Broad-spectrum antiviral GS-5734 inhibits both epidemic and zoonotic coronaviruses
Sheahan, Timothy P, Sims, Amy C, Graham, Rachel L, Menachery, Vineet D, Gralinski, Lisa E, Case, James B, Leist, Sarah R, Pyrc, Krzysztof, Feng, Joy Y, Trantcheva, Iva, Bannister, Roy, Park, Yeojin, Babusis, Darius, Clarke, Michael O, Mackman, Richard L, Spahn, Jamie E, Palmiotti, Christopher A, Siegel, Dustin, Ray, Adrian S, Cihlar, Tomas, Jordan, Robert, Denison, Mark R, Baric, Ralph S
Published in Science translational medicine (28.06.2017)
Published in Science translational medicine (28.06.2017)
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Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease
Agostini, Maria L, Andres, Erica L, Sims, Amy C, Graham, Rachel L, Sheahan, Timothy P, Lu, Xiaotao, Smith, Everett Clinton, Case, James Brett, Feng, Joy Y, Jordan, Robert, Ray, Adrian S, Cihlar, Tomas, Siegel, Dustin, Mackman, Richard L, Clarke, Michael O, Baric, Ralph S, Denison, Mark R
Published in mBio (06.03.2018)
Published in mBio (06.03.2018)
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GS-5734 and its parent nucleoside analog inhibit Filo-, Pneumo-, and Paramyxoviruses
Lo, Michael K., Jordan, Robert, Arvey, Aaron, Sudhamsu, Jawahar, Shrivastava-Ranjan, Punya, Hotard, Anne L., Flint, Mike, McMullan, Laura K., Siegel, Dustin, Clarke, Michael O., Mackman, Richard L., Hui, Hon C., Perron, Michel, Ray, Adrian S., Cihlar, Tomas, Nichol, Stuart T., Spiropoulou, Christina F.
Published in Scientific reports (06.03.2017)
Published in Scientific reports (06.03.2017)
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Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys
Warren, Travis K., Jordan, Robert, Lo, Michael K., Ray, Adrian S., Mackman, Richard L., Soloveva, Veronica, Siegel, Dustin, Perron, Michel, Bannister, Roy, Hui, Hon C., Larson, Nate, Strickley, Robert, Wells, Jay, Stuthman, Kelly S., Van Tongeren, Sean A., Garza, Nicole L., Donnelly, Ginger, Shurtleff, Amy C., Retterer, Cary J., Gharaibeh, Dima, Zamani, Rouzbeh, Kenny, Tara, Eaton, Brett P., Grimes, Elizabeth, Welch, Lisa S., Gomba, Laura, Wilhelmsen, Catherine L., Nichols, Donald K., Nuss, Jonathan E., Nagle, Elyse R., Kugelman, Jeffrey R., Palacios, Gustavo, Doerffler, Edward, Neville, Sean, Carra, Ernest, Clarke, Michael O., Zhang, Lijun, Lew, Willard, Ross, Bruce, Wang, Queenie, Chun, Kwon, Wolfe, Lydia, Babusis, Darius, Park, Yeojin, Stray, Kirsten M., Trancheva, Iva, Feng, Joy Y., Barauskas, Ona, Xu, Yili, Wong, Pamela, Braun, Molly R., Flint, Mike, McMullan, Laura K., Chen, Shan-Shan, Fearns, Rachel, Swaminathan, Swami, Mayers, Douglas L., Spiropoulou, Christina F., Lee, William A., Nichol, Stuart T., Cihlar, Tomas, Bavari, Sina
Published in Nature (London) (17.03.2016)
Published in Nature (London) (17.03.2016)
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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, Dustin, Hui, Hon C, Doerffler, Edward, Clarke, Michael O, Chun, Kwon, Zhang, Lijun, Neville, Sean, Carra, Ernest, Lew, Willard, Ross, Bruce, Wang, Queenie, Wolfe, Lydia, Jordan, Robert, Soloveva, Veronica, Knox, John, Perry, Jason, Perron, Michel, Stray, Kirsten M, Barauskas, Ona, Feng, Joy Y, Xu, Yili, Lee, Gary, Rheingold, Arnold L, Ray, Adrian S, Bannister, Roy, Strickley, Robert, Swaminathan, Swami, Lee, William A, Bavari, Sina, Cihlar, Tomas, Lo, Michael K, Warren, Travis K, Mackman, Richard L
Published in Journal of Medicinal Chemistry (09.03.2017)
Published in Journal of Medicinal Chemistry (09.03.2017)
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Web Resource
Oral prodrug of remdesivir parent GS-441524 is efficacious against SARS-CoV-2 in ferrets
Cox, Robert M., Wolf, Josef D., Lieber, Carolin M., Sourimant, Julien, Lin, Michelle J., Babusis, Darius, DuPont, Venice, Chan, Julie, Barrett, Kim T., Lye, Diane, Kalla, Rao, Chun, Kwon, Mackman, Richard L., Ye, Chengjin, Cihlar, Tomas, Martinez-Sobrido, Luis, Greninger, Alexander L., Bilello, John P., Plemper, Richard K.
