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Items: 45

1.

Efficacy and safety of elbasvir/grazoprevir in participants with hepatitis C virus genotype 1, 4, or 6 infection from the Asia-Pacific region and Russia: Final results from the randomized C-CORAL study.

Wei L, Jia JD, Wang FS, Niu JQ, Zhao XM, Mu S, Liang LW, Wang Z, Hwang P, Robertson MN, Ingravallo P, Asante-Appiah E, Wei B, Evans B, Hanna GJ, Talwani R, Duan ZP, Zhdanov K, Cheng PN, Tanwandee T, Nguyen VK, Heo J, Isakov V, George J; C-CORAL Investigators.

J Gastroenterol Hepatol. 2019 Jan;34(1):12-21. doi: 10.1111/jgh.14509. Epub 2018 Dec 9.

PMID:
30311701
2.

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
3.

Characterization of hepatitis C virus resistance to grazoprevir reveals complex patterns of mutations following on-treatment breakthrough that are not observed at relapse.

Bonsall D, Black S, Howe AY, Chase R, Ingravallo P, Pak I, Brown A, Smith DA, Bowden R, Barnes E.

Infect Drug Resist. 2018 Aug 8;11:1119-1135. doi: 10.2147/IDR.S156581. eCollection 2018.

4.

Evolutionary pathways to NS5A inhibitor resistance in genotype 1 hepatitis C virus.

Zhou S, Williford SE, McGivern DR, Burch CL, Hu F, Benzine T, Ingravallo P, Asante-Appiah E, Howe AYM, Swanstrom R, Lemon SM.

Antiviral Res. 2018 Oct;158:45-51. doi: 10.1016/j.antiviral.2018.07.024. Epub 2018 Aug 3.

PMID:
30081054
5.

Elbasvir/grazoprevir in Asia-Pacific/Russian participants with chronic hepatitis C virus genotype 1, 4, or 6 infection.

George J, Burnevich E, Sheen IS, Heo J, Kinh NV, Tanwandee T, Cheng PN, Kim DY, Tak WY, Kizhlo S, Zhdanov K, Isakov V, Liang L, Lindore P, Ginanni J, Nguyen BY, Wahl J, Barr E, Robertson M, Ingravallo P, Talwani R; Cā€CORAL Study Investigators.

Hepatol Commun. 2018 Apr 4;2(5):595-606. doi: 10.1002/hep4.1177. eCollection 2018 May.

6.

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
7.

MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.

Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer M, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2018 Jun 1;28(10):1954-1957. doi: 10.1016/j.bmcl.2018.03.049. Epub 2018 Mar 20.

PMID:
29653894
8.

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.

9.

Unraveling the structural basis of grazoprevir potency against clinically relevant substitutions in hepatitis C virus NS3/4A protease from genotype 1a.

Guo Z, Black S, Hu Y, McMonagle P, Ingravallo P, Chase R, Curry S, Asante-Appiah E.

J Biol Chem. 2017 Apr 14;292(15):6202-6212. doi: 10.1074/jbc.M116.772996. Epub 2017 Feb 21.

10.

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.

11.

Discovery of Chromane Containing Hepatitis C Virus (HCV) NS5A Inhibitors with Improved Potency against Resistance-Associated Variants.

Yu W, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Coburn CA, Selyutin O, Chen L, Rokosz L, Agrawal S, Liu R, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA.

J Med Chem. 2016 Nov 23;59(22):10228-10243. Epub 2016 Nov 9.

PMID:
27792320
12.

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
13.

Alternative core development around the tetracyclic indole class of HCV NS5A inhibitors.

Tong L, Yu W, Coburn CA, Meinke PT, Nair AG, Dwyer MP, Chen L, Selyutin O, Rosenblum SB, Jiang Y, Fells J, Hu B, Zhong B, Soll RM, Liu R, Agrawal S, Xia E, Zhai Y, Kong R, Ingravallo P, Nomeir A, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5132-5137. doi: 10.1016/j.bmcl.2016.07.057. Epub 2016 Jul 25.

14.

Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Zhou G, Coburn CA, Zeng Q, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Ji T, Zan S, Chen L, Mazzola R, Kim JH, Sha D, Selyutin O, Rosenblum SB, Lavey B, Nair AG, Heon Kim S, Keertikar KM, Rokosz L, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4851-4856. doi: 10.1016/j.bmcl.2016.08.002. Epub 2016 Aug 2.

PMID:
27568086
15.

Matched and mixed cap derivatives in the tetracyclic indole class of HCV NS5A inhibitors.

