC, Simeonov A, Hall MD, Kelly DP, Bosenberg MW, Yan Q. Liu X, et al. Among authors: kales sc. Mol Cancer Ther. 2019 Mar;18(3):706-717. doi: 10.1158/1535-7163.MCT-18-0395. Epub 2018 Dec 6. Mol Cancer Ther. 2019. PMID: 30523048 Free PMC article.
An Enzymatic TMPRSS2 Assay for Assessment of Clinical Candidates and Discovery of Inhibitors as Potential Treatment of COVID-19.
Shrimp JH, Kales SC, Sanderson PE, Simeonov A, Shen M, Hall MD. Shrimp JH, et al. Among authors: kales sc. bioRxiv [Preprint]. 2020 Aug 6:2020.06.23.167544. doi: 10.1101/2020.06.23.167544. bioRxiv. 2020. Update in: ACS Pharmacol Transl Sci. 2020 Sep 07;3(5):997-1007. doi: 10.1021/acsptsci.0c00106 PMID: 32596694 Free PMC article. Updated. Preprint.
A Suite of TMPRSS2 Assays for Screening Drug Repurposing Candidates as Potential Treatments of COVID-19.
Shrimp JH, Janiszewski J, Chen CZ, Xu M, Wilson KM, Kales SC, Sanderson PE, Shinn P, Itkin Z, Guo H, Shen M, Klumpp-Thomas C, Michael SG, Zheng W, Simeonov A, Hall MD. Shrimp JH, et al. Among authors: kales sc. bioRxiv [Preprint]. 2022 Feb 7:2022.02.04.479134. doi: 10.1101/2022.02.04.479134. bioRxiv. 2022. Update in: ACS Infect Dis. 2022 Jun 10;8(6):1191-1203. doi: 10.1021/acsinfecdis.2c00172 PMID: 35169799 Free PMC article. Updated. Preprint.
Suite of TMPRSS2 Assays for Screening Drug Repurposing Candidates as Potential Treatments of COVID-19.
Shrimp JH, Janiszewski J, Chen CZ, Xu M, Wilson KM, Kales SC, Sanderson PE, Shinn P, Schneider R, Itkin Z, Guo H, Shen M, Klumpp-Thomas C, Michael SG, Zheng W, Simeonov A, Hall MD. Shrimp JH, et al. Among authors: kales sc. ACS Infect Dis. 2022 Jun 10;8(6):1191-1203. doi: 10.1021/acsinfecdis.2c00172. Epub 2022 Jun 1. ACS Infect Dis. 2022. PMID: 35648838 Free PMC article.
35 results