Published in Nature communications (05.11.2021)
Published in Nature communications (05.11.2021)
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Journal Article
Oral GS-5806 Activity in a Respiratory Syncytial Virus Challenge Study
DeVincenzo, John P, Whitley, Richard J, Mackman, Richard L, Scaglioni-Weinlich, Cecilia, Harrison, Lisa, Farrell, Eric, McBride, Stephen, Lambkin-Williams, Robert, Jordan, Robert, Xin, Yan, Ramanathan, Srini, O’Riordan, Thomas, Lewis, Sandra A, Li, Xiaoming, Toback, Seth L, Lin, Shao-Lee, Chien, Jason W
Published in The New England journal of medicine (21.08.2014)
Published in The New England journal of medicine (21.08.2014)
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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, Richard L, Sangi, Michael, Sperandio, David, Parrish, Jay P, Eisenberg, Eugene, Perron, Michel, Hui, Hon, Zhang, Lijun, Siegel, Dustin, Yang, Hai, Saunders, Oliver, Boojamra, Constantine, Lee, Gary, Samuel, Dharmaraj, Babaoglu, Kerim, Carey, Anne, Gilbert, Brian E, Piedra, Pedro A, Strickley, Robert, Iwata, Quynh, Hayes, Jaclyn, Stray, Kirsten, Kinkade, April, Theodore, Dorothy, Jordan, Robert, Desai, Manoj, Cihlar, Tomas
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
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Antiviral Efficacy of a Respiratory Syncytial Virus (RSV) Fusion Inhibitor in a Bovine Model of RSV Infection
Jordan, Robert, Shao, Matt, Mackman, Richard L, Perron, Michel, Cihlar, Tomas, Lewis, Sandy A, Eisenberg, Eugene J, Carey, Anne, Strickley, Robert G, Chien, Jason W, Anderson, Mark L, McEligot, Heather A, Behrens, Nicole E, Gershwin, Laurel J
Published in Antimicrobial agents and chemotherapy (01.08.2015)
Published in Antimicrobial agents and chemotherapy (01.08.2015)
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Journey of remdesivir from the inhibition of hepatitis C virus to the treatment of COVID-19
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Design and Profiling of GS-9148, a Novel Nucleotide Analog Active against Nucleoside-Resistant Variants of Human Immunodeficiency Virus Type 1, and Its Orally Bioavailable Phosphonoamidate Prodrug, GS-9131
Cihlar, Tomas, Ray, Adrian S, Boojamra, Constantine G, Zhang, Lijun, Hui, Hon, Laflamme, Genevieve, Vela, Jennifer E, Grant, Deborah, Chen, James, Myrick, Florence, White, Kirsten L, Gao, Ying, Lin, Kuei-Ying, Douglas, Janet L, Parkin, Neil T, Carey, Anne, Pakdaman, Rowchanak, Mackman, Richard L
Published in Antimicrobial Agents and Chemotherapy (01.02.2008)
Published in Antimicrobial Agents and Chemotherapy (01.02.2008)
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Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148
Mackman, Richard L., Ray, Adrian S., Hui, Hon C., Zhang, Lijun, Birkus, Gabriel, Boojamra, Constantine G., Desai, Manoj C., Douglas, Janet L., Gao, Ying, Grant, Deborah, Laflamme, Genevieve, Lin, Kuei-Ying, Markevitch, David Y., Mishra, Ruchika, McDermott, Martin, Pakdaman, Rowchanak, Petrakovsky, Oleg V., Vela, Jennifer E., Cihlar, Tomas
Published in Bioorganic & medicinal chemistry (15.05.2010)
Published in Bioorganic & medicinal chemistry (15.05.2010)
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Journal Article
Intracellular Metabolism of the Nucleotide Prodrug GS-9131, a Potent Anti-Human Immunodeficiency Virus Agent
RAY, Adrian S, VELA, Jennifer E, CIHLAR, Tomas, BOOJAMRA, Constantine G, LIJUN ZHANG, HUI, Hon, CALLEBAUT, Christian, STRAY, Kirsten, LIN, Kuei-Ying, YING GAO, MACKMAN, Richard L
Published in Antimicrobial Agents and Chemotherapy (01.02.2008)
Published in Antimicrobial Agents and Chemotherapy (01.02.2008)
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Synthesis and anti-HIV activity of GS-9148 (2′-Fd4AP), a novel nucleoside phosphonate HIV reverse transcriptase inhibitor
Boojamra, Constantine G., Mackman, Richard L., Markevitch, David Y., Prasad, Vidya, Ray, Adrian S., Douglas, Janet, Grant, Deborah, Kim, Choung U., Cihlar, Tomas
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
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Design, synthesis, and anti-HIV activity of 4′-modified carbocyclic nucleoside phosphonate reverse transcriptase inhibitors
Boojamra, Constantine G., Parrish, Jay P., Sperandio, David, Gao, Ying, Petrakovsky, Oleg V., Lee, Sharon K., Markevitch, David Y., Vela, Jennifer E., Laflamme, Genevieve, Chen, James M., Ray, Adrian S., Barron, Abraham C., Sparacino, Mark L., Desai, Manoj C., Kim, Choung U., Cihlar, Tomas, Mackman, Richard L.
