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27 results on '"Eggers, Betsy"'

6. Functionalized triazines as potent HCV entry inhibitors

Author

Mull, Eric S., Sun, Li-Qiang, Zhao, Qian, Eggers, Betsy, Pokornowski, Kevin, Zhai, Guangzhi, Rajamani, Ramkumar, Jenkins, Susan, Kramer, Melissa, Wang, Ying-Kai, Fang, Hua, Tenney, Daniel, Baldick, Carl J., Cockett, Mark I., Meanwell, Nicholas A., and Scola, Paul M.

Published
2017
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11. Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 12. Structure–Activity Relationships Associated with 4-Fluoro-6-azaindole Derivatives Leading to the Identification of 1-(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-585248)

Author

Regueiro-Ren, Alicia, primary, Xue, Qiufen M., additional, Swidorski, Jacob J., additional, Gong, Yi-Fei, additional, Mathew, Marina, additional, Parker, Dawn D., additional, Yang, Zheng, additional, Eggers, Betsy, additional, D’Arienzo, Celia, additional, Sun, Yongnian, additional, Malinowski, Jacek, additional, Gao, Qi, additional, Wu, Dedong, additional, Langley, David R., additional, Colonno, Richard J., additional, Chien, Caly, additional, Grasela, Dennis M., additional, Zheng, Ming, additional, Lin, Pin-Fang, additional, Meanwell, Nicholas A., additional, and Kadow, John F., additional

Published
2013
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12. High-Throughput Screening and Rapid Inhibitor Triage Using an Infectious Chimeric Hepatitis C Virus

Author

Wichroski, Michael J., primary, Fang, Jie, additional, Eggers, Betsy J., additional, Rose, Ronald E., additional, Mazzucco, Charles E., additional, Pokornowski, Kevin A., additional, Baldick, Carl J., additional, Anthony, Monique N., additional, Dowling, Craig J., additional, Barber, Lauren E., additional, Leet, John E., additional, Beno, Brett R., additional, Gerritz, Samuel W., additional, Agler, Michele L., additional, Cockett, Mark I., additional, and Tenney, Daniel J., additional

Published
2012
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13. In Vitro Antiviral Characteristics of HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068

Author

Nowicka-Sans, Beata, primary, Gong, Yi-Fei, additional, McAuliffe, Brian, additional, Dicker, Ira, additional, Ho, Hsu-Tso, additional, Zhou, Nannan, additional, Eggers, Betsy, additional, Lin, Pin-Fang, additional, Ray, Neelanjana, additional, Wind-Rotolo, Megan, additional, Zhu, Li, additional, Majumdar, Antara, additional, Stock, David, additional, Lataillade, Max, additional, Hanna, George J., additional, Matiskella, John D., additional, Ueda, Yasutsugu, additional, Wang, Tao, additional, Kadow, John F., additional, Meanwell, Nicholas A., additional, and Krystal, Mark, additional

Published
2012
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14. In Vivo Patterns of Resistance to the HIV Attachment Inhibitor BMS-488043

Author

Zhou, Nannan, primary, Nowicka-Sans, Beata, additional, Zhang, Sharon, additional, Fan, Li, additional, Fang, Jie, additional, Fang, Hua, additional, Gong, Yi-Fei, additional, Eggers, Betsy, additional, Langley, David R., additional, Wang, Tao, additional, Kadow, John, additional, Grasela, Dennis, additional, Hanna, George J., additional, Alexander, Louis, additional, Colonno, Richard, additional, Krystal, Mark, additional, and Lin, Pin-Fang, additional

Published
2011
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15. A Novel Small Molecule Inhibitor of Hepatitis C Virus Entry

Author

Baldick, Carl J., primary, Wichroski, Michael J., additional, Pendri, Annapurna, additional, Walsh, Ann W., additional, Fang, Jie, additional, Mazzucco, Charles E., additional, Pokornowski, Kevin A., additional, Rose, Ronald E., additional, Eggers, Betsy J., additional, Hsu, Mayla, additional, Zhai, Weixu, additional, Zhai, Guangzhi, additional, Gerritz, Samuel W., additional, Poss, Michael A., additional, Meanwell, Nicholas A., additional, Cockett, Mark I., additional, and Tenney, Daniel J., additional

