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Items: 30

1.

In Vitro Antiviral Profile of Ruzasvir, a Potent and Pangenotype Inhibitor of Hepatitis C Virus NS5A.

Asante-Appiah E, Liu R, Curry S, McMonagle P, Agrawal S, Carr D, Rokosz L, Lahser F, Bystol K, Chase R, Black S, Ferrari E, Ingravallo P, Tong L, Yu W, Kozlowski J.

Antimicrob Agents Chemother. 2018 Oct 24;62(11). pii: e01280-18. doi: 10.1128/AAC.01280-18. Print 2018 Nov.

PMID:
30150466
2.

Interim analysis of a 3-year follow-up study of NS5A and NS3 resistance-associated substitutions after treatment with grazoprevir-containing regimens in participants with chronic HCV infection.

Lahser F, Galloway A, Hwang P, Palcza J, Brunhofer J, Wahl J, Robertson M, Barr E, Black T, Asante-Appiah E, Haber B.

Antivir Ther. 2018;23(7):593-603. doi: 10.3851/IMP3253. Epub 2018 Jul 24.

PMID:
30038064
3.

Discovery of MK-6169, a Potent Pan-Genotype Hepatitis C Virus NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Substitutions.

Yu W, Tong L, Selyutin O, Chen L, Hu B, Zhong B, Hao J, Ji T, Zan S, Yin J, Ruck RT, Curry S, McMonagle P, Agrawal S, Rokosz L, Carr D, Ingravallo P, Bystol K, Lahser F, Liu R, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA.

J Med Chem. 2018 May 10;61(9):3984-4003. doi: 10.1021/acs.jmedchem.7b01927. Epub 2018 May 1.

PMID:
29681153
4.

Efficacy and safety of 12 weeks of elbasvir ± grazoprevir ± ribavirin in participants with hepatitis C virus genotype 2, 4, 5 or 6 infection: The C-SCAPE study.

Brown A, Hézode C, Zuckerman E, Foster GR, Zekry A, Roberts SK, Lahser F, Durkan C, Badshah C, Zhang B, Robertson M, Wahl J, Barr E, Haber B; C-SCAPE Study Investigators.

J Viral Hepat. 2018 May;25(5):457-464. doi: 10.1111/jvh.12801. Epub 2018 Mar 14.

PMID:
29152828
5.

Antiviral Activity and Resistance Analysis of NS3/4A Protease Inhibitor Grazoprevir and NS5A Inhibitor Elbasvir in Hepatitis C Virus GT4 Replicons.

Asante-Appiah E, Curry S, McMonagle P, Ingravallo P, Chase R, Nickle D, Qiu P, Howe A, Lahser FC.

Antimicrob Agents Chemother. 2017 Jun 27;61(7). pii: e00363-17. doi: 10.1128/AAC.00363-17. Print 2017 Jul.

6.

Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.

Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA.

J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15.

7.

Structure-activity relationships of proline modifications around the tetracyclic-indole class of NS5A inhibitors.

Tong L, Yu W, Coburn CA, Chen L, Selyutin O, Zeng Q, Dwyer MP, Nair AG, Shankar BB, Kim SH, Yang DY, Rosenblum SB, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Carr D, Curry S, McMonagle P, Bystol K, Lahser F, Ingravallo P, Chen S, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5354-5360. doi: 10.1016/j.bmcl.2016.08.097. Epub 2016 Sep 2.

PMID:
27680588
8.

PTC725, an NS4B-Targeting Compound, Inhibits a Hepatitis C Virus Genotype 3 Replicon, as Predicted by Genome Sequence Analysis and Determined Experimentally.

Graci JD, Jung SP, Pichardo J, Lahser F, Tong X, Gu Z, Colacino JM.

Antimicrob Agents Chemother. 2016 Nov 21;60(12):7060-7066. Print 2016 Dec.

9.

Development and Validation of a Template-Independent Next-Generation Sequencing Assay for Detecting Low-Level Resistance-Associated Variants of Hepatitis C Virus.

Wei B, Kang J, Kibukawa M, Chen L, Qiu P, Lahser F, Marton M, Levitan D.

