A highly potent long-acting small-molecule HIV-1 capsid inhibitor with efficacy in a humanized mouse model
Yant, Stephen R., Mulato, Andrew, Hansen, Derek, Tse, Winston C., Niedziela-Majka, Anita, Zhang, Jennifer R., Stepan, George J., Jin, Debi, Wong, Melanie H., Perreira, Jill M., Singer, Eric, Papalia, Giuseppe A., Hu, Eric Y., Zheng, Jim, Lu, Bing, Schroeder, Scott D., Chou, Kevin, Ahmadyar, Shekeba, Liclican, Albert, Yu, Helen, Novikov, Nikolai, Paoli, Eric, Gonik, Daniel, Ram, Renee R., Hung, Magdeleine, McDougall, William M., Brass, Abraham L., Sundquist, Wesley I., Cihlar, Tomas, Link, John O.
Published in Nature medicine (01.09.2019)
Published in Nature medicine (01.09.2019)
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Histone deacetylase inhibitor romidepsin induces HIV expression in CD4 T cells from patients on suppressive antiretroviral therapy at concentrations achieved by clinical dosing
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Published in PLoS pathogens (01.04.2014)
Published in PLoS pathogens (01.04.2014)
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Lenacapavir: A Novel, Potent, and Selective First-in-Class Inhibitor of HIV-1 Capsid Function Exhibits Optimal Pharmacokinetic Properties for a Long-Acting Injectable Antiretroviral Agent
Subramanian, Raju, Tang, Jennifer, Zheng, Jim, Lu, Bing, Wang, Kelly, Yant, Stephen R, Stepan, George J, Mulato, Andrew, Yu, Helen, Schroeder, Scott, Shaik, Naveed, Singh, Renu, Wolckenhauer, Scott, Chester, Anne, Tse, Winston C, Chiu, Anna, Rhee, Martin, Cihlar, Tomas, Rowe, William, Smith, Bill J
Published in Molecular pharmaceutics (04.12.2023)
Published in Molecular pharmaceutics (04.12.2023)
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Preclinical characterization of a non-peptidomimetic HIV protease inhibitor with improved metabolic stability
Mulato, Andrew, Lansdon, Eric, Aoyama, Ron, Voigt, Johannes, Lee, Michael, Liclican, Albert, Lee, Gary, Singer, Eric, Stafford, Brian, Gong, Ruoyu, Murray, Bernard, Chan, Julie, Lee, Johnny, Xu, Yili, Ahmadyar, Shekeba, Gonzalez, Ana, Cho, Aesop, Stepan, George J, Schmitz, Uli, Schultz, Brian, Marchand, Bruno, Brumshtein, Boris, Wang, Ruth, Yu, Helen, Cihlar, Tomas, Xu, Lianhong, Yant, Stephen R
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Role of Mitochondrial RNA Polymerase in the Toxicity of Nucleotide Inhibitors of Hepatitis C Virus
Feng, Joy Y, Xu, Yili, Barauskas, Ona, Perry, Jason K, Ahmadyar, Shekeba, Stepan, George, Yu, Helen, Babusis, Darius, Park, Yeojin, McCutcheon, Krista, Perron, Michel, Schultz, Brian E, Sakowicz, Roman, Ray, Adrian S
Published in Antimicrobial agents and chemotherapy (01.02.2016)
Published in Antimicrobial agents and chemotherapy (01.02.2016)
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Search for small molecule activators of latent HIV
Geleziunas, Romas, Stepan, George, Wei, George, Yu, Helen, Graupe, Michael, Pagratis, Nikos, Barnes, Tiffany, Cihlar, Tomas, Hesselgesser, Joe
Published in Retrovirology (25.05.2012)
Published in Retrovirology (25.05.2012)
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539. GS-CA2: A Novel, Potent, and Selective First-In-class Inhibitor of HIV-1 Capsid Function Displays Nonclinical Pharmacokinetics Supporting Long-Acting Potential in Humans
Zheng, Jim, Yant, Stephen R, Ahmadyar, Shekeba, Chan, Tiffany Y, Chiu, Anna, Cihlar, Tomas, Link, John O, Lu, Bing, Mwangi, Judy, Rowe, William, Schroeder, Scott D, Stepan, George J, Wang, Kelly Wei, Subramanian, Raju, Tse, Winston C
Published in Open forum infectious diseases (26.11.2018)
Published in Open forum infectious diseases (26.11.2018)