Published
2010
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16. Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects

Author

Wang, Tao, primary, Yin, Zhiwei, additional, Zhang, Zhongxing, additional, Bender, John A., additional, Yang, Zhong, additional, Johnson, Graham, additional, Yang, Zheng, additional, Zadjura, Lisa M., additional, D’Arienzo, Celia J., additional, DiGiugno Parker, Dawn, additional, Gesenberg, Christophe, additional, Yamanaka, Gregory A., additional, Gong, Yi-Fei, additional, Ho, Hsu-Tso, additional, Fang, Hua, additional, Zhou, Nannan, additional, McAuliffe, Brian V., additional, Eggers, Betsy J., additional, Fan, Li, additional, Nowicka-Sans, Beata, additional, Dicker, Ira B., additional, Gao, Qi, additional, Colonno, Richard J., additional, Lin, Pin-Fang, additional, Meanwell, Nicholas A., additional, and Kadow, John F., additional

Published
2009
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17. W1805 Entecavir Maintains a High Genetic Barrier to HBV Resistance Through 6 Years in NaïVE Patients

Author

Tenney, Daniel J., primary, Pokornowski, Kevin A., additional, Rose, Ronald E., additional, Baldick, Carl J., additional, Eggers, Betsy J., additional, Fang, Jie, additional, Wichroski, Michael J., additional, Diva, Ulysses A., additional, Xu, Dong, additional, Wilber, Richard B., additional, Brett-Smith, Helena, additional, and Iloeje, Uchenna H., additional

Published
2009
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18. Inhibition of Hepatitis B Virus Polymerase by Entecavir

Author

Langley, David R., primary, Walsh, Ann W., additional, Baldick, Carl J., additional, Eggers, Betsy J., additional, Rose, Ronald E., additional, Levine, Steven M., additional, Kapur, A. Jayne, additional, Colonno, Richard J., additional, and Tenney, Daniel J., additional

Published
2007
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19. Two-Year Assessment of Entecavir Resistance in Lamivudine-Refractory Hepatitis B Virus Patients Reveals Different Clinical Outcomes Depending on the Resistance Substitutions Present

Author

Tenney, Daniel J., primary, Rose, Ronald E., additional, Baldick, Carl J., additional, Levine, Steven M., additional, Pokornowski, Kevin A., additional, Walsh, Ann W., additional, Fang, Jie, additional, Yu, Cheng-Fang, additional, Zhang, Sharon, additional, Mazzucco, Charles E., additional, Eggers, Betsy, additional, Hsu, Mayla, additional, Plym, Mary Jane, additional, Poundstone, Patricia, additional, Yang, Joanna, additional, and Colonno, Richard J., additional

Published
2007
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21. In VitroAntiviral Characteristics of HIV-1 Attachment Inhibitor BMS-626529, the Active Component of the Prodrug BMS-663068

Author

Nowicka-Sans, Beata, Gong, Yi-Fei, McAuliffe, Brian, Dicker, Ira, Ho, Hsu-Tso, Zhou, Nannan, Eggers, Betsy, Lin, Pin-Fang, Ray, Neelanjana, Wind-Rotolo, Megan, Zhu, Li, Majumdar, Antara, Stock, David, Lataillade, Max, Hanna, George J., Matiskella, John D., Ueda, Yasutsugu, Wang, Tao, Kadow, John F., Meanwell, Nicholas A., and Krystal, Mark

Abstract

ABSTRACTBMS-663068 is the phosphonooxymethyl prodrug of BMS-626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+T cells. The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. In order to better understand the anti-HIV-1 spectrum of BMS-626529 against HIV-1, in vitroactivities against a wide variety of laboratory strains and clinical isolates were determined. BMS-626529 had half-maximal effective concentration (EC50) values of <10 nM against the vast majority of viral isolates; however, susceptibility varied by >6 log10, with half-maximal effective concentration values in the low pM range against the most susceptible viruses. The in vitroantiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life. Finally, in two-drug combination studies, BMS-626529 demonstrated additive or synergistic interactions with antiretroviral drugs of different mechanistic classes. These results suggest that BMS-626529 should be active against the majority of HIV-1 viruses and support the continued clinical development of the compound.