Published in Bioorganic & medicinal chemistry (15.02.2009)
Published in Bioorganic & medicinal chemistry (15.02.2009)
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Journal Article
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B
Mackman, Richard L, Mish, Michael, Chin, Gregory, Perry, Jason K, Appleby, Todd, Aktoudianakis, Vangelis, Metobo, Sammy, Pyun, Peter, Niu, Congrong, Daffis, Stephane, Yu, Helen, Zheng, Jim, Villasenor, Armando G, Zablocki, Jeff, Chamberlain, Jason, Jin, Haolun, Lee, Gary, Suekawa-Pirrone, Kimberley, Santos, Rex, Delaney, William E, Fletcher, Simon P
Published in Journal of medicinal chemistry (24.09.2020)
Published in Journal of medicinal chemistry (24.09.2020)
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Prodrugs of a 1′-CN-4-Aza-7,9-dideazaadenosine C‑Nucleoside Leading to the Discovery of Remdesivir (GS-5734) as a Potent Inhibitor of Respiratory Syncytial Virus with Efficacy in the African Green Monkey Model of RSV
Mackman, Richard L, Hui, Hon C, Perron, Michel, Murakami, Eisuke, Palmiotti, Christopher, Lee, Gary, Stray, Kirsten, Zhang, Lijun, Goyal, Bindu, Chun, Kwon, Byun, Daniel, Siegel, Dustin, Simonovich, Scott, Du Pont, Venice, Pitts, Jared, Babusis, Darius, Vijjapurapu, Arya, Lu, Xianghan, Kim, Cynthia, Zhao, Xiaofeng, Chan, Julie, Ma, Bin, Lye, Diane, Vandersteen, Adelle, Wortman, Sarah, Barrett, Kimberly T, Toteva, Maria, Jordan, Robert, Subramanian, Raju, Bilello, John P, Cihlar, Tomas
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
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Journal Article
Inhaled remdesivir reduces viral burden in a nonhuman primate model of SARS-CoV-2 infection
Vermillion, Meghan S, Murakami, Eisuke, Ma, Bin, Pitts, Jared, Tomkinson, Adrian, Rautiola, Davin, Babusis, Darius, Irshad, Hammad, Seigel, Dustin, Kim, Cynthia, Zhao, Xiaofeng, Niu, Congrong, Yang, Jesse, Gigliotti, Andrew, Kadrichu, Nani, Bilello, John P, Ellis, Scott, Bannister, Roy, Subramanian, Raju, Smith, Bill, Mackman, Richard L, Lee, William A, Kuehl, Philip J, Hartke, Jim, Cihlar, Tomas, Porter, Danielle P
Published in Science translational medicine (23.02.2022)
Published in Science translational medicine (23.02.2022)
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Therapeutic treatment with an oral prodrug of the remdesivir parental nucleoside is protective against SARS-CoV-2 pathogenesis in mice
Schäfer, Alexandra, Martinez, David R, Won, John J, Meganck, Rita M, Moreira, Fernando R, Brown, Ariane J, Gully, Kendra L, Zweigart, Mark R, Conrad, William S, May, Samantha R, Dong, Stephanie, Kalla, Rao, Chun, Kwon, Du Pont, Venice, Babusis, Darius, Tang, Jennifer, Murakami, Eisuke, Subramanian, Raju, Barrett, Kimberly T, Bleier, Blake J, Bannister, Roy, Feng, Joy Y, Bilello, John P, Cihlar, Tomas, Mackman, Richard L, Montgomery, Stephanie A, Baric, Ralph S, Sheahan, Timothy P
Published in Science translational medicine (04.05.2022)
Published in Science translational medicine (04.05.2022)
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