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Recent Patents on Anti-Infective Drug Discovery

Editor-in-Chief

ISSN (Print): 1574-891X
ISSN (Online): 2212-4071

Biography

Meet Our Associate Editor

Author(s): Atli Thorarensen

Volume 15, Issue 2, 2020

Page: [87 - 88] Pages: 2

DOI: 10.2174/1574891X1502201210094603

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[1]
Hua, X.; Jesson, M.J.; Seneviratne, U.I.; Lin, T.H.; Sharif, N.M.; Xue, L.; Nguyen, C.; Everley, R.A.; Trujillo, J.I.; Johnson, D.S.; Point, G.R. Thorarensen, A.; Kilty, I.; Telliez, J-B.; PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor. ACS Chem. Biol., 2019, 14, 1235-1242.
[2]
Schnute, M.E.; Wennerstål, M.; Alley, J.; Bengtsson, M.; Blinn, J.R.; Bolten, C.W.; Braden, T.; Bonn, T.; Carlsson, B.; Caspers, N.; Chen, M.; Choi, C.; Collis, L.P.; Crouse, K.; Färnegårdh, M.; Fennell, K.F.; Fish, S.; Flick, A.C.; Goos-Nilsson, A.; Gullberg, H.; Harris, P.K.; Heasley, S.E.; Hegen, M.; Hromockyj, A.E.; Hu, X.; Husman, B.; Janosik, T.; Jones, P.; Kaila, N.; Kallin, E.; Kaupp, B.; Kiefer, J.R.; Knafels, J.; Koehler, K.; Kruger, L.; Kurumbail, R.G.; Kyne, Jr R.E.; Li, W.; Löfstedt, J.; Long, S.A.; Menard, C.A.; Mente, S.; Messing, D.; Meyers, M.J.; Napierata, L.; Nöteberg, D.; Nuhant, P.; Pelc, M.J.; Prinsen, M.J.; Rhönnstad, P.; Backström-Rydin, E.; Sandberg, J.; Sandström, M.; Shah, F.; Sjöberg, M.; Sundell, A.; Taylor, A.P. Thorarensen, A.; Trujillo, J.I.; Trzupek, J.D.; Unwalla, R.; Vajdos, F.F.; Weinberg, R.A.; Wood, D.C.; Xing, L.; Zamaratski, E.; Zapf, C.W.; Zhao, Y.; Wilhelmsson, A.; Berstein G. Discovery of 3-Cyano-N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist. J. Med. Chem., 2018, 61, 10415-10439.
[3]
Casimiro-Garcia, A.; Trujillo, J.I.; Vajdos, F.; Juba, B.; Banker, M.E. Aulabaugh, A.; Balbo, P.; Bauman, J.; Chrencik, J.; Coe, J.W.; Czerwinski, R.; Dowty, M.; Knafels, J.D.; Kwon, S.; Leung, L.; Liang, S.; Robinson, R.P.; Telliez, J-B.; Unwalla, R.; Yang, X.; Thorarensen A. Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors. J. Med. Chem., 2018, 61, 10665-10699.
[4]
Thorarensen, A. Dowty, M.E.; Banker, M.E.; Juba, B.; Jussif, J.; Lin, T.; Vincent, F.; Czerwinski, R.M.; Casimiro-Garcia, A.; Unwalla, R.; Trujillo, J.I.; Liang, S.; Balbo, P.; Che, Y.; Gilbert, A.M.; Brown, M.F.; Hayward, M.; Montgomery, J.; Leung, L.; Yang, X.; Soucy, S.; Hegen, M.; Coe, J.W.; Langille, J.; Vajdos, F.; Chrencik, J.; Telliez, J-B.; Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans. J. Med. Chem., 2017, 60, 1971-1993.
[5]
Leung, L.; Yang, X.; Strelevitz, T.J.; Montgomery, J.; Brown, M.F.; Zientek, M.A.; Banfield, C.; Gilbert, A.M. Thorarensen, A.; Dowty, M.E. Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms. Drug Metab. Dispos., 2017, 45, 1-7.
[6]
Li, J.; Wang, B.; Juba, B.M.; Vazquez, M.; Kortum, S.W.; Pierce, B.S.; Pacheco, M.; Roberts, L.; Strohbach, J.W.; Jones, L.H.; Hett, E. Thorarensen, A.; Telliez, J-B.; Sharei, A.; Bunnage, M.; Gilbert, J.B. Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells. ACS Chem. Biol., 2017, 12, 2970-2974.
[7]
Telliez, J-B.; Dowty, M.E.; Wang, L.; Jussif, J.; Lin, T.; Li, L.; Moy, E.; Balbo, P.; Li, W.; Zhao, Y.; Crouse, K.; Dickinson, C.; Symanowicz, P.; Hegen, M.; Banker, M.E.; Vincent, F.; Unwalla, R.; Liang, S.; Gilbert, A.M.; Brown, M.F.; Hayward, M.; Montgomery, J.; Yang, X.; Bauman, J.; Trujillo, J.I.; Casimiro-Garcia, A.; Vajdos, F.F.; Leung, L.; Geoghegan, K.F.; Quazi, A.; Xuan, D.; Jones, L.; Hett, E.; Wright, K.; Clark, J.D. Thorarensen A. Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition. ACS Chem. Biol., 2016, 16, 3442-3451.
[8]
Liu, S.; Desharnais, J.; Sahasrabudhe, P.V.; Jin, P.; Li, W.; Oates, B.D.; Shanker, S.; Banker, M.E.; Chrunyk, B.A.; Song, X.; Feng, X.; Griffor, M.; Jimenez, J.; Chen, G.; Tumelty, D.; Bhat, A.; Bradshaw, C.W.; Woodnutt, G.; Lappe, R.W. Thorarensen, Atli; Qiu, X.; Withka, J.M.; Wood, L.D. Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide. Sci. Rep., 2016, 6, 26071.
[9]
Liu, S.; Dakin, L.A.; Xing, L.; Withka, J.M.; Sahasrabudhe, P.V.; Li, W.; Banker, M.E.; Balbo, P.; Shanker, S.; Chrunyk, B.A.; Guo, Z.; Chen, J.M.; Young, J.A.; Bai, G.; Starr, J.T.; Wright, S.W.; Bussenius, J.; Tan, S.; Gopalsamy, A.; Lefker, B.A.; Vincent, F.; Jones, L.H.; Xu, H.; Hoth, L.R.; Geoghegan, K.F.; Qiu, X.; Bunnage, M.E. Thorarensen, A. Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists. Sci. Rep., 2016, 16, 30859.
[10]
Lovering, F.; Aevazelis, C.; Chang, J.; Dehnhardt, C.; Fitz, L.; Han, S.; Janz, K.; Lee, J.; Kaila, N.; McDonald, J.; Moore, W.; Moretto, A.; Papaioannou, N.; Richard, D.; Ryan, M.S.; Wan, Z-K. Thorarensen, A. Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free-Energy Perturbation (FEP). ChemMedChem, 2016, 11, 217-233.

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