Published
2012
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22. In Vivo Patterns of Resistance to the HIV Attachment Inhibitor BMS-488043

Author

Zhou, Nannan, Nowicka-Sans, Beata, Zhang, Sharon, Fan, Li, Fang, Jie, Fang, Hua, Gong, Yi-Fei, Eggers, Betsy, Langley, David R., Wang, Tao, Kadow, John, Grasela, Dennis, Hanna, George J., Alexander, Louis, Colonno, Richard, Krystal, Mark, and Lin, Pin-Fang

Abstract

Attachment inhibitors (AI) are a novel class of HIV-1 antivirals, with little information available on clinical resistance. BMS-488043 is an orally bioavailable AI that binds to gp120 of HIV-1 and abrogates its binding to CD4+lymphocytes. A clinical proof-of-concept study of the AI BMS-488043, administered as monotherapy for 8 days, demonstrated significant viral load reductions. In order to examine the effects of AI monotherapy on HIV-1 sensitivity, phenotypic sensitivity assessment of baseline and postdosing (day 8) samples was performed. These analyses revealed that four subjects had emergent phenotypic resistance (a 50% effective concentration [EC50] >10-fold greater than the baseline value) and four had high baseline EC50s (>200 nM). Population sequencing and sequence determination of cloned envelope genes uncovered five gp120 mutations at four loci (V68A, L116I, S375I/N, and M426L) associated with BMS-488043 resistance. Substitution at the 375 locus, located near the CD4 binding pocket, was the most common (maintained in 5/8 subjects at day 8). The five substitutions were evaluated for their effects on AI sensitivity through reverse genetics in functional envelopes, confirming their role in decreasing sensitivity to the drug. Additional analyses revealed that these substitutions did not alter sensitivity to other HIV-1 entry inhibitors. Thus, our studies demonstrate that although the majority of the subjects' viruses maintained sensitivity to BMS-488043, substitutions can be selected that decrease HIV-1 susceptibility to the AI. Most importantly, the substitutions described here are not associated with resistance to other approved antiretrovirals, and therefore, attachment inhibitors could complement the current arsenal of anti-HIV agents.

Published
2010

23. In VivoPatterns of Resistance to the HIV Attachment Inhibitor BMS-488043

Author

Zhou, Nannan, Nowicka-Sans, Beata, Zhang, Sharon, Fan, Li, Fang, Jie, Fang, Hua, Gong, Yi-Fei, Eggers, Betsy, Langley, David R., Wang, Tao, Kadow, John, Grasela, Dennis, Hanna, George J., Alexander, Louis, Colonno, Richard, Krystal, Mark, and Lin, Pin-Fang

Abstract

ABSTRACTAttachment inhibitors (AI) are a novel class of HIV-1 antivirals, with little information available on clinical resistance. BMS-488043 is an orally bioavailable AI that binds to gp120 of HIV-1 and abrogates its binding to CD4+lymphocytes. A clinical proof-of-concept study of the AI BMS-488043, administered as monotherapy for 8 days, demonstrated significant viral load reductions. In order to examine the effects of AI monotherapy on HIV-1 sensitivity, phenotypic sensitivity assessment of baseline and postdosing (day 8) samples was performed. These analyses revealed that four subjects had emergent phenotypic resistance (a 50% effective concentration [EC50] >10-fold greater than the baseline value) and four had high baseline EC50s (>200 nM). Population sequencing and sequence determination of cloned envelope genes uncovered five gp120 mutations at four loci (V68A, L116I, S375I/N, and M426L) associated with BMS-488043 resistance. Substitution at the 375 locus, located near the CD4 binding pocket, was the most common (maintained in 5/8 subjects at day 8). The five substitutions were evaluated for their effects on AI sensitivity through reverse genetics in functional envelopes, confirming their role in decreasing sensitivity to the drug. Additional analyses revealed that these substitutions did not alter sensitivity to other HIV-1 entry inhibitors. Thus, our studies demonstrate that although the majority of the subjects' viruses maintained sensitivity to BMS-488043, substitutions can be selected that decrease HIV-1 susceptibility to the AI. Most importantly, the substitutions described here are not associated with resistance to other approved antiretrovirals, and therefore, attachment inhibitors could complement the current arsenal of anti-HIV agents.