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In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate
Callebaut, Christian, Stepan, George, Tian, Yang, Miller, Michael D
Published in Antimicrobial agents and chemotherapy (01.10.2015)
Published in Antimicrobial agents and chemotherapy (01.10.2015)
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Clinical targeting of HIV capsid protein with a long-acting small molecule
Link, John O., Rhee, Martin S., Tse, Winston C., Zheng, Jim, Somoza, John R., Rowe, William, Begley, Rebecca, Chiu, Anna, Mulato, Andrew, Hansen, Derek, Singer, Eric, Tsai, Luong K., Bam, Rujuta A., Chou, Chien-Hung, Canales, Eda, Brizgys, Gediminas, Zhang, Jennifer R., Li, Jiayao, Graupe, Michael, Morganelli, Philip, Liu, Qi, Wu, Qiaoyin, Halcomb, Randall L., Saito, Roland D., Schroeder, Scott D., Lazerwith, Scott E., Bondy, Steven, Jin, Debi, Hung, Magdeleine, Novikov, Nikolai, Liu, Xiaohong, Villaseñor, Armando G., Cannizzaro, Carina E., Hu, Eric Y., Anderson, Robert L., Appleby, Todd C., Lu, Bing, Mwangi, Judy, Liclican, Albert, Niedziela-Majka, Anita, Papalia, Giuseppe A., Wong, Melanie H., Leavitt, Stephanie A., Xu, Yili, Koditek, David, Stepan, George J., Yu, Helen, Pagratis, Nikos, Clancy, Sheila, Ahmadyar, Shekeba, Cai, Terrence Z., Sellers, Scott, Wolckenhauer, Scott A., Ling, John, Callebaut, Christian, Margot, Nicolas, Ram, Renee R., Liu, Ya-Pei, Hyland, Rob, Sinclair, Gary I., Ruane, Peter J., Crofoot, Gordon E., McDonald, Cheryl K., Brainard, Diana M., Lad, Latesh, Swaminathan, Swami, Sundquist, Wesley I., Sakowicz, Roman, Chester, Anne E., Lee, William E., Daar, Eric S., Yant, Stephen R., Cihlar, Tomas
Published in Nature (London) (27.08.2020)
Published in Nature (London) (27.08.2020)
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Off-Target In Vitro Profiling Demonstrates that Remdesivir Is a Highly Selective Antiviral Agent
Xu, Yili, Barauskas, Ona, Kim, Cynthia, Babusis, Darius, Murakami, Eisuke, Kornyeyev, Dmytro, Lee, Gary, Stepan, George, Perron, Michel, Bannister, Roy, Schultz, Brian E, Sakowicz, Roman, Porter, Danielle, Cihlar, Tomas, Feng, Joy Y
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Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile
Tsiang, Manuel, Jones, Gregg S, Goldsmith, Joshua, Mulato, Andrew, Hansen, Derek, Kan, Elaine, Tsai, Luong, Bam, Rujuta A, Stepan, George, Stray, Kirsten M, Niedziela-Majka, Anita, Yant, Stephen R, Yu, Helen, Kukolj, George, Cihlar, Tomas, Lazerwith, Scott E, White, Kirsten L, Jin, Haolun
Published in Antimicrobial agents and chemotherapy (01.12.2016)
Published in Antimicrobial agents and chemotherapy (01.12.2016)
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Design and Synthesis of Novel HIV‑1 NNRTIs with Bicyclic Cores and with Improved Physicochemical Properties
Prener, Ladislav, Baszczyňski, Ondřej, Kaiser, Martin M., Dračínský, Martin, Stepan, George, Lee, Yu-Jen, Brumshtein, Boris, Yu, Helen, Jansa, Petr, Lansdon, Eric B., Janeba, Zlatko
Published in Journal of medicinal chemistry (09.02.2023)
Published in Journal of medicinal chemistry (09.02.2023)
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Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle
Mackman, Richard L, Steadman, Victoria A, Dean, David K, Jansa, Petr, Poullennec, Karine G, Appleby, Todd, Austin, Carol, Blakemore, Caroline A, Cai, Ruby, Cannizzaro, Carina, Chin, Gregory, Chiva, Jean-Yves C, Dunbar, Neil A, Fliri, Hans, Highton, Adrian J, Hui, Hon, Ji, Mingzhe, Jin, Haolun, Karki, Kapil, Keats, Andrew J, Lazarides, Linos, Lee, Yu-Jen, Liclican, Albert, Mish, Michael, Murray, Bernard, Pettit, Simon B, Pyun, Peter, Sangi, Michael, Santos, Rex, Sanvoisin, Jonathan, Schmitz, Uli, Schrier, Adam, Siegel, Dustin, Sperandio, David, Stepan, George, Tian, Yang, Watt, Gregory M, Yang, Hai, Schultz, Brian E