Dwyer MP, Keertikar KM, Chen L, Tong L, Selyutin O, Nair AG, Yu W, Zhou G, Lavey BJ, Yang DY, Wong M, Kim SH, Coburn CA, Rosenblum SB, Zeng Q, Jiang Y, Shankar BB, Rizvi R, Nomeir AA, Liu R, Agrawal S, Xia E, Kong R, Zhai Y, Ingravallo P, Asante-Appiah E, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):4106-11. doi: 10.1016/j.bmcl.2016.06.063. Epub 2016 Jun 25.

PMID:
27423481
16.

Aryl or heteroaryl substituted aminal derivatives of HCV NS5A inhibitor MK-8742.

Yu W, Coburn CA, Nair AG, Wong M, Rosenblum SB, Zhou G, Dwyer MP, Tong L, Hu B, Zhong B, Hao J, Ji T, Zan S, Kim SH, Zeng Q, Selyutin O, Chen L, Masse F, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Lin M, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Aug 1;26(15):3414-20. doi: 10.1016/j.bmcl.2016.06.056. Epub 2016 Jun 22.

PMID:
27394665
17.

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
18.

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
19.

Discovery of fused tricyclic core containing HCV NS5A inhibitors with pan-genotype activity.

Yu W, Coburn CA, Yang DY, Meinke PT, Wong M, Rosenblum SB, Chen KX, Njoroge GF, Chen L, Dwyer MP, Jiang Y, Nair AG, Selyutin O, Tong L, Zeng Q, Zhong B, Ji T, Hu B, Agrawal S, Xia E, Zhai Y, Liu R, Kong R, Ingravallo P, Asante-Appiah E, Nomeir A, Fells J, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Jul 1;26(13):3158-3162. doi: 10.1016/j.bmcl.2016.04.084. Epub 2016 Apr 30.

PMID:
27180013
20.

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.

21.

Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.

Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA.

Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19.

PMID:
26850003
22.

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
23.

Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor elbasvir.

Liu R, Curry S, McMonagle P, Yeh WW, Ludmerer SW, Jumes PA, Marshall WL, Kong S, Ingravallo P, Black S, Pak I, DiNubile MJ, Howe AY.

Antimicrob Agents Chemother. 2015 Nov;59(11):6922-9. doi: 10.1128/AAC.01390-15. Epub 2015 Aug 24.

24.

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.

25.

A peptide derived from hepatitis C virus E2 envelope protein inhibits a post-binding step in HCV entry.

Liu R, Tewari M, Kong R, Zhang R, Ingravallo P, Ralston R.

Antiviral Res. 2010 May;86(2):172-9. doi: 10.1016/j.antiviral.2010.02.316. Epub 2010 Feb 13.

PMID:
20156485
26.

Screening for antiviral inhibitors of the HIV integrase-LEDGF/p75 interaction using the AlphaScreen luminescent proximity assay.

Hou Y, McGuinness DE, Prongay AJ, Feld B, Ingravallo P, Ogert RA, Lunn CA, Howe JA.

J Biomol Screen. 2008 Jun;13(5):406-14. doi: 10.1177/1087057108317060. Epub 2008 May 14.

PMID:
18480474
27.

In vitro antiviral activity of SCH446211 (SCH6), a novel inhibitor of the hepatitis C virus NS3 serine protease.

Liu R, Abid K, Pichardo J, Pazienza V, Ingravallo P, Kong R, Agrawal S, Bogen S, Saksena A, Cheng KC, Prongay A, Njoroge FG, Baroudy BM, Negro F.

J Antimicrob Chemother. 2007 Jan;59(1):51-8. Epub 2006 Dec 5.

PMID:
17151003
28.

Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection.

Venkatraman S, Bogen SL, Arasappan A, Bennett F, Chen K, Jao E, Liu YT, Lovey R, Hendrata S, Huang Y, Pan W, Parekh T, Pinto P, Popov V, Pike R, Ruan S, Santhanam B, Vibulbhan B, Wu W, Yang W, Kong J, Liang X, Wong J, Liu R, Butkiewicz N, Chase R, Hart A, Agrawal S, Ingravallo P, Pichardo J, Kong R, Baroudy B, Malcolm B, Guo Z, Prongay A, Madison V, Broske L, Cui X, Cheng KC, Hsieh Y, Brisson JM, Prelusky D, Korfmacher W, White R, Bogdanowich-Knipp S, Pavlovsky A, Bradley P, Saksena AK, Ganguly A, Piwinski J, Girijavallabhan V, Njoroge FG.