Published
2010
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24. parCMutations in Fluoroquinolone-Resistant Borrelia burgdorferi

Author

Galbraith, Kendal M., Ng, Amanda C., Eggers, Betsy J., Kuchel, Craig R., Eggers, Christian H., and Samuels, D. Scott

Abstract

ABSTRACTWe have isolated in vitro fluoroquinolone-resistant mutants of the Lyme disease agent, Borrelia burgdorferi. Mutations in parC, which encodes a subunit of topoisomerase IV, were associated with loss of susceptibility to sparfloxacin, moxifloxacin, and Bay-Y3118, but not ciprofloxacin. This is the first description of fluoroquinolone resistance in the spirochete phylum.

Published
2005
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25. Open to the Future.

Author

Eggers, Betsy

Subjects
*INTERIOR architecture, *REGIONAL libraries
Abstract

The article evaluates the architectural design of the Vancouver Community library in Vancouver, Washington that was designed by architectural firm Miller Hull Partnership LLC.

Published
2015

26. From Disaster to Delight.

Author

Eggers, Betsy

Subjects
*INTERIOR architecture, *PUBLIC libraries
Abstract

The article evaluates the architectural design of the Cedar Rapids Public Library in Cedar Rapids, Iowa that was designed by architectural firm OPN Architects Inc.

Published
2015

27. Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 12. Structure–Activity Relationships Associated with 4-Fluoro-6-azaindole Derivatives Leading to the Identification of 1-(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione(BMS-585248)

Author

Regueiro-Ren, Alicia, Xue, Qiufen M., Swidorski, Jacob J., Gong, Yi-Fei, Mathew, Marina, Parker, Dawn D., Yang, Zheng, Eggers, Betsy, D’Arienzo, Celia, Sun, Yongnian, Malinowski, Jacek, Gao, Qi, Wu, Dedong, Langley, David R., Colonno, Richard J., Chien, Caly, Grasela, Dennis M., Zheng, Ming, Lin, Pin-Fang, and Meanwell, Nicholas A.

Subjects
*ANTI-HIV agents, *STRUCTURE-activity relationships, *AZAINDOLE derivatives, *VIRAL envelope proteins, *HETEROCYCLIC compounds synthesis, *PHARMACOKINETICS, *HYDROGEN bonding
Abstract

A series of highly potent HIV-1 attachment inhibitorswith 4-fluoro-6-azaindole core heterocycles that target the viralenvelope protein gp120 has been prepared. Substitution in the 7-positionof the azaindole core with amides (12a,b), C-linked heterocycles (12c–l),and N-linked heterocycles (12m–u)provided compounds with subnanomolar potency in a pseudotype infectivityassay and good pharmacokinetic profiles in vivo. A predictive model was developed from the initial SAR in which thepotency of the analogues correlated with the ability of the substituentin the 7-position of the azaindole to adopt a coplanar conformationby either forming internal hydrogen bonds or avoiding repulsive substitutionpatterns. 1-(4-Benzoylpiperazin-1-yl)-2-(4-fluoro-7-[1,2,3]triazol-1-yl-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione(BMS-585248, 12m) exhibited much improved in vitro potencyand pharmacokinetic properties than the previous clinical candidateBMS-488043 (1). The predicted low clearance in humans,modest protein binding, and good potency in the presence of 40% humanserum for 12mled to its selection for human clinicalstudies. [ABSTRACT FROM AUTHOR]

Published
2013
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