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Items: 20


Potent Inhibitors of Hepatitis C Virus NS3 Protease: Employment of a Difluoromethyl Group as a Hydrogen-Bond Donor.

Zheng B, D'Andrea SV, Sun LQ, Wang AX, Chen Y, Hrnciar P, Friborg J, Falk P, Hernandez D, Yu F, Sheaffer AK, Knipe JO, Mosure K, Rajamani R, Good AC, Kish K, Tredup J, Klei HE, Paruchuri M, Ng A, Gao Q, Rampulla RA, Mathur A, Meanwell NA, McPhee F, Scola PM.

ACS Med Chem Lett. 2018 Jan 19;9(2):143-148. doi: 10.1021/acsmedchemlett.7b00503. eCollection 2018 Feb 8.


Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.

Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM.

J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26.


A Small Molecule Inhibitor Selectively Induces Apoptosis in Cells Transformed by High Risk Human Papilloma Viruses.

Sheaffer AK, Lee MS, Qi H, Chaniewski S, Zheng X, Farr GA, Esposito K, Harden D, Lei M, Schweizer L, Friborg J, Agler M, McPhee F, Gentles R, Beno BR, Chupak L, Mason S.

PLoS One. 2016 Jun 9;11(6):e0155909. doi: 10.1371/journal.pone.0155909. eCollection 2016.


The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5.


Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20.


Combinations of lambda interferon with direct-acting antiviral agents are highly efficient in suppressing hepatitis C virus replication.

Friborg J, Levine S, Chen C, Sheaffer AK, Chaniewski S, Voss S, Lemm JA, McPhee F.

Antimicrob Agents Chemother. 2013 Mar;57(3):1312-22. doi: 10.1128/AAC.02239-12. Epub 2012 Dec 28.


Preclinical Profile and Characterization of the Hepatitis C Virus NS3 Protease Inhibitor Asunaprevir (BMS-650032).

McPhee F, Sheaffer AK, Friborg J, Hernandez D, Falk P, Zhai G, Levine S, Chaniewski S, Yu F, Barry D, Chen C, Lee MS, Mosure K, Sun LQ, Sinz M, Meanwell NA, Colonno RJ, Knipe J, Scola P.

Antimicrob Agents Chemother. 2012 Oct;56(10):5387-96. doi: 10.1128/AAC.01186-12. Epub 2012 Aug 6.


Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.

McPhee F, Friborg J, Levine S, Chen C, Falk P, Yu F, Hernandez D, Lee MS, Chaniewski S, Sheaffer AK, Pasquinelli C.

Antimicrob Agents Chemother. 2012 Jul;56(7):3670-81. doi: 10.1128/AAC.00308-12. Epub 2012 Apr 16.


Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C.

Pasquinelli C, McPhee F, Eley T, Villegas C, Sandy K, Sheridan P, Persson A, Huang SP, Hernandez D, Sheaffer AK, Scola P, Marbury T, Lawitz E, Goldwater R, Rodriguez-Torres M, Demicco M, Wright D, Charlton M, Kraft WK, Lopez-Talavera JC, Grasela DM.

Antimicrob Agents Chemother. 2012 Apr;56(4):1838-44. doi: 10.1128/AAC.05854-11. Epub 2012 Jan 30.


Development of a chimeric replicon system for phenotypic analysis of NS3 protease sequences from HCV clinical isolates.

Sheaffer AK, Lee MS, Hernandez D, Chaniewski S, Yu F, Falk P, Friborg J, Zhai G, McPhee F.

Antivir Ther. 2011;16(5):705-18. doi: 10.3851/IMP1825.


Herpes simplex virus DNA cleavage and packaging proteins associate with the procapsid prior to its maturation.

Sheaffer AK, Newcomb WW, Gao M, Yu D, Weller SK, Brown JC, Tenney DJ.

J Virol. 2001 Jan;75(2):687-98.


Evidence for controlled incorporation of herpes simplex virus type 1 UL26 protease into capsids.

Sheaffer AK, Newcomb WW, Brown JC, Gao M, Weller SK, Tenney DJ.

J Virol. 2000 Aug;74(15):6838-48.


Isolation of herpes simplex virus procapsids from cells infected with a protease-deficient mutant virus.

Newcomb WW, Trus BL, Cheng N, Steven AC, Sheaffer AK, Tenney DJ, Weller SK, Brown JC.

J Virol. 2000 Feb;74(4):1663-73.


Physical and functional interactions between the herpes simplex virus UL15 and UL28 DNA cleavage and packaging proteins.

Koslowski KM, Shaver PR, Casey JT 2nd, Wilson T, Yamanaka G, Sheaffer AK, Tenney DJ, Pederson NE.

J Virol. 1999 Feb;73(2):1704-7.


Lobucavir is phosphorylated in human cytomegalovirus-infected and -uninfected cells and inhibits the viral DNA polymerase.

Tenney DJ, Yamanaka G, Voss SM, Cianci CW, Tuomari AV, Sheaffer AK, Alam M, Colonno RJ.

Antimicrob Agents Chemother. 1997 Dec;41(12):2680-5.


The human cytomegalovirus UL98 gene encodes the conserved herpesvirus alkaline nuclease.

Sheaffer AK, Weinheimer SP, Tenney DJ.

J Gen Virol. 1997 Nov;78 ( Pt 11):2953-61.


Aminodiol HIV protease inhibitors. Synthesis and structure-activity relationships of P1/P1' compounds: correlation between lipophilicity and cytotoxicity.

Chen P, Cheng PT, Alam M, Beyer BD, Bisacchi GS, Dejneka T, Evans AJ, Greytok JA, Hermsmeier MA, Humphreys WG, Jacobs GA, Kocy O, Lin PF, Lis KA, Marella MA, Ryono DE, Sheaffer AK, Spergel SH, Sun CQ, Tino JA, Vite G, Colonno RJ, Zahler R, Barrish JC.

J Med Chem. 1996 May 10;39(10):1991-2007.


Characterization of monoclonal antibodies recognizing amino- and carboxy-terminal epitopes of the herpes simplex virus UL42 protein.

Sheaffer AK, Hurlburt WW, Stevens JT, Bifano M, Hamatake RK, Colonno RJ, Tenney DJ.

Virus Res. 1995 Oct;38(2-3):305-14.


Sequence-dependent primer synthesis by the herpes simplex virus helicase-primase complex.

Tenney DJ, Sheaffer AK, Hurlburt WW, Bifano M, Hamatake RK.

J Biol Chem. 1995 Apr 21;270(16):9129-36.

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