J Med Chem. 2006 Oct 5;49(20):6074-86.

PMID:
17004721
29.

Discovery of SCH446211 (SCH6): a new ketoamide inhibitor of the HCV NS3 serine protease and HCV subgenomic RNA replication.

Bogen SL, Arasappan A, Bennett F, Chen K, Jao E, Liu YT, Lovey RG, Venkatraman S, Pan W, Parekh T, Pike RE, Ruan S, Liu R, Baroudy B, Agrawal S, Chase R, Ingravallo P, Pichardo J, Prongay A, Brisson JM, Hsieh TY, Cheng KC, Kemp SJ, Levy OE, Lim-Wilby M, Tamura SY, Saksena AK, Girijavallabhan V, Njoroge FG.

J Med Chem. 2006 May 4;49(9):2750-7.

PMID:
16640336
30.

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.

31.

Plasmodium vivax merozoite surface protein PvMSP-3 beta is radically polymorphic through mutation and large insertions and deletions.

Rayner JC, Huber CS, Feldman D, Ingravallo P, Galinski MR, Barnwell JW.

Infect Genet Evol. 2004 Dec;4(4):309-19.

PMID:
15374528
32.

Extensive polymorphism in the plasmodium vivax merozoite surface coat protein MSP-3alpha is limited to specific domains.

Rayner JC, Corredor V, Feldman D, Ingravallo P, Iderabdullah F, Galinski MR, Barnwell JW.

Parasitology. 2002 Nov;125(Pt 5):393-405.

PMID:
12458823
33.

Merozoite surface protein-9 of Plasmodium vivax and related simian malaria parasites is orthologous to p101/ABRA of P. falciparum.

Vargas-Serrato E, Barnwell JW, Ingravallo P, Perler FB, Galinski MR.

Mol Biochem Parasitol. 2002 Mar;120(1):41-52.

PMID:
11849704
34.

Plasmodium vivax merozoite surface proteins-3beta and-3gamma share structural similarities with P. vivax merozoite surface protein-3alpha and define a new gene family.

Galinski MR, Ingravallo P, Corredor-Medina C, Al-Khedery B, Povoa M, Barnwell JW.

Mol Biochem Parasitol. 2001 Jun;115(1):41-53.

PMID:
11377738
35.

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
36.

Virus-specific cofactor requirement and chimeric hepatitis C virus/GB virus B nonstructural protein 3.

Butkiewicz N, Yao N, Zhong W, Wright-Minogue J, Ingravallo P, Zhang R, Durkin J, Standring DN, Baroudy BM, Sangar DV, Lemon SM, Lau JY, Hong Z.

J Virol. 2000 May;74(9):4291-301.

37.

RNA-dependent RNA polymerase activity encoded by GB virus-B non-structural protein 5B.

Zhong W, Ingravallo P, Wright-Minogue J, Uss AS, Skelton A, Ferrari E, Lau JY, Hong Z.

J Viral Hepat. 2000 Sep;7(5):335-42.

PMID:
10971821
38.
39.

Generation and characterization of a hepatitis C virus NS3 protease-dependent bovine viral diarrhea virus.

Lai VC, Zhong W, Skelton A, Ingravallo P, Vassilev V, Donis RO, Hong Z, Lau JY.

J Virol. 2000 Jul;74(14):6339-47.

40.

Nucleoside triphosphatase and RNA helicase activities associated with GB virus B nonstructural protein 3.

Zhong W, Ingravallo P, Wright-Minogue J, Skelton A, Uss AS, Chase R, Yao N, Lau JY, Hong Z.

Virology. 1999 Sep 1;261(2):216-26.

41.

Plasmodium vivax merozoite surface protein-3 contains coiled-coil motifs in an alanine-rich central domain.

Galinski MR, Corredor-Medina C, Povoa M, Crosby J, Ingravallo P, Barnwell JW.

Mol Biochem Parasitol. 1999 Jun 25;101(1-2):131-47.

PMID:
10413049
42.

Plasmodium vivax, P. cynomolgi, and P. knowlesi: identification of homologue proteins associated with the surface of merozoites.

Barnwell JW, Galinski MR, DeSimone SG, Perler F, Ingravallo P.

Exp Parasitol. 1999 Mar;91(3):238-49.

PMID:
10072326
43.

A reticulocyte-binding protein complex of Plasmodium vivax merozoites.

Galinski MR, Medina CC, Ingravallo P, Barnwell JW.

Cell. 1992 Jun 26;69(7):1213-26.

PMID:
1617731
44.
45.

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