J Mol Diagn. 2016 Sep;18(5):643-656. doi: 10.1016/j.jmoldx.2016.04.001. Epub 2016 Jul 7.

10.

Discovery of potent macrocyclic HCV NS5A inhibitors.

Yu W, Vibulbhan B, Rosenblum SB, Martin GS, Vellekoop AS, Holst CL, Coburn CA, Wong M, Selyutin O, Ji T, Zhong B, Hu B, Chen L, Dwyer MP, Jiang Y, Nair AG, Tong L, Zeng Q, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Fells J, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3793-9. doi: 10.1016/j.bmcl.2016.05.042. Epub 2016 May 17.

PMID:
27282743
11.

Alkyl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Coburn CA, Nair AG, Wong M, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Yang DY, Selyutin O, Jiang Y, Rosenblum SB, Kim SH, Lavey BJ, Zhou G, Rizvi R, Shankar BB, Zeng Q, Chen L, Agrawal S, Carr D, Rokosz L, Liu R, Curry S, McMonagle P, Ingravallo P, Lahser F, Asante-Appiah E, Nomeir A, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3800-5. doi: 10.1016/j.bmcl.2016.05.041. Epub 2016 May 14.

PMID:
27282742
12.

The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons.

Lahser FC, Bystol K, Curry S, McMonagle P, Xia E, Ingravallo P, Chase R, Liu R, Black T, Hazuda D, Howe AY, Asante-Appiah E.

Antimicrob Agents Chemother. 2016 Apr 22;60(5):2954-64. doi: 10.1128/AAC.00051-16. Print 2016 May.

13.

Discovery of 2-(4-sulfonamidophenyl)-indole 3-carboxamides as potent and selective inhibitors with broad hepatitis C virus genotype activity targeting HCV NS4B.

Zhang N, Turpoff A, Zhang X, Huang S, Liu Y, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Pichardo J, Colacino J, Lahser F, Ingravallo P, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):594-601. doi: 10.1016/j.bmcl.2015.11.065. Epub 2015 Nov 19.

PMID:
26652483
14.

HCV genotyping from NGS short reads and its application in genotype detection from HCV mixed infected plasma.

Qiu P, Stevens R, Wei B, Lahser F, Howe AY, Klappenbach JA, Marton MJ.

PLoS One. 2015 Apr 1;10(4):e0122082. doi: 10.1371/journal.pone.0122082. eCollection 2015.

15.

6-(Azaindol-2-yl)pyridine-3-sulfonamides as potent and selective inhibitors targeting hepatitis C virus NS4B.

Chen G, Ren H, Zhang N, Lennox W, Turpoff A, Paget S, Li C, Almstead N, Njoroge FG, Gu Z, Graci J, Jung SP, Colacino J, Lahser F, Zhao X, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):781-6. doi: 10.1016/j.bmcl.2014.12.093. Epub 2015 Jan 7.

PMID:
25613678
16.

Kinetic analyses reveal potent and early blockade of hepatitis C virus assembly by NS5A inhibitors.

McGivern DR, Masaki T, Williford S, Ingravallo P, Feng Z, Lahser F, Asante-Appiah E, Neddermann P, De Francesco R, Howe AY, Lemon SM.

Gastroenterology. 2014 Aug;147(2):453-62.e7. doi: 10.1053/j.gastro.2014.04.021. Epub 2014 Apr 22.

17.

Structure-activity relationship (SAR) optimization of 6-(indol-2-yl)pyridine-3-sulfonamides: identification of potent, selective, and orally bioavailable small molecules targeting hepatitis C (HCV) NS4B.

Zhang N, Zhang X, Zhu J, Turpoff A, Chen G, Morrill C, Huang S, Lennox W, Kakarla R, Liu R, Li C, Ren H, Almstead N, Venkatraman S, Njoroge FG, Gu Z, Clausen V, Graci J, Jung SP, Zheng Y, Colacino JM, Lahser F, Sheedy J, Mollin A, Weetall M, Nomeir A, Karp GM.