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Published in Journal of medicinal chemistry (08.11.2018)
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Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1
Šimon, Petr, Baszczyňski, Ondřej, Šaman, David, Stepan, George, Hu, Eric, Lansdon, Eric B., Jansa, Petr, Janeba, Zlatko
Published in European journal of medicinal chemistry (21.10.2016)
Published in European journal of medicinal chemistry (21.10.2016)
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Abyssomicin 2 Reactivates Latent HIV‑1 by a PKC- and HDAC-Independent Mechanism
León, Brian, Navarro, Gabriel, Dickey, Bailey J, Stepan, George, Tsai, Angela, Jones, Gregg S, Morales, Monica E, Barnes, Tiffany, Ahmadyar, Shekeba, Tsiang, Manuel, Geleziunas, Romas, Cihlar, Tomas, Pagratis, Nikos, Tian, Yang, Yu, Helen, Linington, Roger G
Published in Organic letters (16.01.2015)
Published in Organic letters (16.01.2015)
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A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities
Jansa, Petr, Baszczyňski, Ondřej, Dračínský, Martin, Votruba, Ivan, Zídek, Zdeněk, Bahador, Gina, Stepan, George, Cihlar, Tomas, Mackman, Richard, Holý, Antonín, Janeba, Zlatko
Published in European journal of medicinal chemistry (01.09.2011)
Published in European journal of medicinal chemistry (01.09.2011)
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Rapid In Vitro Evaluation of Antiretroviral Barrier to Resistance at Therapeutic Drug Levels
Mulato, Andrew, Hansen, Derek, Thielen, Alex, Porter, Danielle, Stepan, George, White, Kirsten, Daeumer, Martin, Cihlar, Tomas, Yant, Stephen R
Published in AIDS research and human retroviruses (01.12.2016)
Published in AIDS research and human retroviruses (01.12.2016)
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Inhibition of Hepatitis C Virus Replication by GS-6620, a Potent C-Nucleoside Monophosphate Prodrug
FENG, Joy Y, GUOFENG CHENG, YANG TIAN, LEE, Yu-Jen, STEPAN, George, LAGPACAN, Leanna L, DEBI JIN, HUNG, Magdeleine, KU, Karin S, BIN HAN, KITRINOS, Kathryn, PERRON, Michel, PERRY, Jason, BIRKUS, Gabriel, WONG, Kelly A, WEIDONG ZHONG, KIM, Choung U, CAREY, Anne, AESOP CHO, RAY, Adrian S, BARAUSKAS, Ona, YILI XU, FENAUX, Martijn, ENG, Stacey, TIRUNAGARI, Neeraj, BETTY PENG, MEI YU
Published in Antimicrobial agents and chemotherapy (01.04.2014)
Published in Antimicrobial agents and chemotherapy (01.04.2014)
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Synthesis and anti-human immunodeficiency virus activity of substituted (o,o-difluorophenyl)-linked-pyrimidines as potent non‐nucleoside reverse transcriptase inhibitors
Čechová, Lucie, Dejmek, Milan, Baszczyňski, Ondřej, Šaman, David, Gao, Liping, Hu, Eric, Stepan, George, Jansa, Petr, Janeba, Zlatko, Šimon, Petr
Published in Antiviral chemistry & chemotherapy (01.01.2019)
Published in Antiviral chemistry & chemotherapy (01.01.2019)
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Human cloned α1A-adrenoceptor isoforms display α1L-adrenoceptor pharmacology in functional studies
Daniels, Donald V., Gever, Joel R., Jasper, Jeffrey R., Kava, M.Shannon, Lesnick, John D., Meloy, Trena D., Stepan, George, Williams, Timothy J., Clarke, David E., Chang, David J., Ford, Anthony P.D.W.
Published in European journal of pharmacology (01.04.1999)
Published in European journal of pharmacology (01.04.1999)
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