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Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study.
Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Mackman RL, et al. Among authors: lee g. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. J Med Chem. 2015. PMID: 25574686 Clinical Trial.
Highly Selective Phosphatidylinositol 4-Kinase IIIβ Inhibitors and Structural Insight into Their Mode of Action.
Mejdrová I, Chalupská D, Kögler M, Šála M, Plačková P, Baumlová A, Hřebabecký H, Procházková E, Dejmek M, Guillon R, Strunin D, Weber J, Lee G, Birkus G, Mertlíková-Kaiserová H, Boura E, Nencka R. Mejdrová I, et al. Among authors: lee g. J Med Chem. 2015 May 14;58(9):3767-93. doi: 10.1021/acs.jmedchem.5b00499. Epub 2015 May 4. J Med Chem. 2015. PMID: 25897704
Discovery of β-D-2'-deoxy-2'-α-fluoro-4'-α-cyano-5-aza-7,9-dideaza adenosine as a potent nucleoside inhibitor of respiratory syncytial virus with excellent selectivity over mitochondrial RNA and DNA polymerases.
Clarke MO, Mackman R, Byun D, Hui H, Barauskas O, Birkus G, Chun BK, Doerffler E, Feng J, Karki K, Lee G, Perron M, Siegel D, Swaminathan S, Lee W. Clarke MO, et al. Among authors: lee g, lee w. Bioorg Med Chem Lett. 2015 Jun 15;25(12):2484-7. doi: 10.1016/j.bmcl.2015.04.073. Epub 2015 Apr 29. Bioorg Med Chem Lett. 2015. PMID: 25978965
Purine analogs as phosphatidylinositol 4-kinase IIIβ inhibitors.
Šála M, Kögler M, Plačková P, Mejdrová I, Hřebabecký H, Procházková E, Strunin D, Lee G, Birkus G, Weber J, Mertlíková-Kaiserová H, Nencka R. Šála M, et al. Among authors: lee g. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2706-12. doi: 10.1016/j.bmcl.2016.04.002. Epub 2016 Apr 5. Bioorg Med Chem Lett. 2016. PMID: 27090557 Free PMC article.
Rational Design of Novel Highly Potent and Selective Phosphatidylinositol 4-Kinase IIIβ (PI4KB) Inhibitors as Broad-Spectrum Antiviral Agents and Tools for Chemical Biology.
Mejdrová I, Chalupská D, Plačková P, Müller C, Šála M, Klíma M, Baumlová A, Hřebabecký H, Procházková E, Dejmek M, Strunin D, Weber J, Lee G, Matoušová M, Mertlíková-Kaiserová H, Ziebuhr J, Birkus G, Boura E, Nencka R. Mejdrová I, et al. Among authors: lee g. J Med Chem. 2017 Jan 12;60(1):100-118. doi: 10.1021/acs.jmedchem.6b01465. Epub 2016 Dec 22. J Med Chem. 2017. PMID: 28004945
Discovery and Synthesis of a Phosphoramidate Prodrug of a Pyrrolo[2,1-f][triazin-4-amino] Adenine C-Nucleoside (GS-5734) for the Treatment of Ebola and Emerging Viruses.
Siegel D, Hui HC, Doerffler E, Clarke MO, Chun K, Zhang L, Neville S, Carra E, Lew W, Ross B, Wang Q, Wolfe L, Jordan R, Soloveva V, Knox J, Perry J, Perron M, Stray KM, Barauskas O, Feng JY, Xu Y, Lee G, Rheingold AL, Ray AS, Bannister R, Strickley R, Swaminathan S, Lee WA, Bavari S, Cihlar T, Lo MK, Warren TK, Mackman RL. Siegel D, et al. Among authors: lee g, lee wa. J Med Chem. 2017 Mar 9;60(5):1648-1661. doi: 10.1021/acs.jmedchem.6b01594. Epub 2017 Feb 14. J Med Chem. 2017. PMID: 28124907
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
Mackman RL, Mish M, Chin G, Perry JK, Appleby T, Aktoudianakis V, Metobo S, Pyun P, Niu C, Daffis S, Yu H, Zheng J, Villasenor AG, Zablocki J, Chamberlain J, Jin H, Lee G, Suekawa-Pirrone K, Santos R, Delaney WE 4th, Fletcher SP. Mackman RL, et al. Among authors: lee g. J Med Chem. 2020 Sep 24;63(18):10188-10203. doi: 10.1021/acs.jmedchem.0c00100. Epub 2020 Jun 3. J Med Chem. 2020. PMID: 32407112
Off-Target In Vitro Profiling Demonstrates that Remdesivir Is a Highly Selective Antiviral Agent.
Xu Y, Barauskas O, Kim C, Babusis D, Murakami E, Kornyeyev D, Lee G, Stepan G, Perron M, Bannister R, Schultz BE, Sakowicz R, Porter D, Cihlar T, Feng JY. Xu Y, et al. Among authors: lee g. Antimicrob Agents Chemother. 2021 Jan 20;65(2):e02237-20. doi: 10.1128/AAC.02237-20. Print 2021 Jan 20. Antimicrob Agents Chemother. 2021. PMID: 33229429 Free PMC article.
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