J Med Chem. 2014 Mar 13;57(5):2121-35. doi: 10.1021/jm401621g. Epub 2013 Dec 4.

PMID:
24266880
18.

Discovery of novel HCV inhibitors: synthesis and biological activity of 6-(indol-2-yl)pyridine-3-sulfonamides targeting hepatitis C virus NS4B.

Zhang X, Zhang N, Chen G, Turpoff A, Ren H, Takasugi J, Morrill C, Zhu J, Li C, Lennox W, Paget S, Liu Y, Almstead N, Njoroge FG, Gu Z, Komatsu T, Clausen V, Espiritu C, Graci J, Colacino J, Lahser F, Risher N, Weetall M, Nomeir A, Karp GM.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3947-53. doi: 10.1016/j.bmcl.2013.04.049. Epub 2013 Apr 30.

PMID:
23683597
19.

Identification of PTC725, an orally bioavailable small molecule that selectively targets the hepatitis C Virus NS4B protein.

Gu Z, Graci JD, Lahser FC, Breslin JJ, Jung SP, Crona JH, McMonagle P, Xia E, Liu S, Karp G, Zhu J, Huang S, Nomeir A, Weetall M, Almstead NG, Peltz SW, Tong X, Ralston R, Colacino JM.

Antimicrob Agents Chemother. 2013 Jul;57(7):3250-61. doi: 10.1128/AAC.00527-13. Epub 2013 Apr 29.

20.

Antiviral activity of boceprevir monotherapy in treatment-naive subjects with chronic hepatitis C genotype 2/3.

Silva MO, Treitel M, Graham DJ, Curry S, Frontera MJ, McMonagle P, Gupta S, Hughes E, Chase R, Lahser F, Barnard RJ, Howe AY, Howe JA.

J Hepatol. 2013 Jul;59(1):31-7. doi: 10.1016/j.jhep.2013.02.018. Epub 2013 Feb 27.

PMID:
23454058
21.

SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells.

Malcolm BA, Liu R, Lahser F, Agrawal S, Belanger B, Butkiewicz N, Chase R, Gheyas F, Hart A, Hesk D, Ingravallo P, Jiang C, Kong R, Lu J, Pichardo J, Prongay A, Skelton A, Tong X, Venkatraman S, Xia E, Girijavallabhan V, Njoroge FG.

Antimicrob Agents Chemother. 2006 Mar;50(3):1013-20.

22.

A continuous nonradioactive assay for RNA-dependent RNA polymerase activity.

Lahser FC, Malcolm BA.

Anal Biochem. 2004 Feb 15;325(2):247-54.

PMID:
14751259
23.

Conserved C-terminal threonine of hepatitis C virus NS3 regulates autoproteolysis and prevents product inhibition.

Wang W, Lahser FC, Yi M, Wright-Minogue J, Xia E, Weber PC, Lemon SM, Malcolm BA.

J Virol. 2004 Jan;78(2):700-9.

24.

Quantitative estimation of viral fitness using Pyrosequencing.

Lahser FC, Wright-Minogue J, Skelton A, Malcolm BA.

Biotechniques. 2003 Jan;34(1):26-8. No abstract available.

25.

Characterization of monoclonal antibodies that specifically recognize the palm subdomain of hepatitis C virus nonstructural protein 5B polymerase.

Ingravallo P, Lahser F, Xia E, Sodowich B, Lai VC, Hong Z, Zhong W.

Virus Res. 2001 Jun;75(2):179-87.

PMID:
11325472
28.

A small yeast RNA blocks hepatitis C virus internal ribosome entry site (HCV IRES)-mediated translation and inhibits replication of a chimeric poliovirus under translational control of the HCV IRES element.

Das S, Ott M, Yamane A, Tsai W, Gromeier M, Lahser F, Gupta S, Dasgupta A.

J Virol. 1998 Jul;72(7):5638-47. Erratum in: J Virol 1998 Nov;72(11):9419.

29.

A protein linkage map of the P2 nonstructural proteins of poliovirus.

Cuconati A, Xiang W, Lahser F, Pfister T, Wimmer E.

J Virol. 1998 Feb;72(2):1297-307.

30.

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