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Your search keyword '"Babusis, Darius"' showing total 13 results
Start Over Author "Babusis, Darius" Journal antimicrobial agents and chemotherapy
13 results on '"Babusis, Darius"'

1. Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells

Author

Li, Ruidong, primary, Liclican, Albert, additional, Xu, Yili, additional, Pitts, Jared, additional, Niu, Congrong, additional, Zhang, Jingyu, additional, Kim, Cynthia, additional, Zhao, Xiaofeng, additional, Soohoo, Daniel, additional, Babusis, Darius, additional, Yue, Qin, additional, Ma, Bin, additional, Murray, Bernard P., additional, Subramanian, Raju, additional, Xie, Xuping, additional, Zou, Jing, additional, Bilello, John P., additional, Li, Li, additional, Schultz, Brian E., additional, Sakowicz, Roman, additional, Smith, Bill J., additional, Shi, Pei-Yong, additional, Murakami, Eisuke, additional, and Feng, Joy Y., additional

Published
2021
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2. Off-Target In Vitro Profiling Demonstrates that Remdesivir Is a Highly Selective Antiviral Agent

Author

Xu, Yili, primary, Barauskas, Ona, additional, Kim, Cynthia, additional, Babusis, Darius, additional, Murakami, Eisuke, additional, Kornyeyev, Dmytro, additional, Lee, Gary, additional, Stepan, George, additional, Perron, Michel, additional, Bannister, Roy, additional, Schultz, Brian E., additional, Sakowicz, Roman, additional, Porter, Danielle, additional, Cihlar, Tomas, additional, and Feng, Joy Y., additional

Published
2021
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3. Nucleotide Prodrug Containing a Nonproteinogenic Amino Acid To Improve Oral Delivery of a Hepatitis C Virus Treatment

Author

Feng, Joy Y., primary, Wang, Ting, additional, Park, Yeojin, additional, Babusis, Darius, additional, Birkus, Gabriel, additional, Xu, Yili, additional, Voitenleitner, Christian, additional, Fenaux, Martijn, additional, Yang, Huiling, additional, Eng, Stacey, additional, Tirunagari, Neeraj, additional, Kirschberg, Thorsten, additional, Cho, Aesop, additional, and Ray, Adrian S., additional

Published
2018
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5. Off-Target In VitroProfiling Demonstrates that Remdesivir Is a Highly Selective Antiviral Agent

Author

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, and Feng, Joy Y.

Abstract

Remdesivir (RDV, GS-5734), the first FDA-approved antiviral for the treatment of COVID-19, is a single diastereomer monophosphoramidate prodrug of an adenosine analogue. It is intracellularly metabolized into the active triphosphate form, which in turn acts as a potent and selective inhibitor of multiple viral RNA polymerases.

Published
2021
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6. Role of Mitochondrial RNA Polymerase in the Toxicity of Nucleotide Inhibitors of Hepatitis C Virus

Author

Feng, Joy Y., primary, Xu, Yili, additional, Barauskas, Ona, additional, Perry, Jason K., additional, Ahmadyar, Shekeba, additional, Stepan, George, additional, Yu, Helen, additional, Babusis, Darius, additional, Park, Yeojin, additional, McCutcheon, Krista, additional, Perron, Michel, additional, Schultz, Brian E., additional, Sakowicz, Roman, additional, and Ray, Adrian S., additional

Published
2016
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8. Metabolism and Pharmacokinetics of the Anti-Hepatitis C Virus Nucleotide Prodrug GS-6620

Author

Murakami, Eisuke, primary, Wang, Ting, additional, Babusis, Darius, additional, Lepist, Eve-Irene, additional, Sauer, Dorothea, additional, Park, Yeojin, additional, Vela, Jennifer E., additional, Shih, Robert, additional, Birkus, Gabriel, additional, Stefanidis, Dimitrios, additional, Kim, Choung U., additional, Cho, Aesop, additional, and Ray, Adrian S., additional

Published
2014
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9. Compared to Subcutaneous Tenofovir, Oral Tenofovir Disoproxyl Fumarate Administration Preferentially Concentrates the Drug into Gut-Associated Lymphoid Cells in Simian Immunodeficiency Virus-Infected Macaques

Author

Van Rompay, Koen K. A., primary, Babusis, Darius, additional, Abbott, Zachary, additional, Geng, Yongzhi, additional, Jayashankar, Kartika, additional, Johnson, Jeffrey A., additional, Lipscomb, Jonathan, additional, Heneine, Walid, additional, Abel, Kristina, additional, and Ray, Adrian S., additional

Published
2012
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10. Metabolic Activation of the Anti-Hepatitis C Virus Nucleotide Prodrug PSI-352938

Author

Niu, Congrong, primary, Tolstykh, Tatiana, additional, Bao, Haiying, additional, Park, Yeojin, additional, Babusis, Darius, additional, Lam, Angela M., additional, Bansal, Shalini, additional, Du, Jinfa, additional, Chang, Wonsuk, additional, Reddy, P. Ganapati, additional, Zhang, Hai-Ren, additional, Woolley, Joseph, additional, Wang, Li-Quan, additional, Chao, Piyun B., additional, Ray, Adrian S., additional, Otto, Michael J., additional, Sofia, Michael J., additional, Furman, Phillip A., additional, and Murakami, Eisuke, additional

Published
2012
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13. Role of Mitochondrial RNA Polymerase in the Toxicity of Nucleotide Inhibitors of Hepatitis C Virus

Author

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, and Ray, Adrian S.

Abstract

ABSTRACTToxicity has emerged during the clinical development of many but not all nucleotide inhibitors (NI) of hepatitis C virus (HCV). To better understand the mechanism for adverse events, clinically relevant HCV NI were characterized in biochemical and cellular assays, including assays of decreased viability in multiple cell lines and primary cells, interaction with human DNA and RNA polymerases, and inhibition of mitochondrial protein synthesis and respiration. NI that were incorporated by the mitochondrial RNA polymerase (PolRMT) inhibited mitochondrial protein synthesis and showed a corresponding decrease in mitochondrial oxygen consumption in cells. The nucleoside released by the prodrug balapiravir (R1626), 4′-azido cytidine, was a highly selective inhibitor of mitochondrial RNA transcription. The nucleotide prodrug of 2′-C-methyl guanosine, BMS-986094, showed a primary effect on mitochondrial function at submicromolar concentrations, followed by general cytotoxicity. In contrast, NI containing multiple ribose modifications, including the active forms of mericitabine and sofosbuvir, were poor substrates for PolRMT and did not show mitochondrial toxicity in cells. In general, these studies identified the prostate cell line PC-3 as more than an order of magnitude more sensitive to mitochondrial toxicity than the commonly used HepG2 cells. In conclusion, analogous to the role of mitochondrial DNA polymerase gamma in toxicity caused by some 2′-deoxynucleotide analogs, there is an association between HCV NI that interact with PolRMT and the observation of adverse events. More broadly applied, the sensitive methods for detecting mitochondrial toxicity described here may help in the identification of mitochondrial toxicity prior to clinical testing.

Published
2015
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