Characterization of HCV Ns3/4a protease inhibition by Itmn-191 reveals picomolar potency and slow dissociation: Implications for the use of Itmn-191 in chronic HCV treatment

被引:0
|
作者
Rajagopalan, P. I. Ravi
Misialek, Shawn
Blatt, Lawrence M.
Seiwert, Scott D.
Kossen, Karl
机构
关键词
D O I
暂无
中图分类号
R57 [消化系及腹部疾病];
学科分类号
摘要
引用
收藏
页码:A782 / A782
页数:1
相关论文
共 24 条
  • [1] IMPACT OF LOW DOSE RITONAVIR BOOSTING ON THE PHARMACOKINETICS OF RG7227 (ITMN-191), A HIGHLY POTENT AND SELECTIVE INHIBITOR OF THE HCV NS3/4A PROTEASE
    Haznedar, J. Oe.
    Fretland, J.
    Leong, G.
    Blotner, S.
    Hill, T.
    Smith, P.
    Tran, J. Q.
    [J]. JOURNAL OF HEPATOLOGY, 2010, 52 : S293 - S293
  • [2] Discovery of Danoprevir (ITMN-191/R7227), a Highly Selective and Potent Inhibitor of Hepatitis C Virus (HCV) NS3/4A Protease
    Jiang, Yutong
    Andrews, Steven W.
    Condroski, Kevin R.
    Buckman, Brad
    Serebryany, Vlad
    Wenglowsky, Steve
    Kennedy, April L.
    Madduru, Machender R.
    Wang, Bin
    Lyon, Michael
    Doherty, George A.
    Woodard, Benjamin T.
    Lemieux, Christine
    Do, Mary Geck
    Zhang, Hailong
    Ballard, Joshua
    Vigers, Guy
    Brandhuber, Barbra J.
    Stengel, Peter
    Josey, John A.
    Beigelman, Leonid
    Blatt, Lawrence
    Seiwert, Scott D.
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2014, 57 (05) : 1753 - 1769
  • [3] Preclinical Characteristics of the Hepatitis C Virus NS3/4A Protease Inhibitor ITMN-191 (R7227)
    Seiwert, Scott D.
    Andrews, Steven W.
    Jiang, Yutong
    Serebryany, Vladimir
    Tan, Hua
    Kossen, Karl
    Rajagopalan, P. T. Ravi
    Misialek, Shawn
    Stevens, Sarah K.
    Stoycheva, Antitsa
    Hong, Jin
    Lim, Sharlene R.
    Qin, Xiaoli
    Rieger, Robert
    Condroski, Kevin R.
    Zhang, Hailong
    Do, Mary Geck
    Lemieux, Christine
    Hingorani, Gary P.
    Hartley, Dylan P.
    Josey, John A.
    Pan, Lin
    Beigelman, Leonid
    Blatt, Lawrence M.
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2008, 52 (12) : 4432 - 4441
  • [4] Sequence variation of NS3/4A in HCV replicons exposed to ITMN-191 concentrations encompassing those likely to be achieved following clinical dosing
    Seiwert, S. D.
    Hong, J.
    Lim, S. R.
    Wang, T.
    Tan, H.
    Blatt, L. M.
    [J]. JOURNAL OF HEPATOLOGY, 2007, 46 : S244 - S245
  • [5] Inhibition and Binding Kinetics of the Hepatitis C Virus NS3 Protease Inhibitor ITMN-191 Reveals Tight Binding and Slow Dissociative Behavior
    Rajagopalan, Ravi
    Misialck, Shawn
    Stevens, Sarah K.
    Myszka, David G.
    Brandhuber, Barbara J.
    Ballard, Joshua A.
    Andrews, Steven W.
    Seiwert, Scott D.
    Kossen, Karl
    [J]. BIOCHEMISTRY, 2009, 48 (11) : 2559 - 2568
  • [6] Generation and characterization of HCV replicons with reduced sensitivity to ITMN 191, a macrocyclic inhibitor of NS3/4A
    Seiwert, Scott
    Andrews, Steven W.
    Tan, Hua
    Condroski, Kevin R.
    Ballard, Joshua A.
    Bernat, Bryan A.
    Josey, John A.
    Blatt, Lawrence M.
    [J]. GASTROENTEROLOGY, 2006, 130 (04) : A754 - A754
  • [7] RITONAVIR BOOSTING OF LOW DOSE RG7227/ITMN-191, HCV NS3/4A PROTEASE INHIBITOR, RESULTS IN ROBUST REDUCTION IN HCV RNA AT LOWER EXPOSURES THAN PROVIDED BY UNBOOSTED REGIMENS
    Gane, E.
    Rouzier, R.
    Stedman, C.
    Wiercinska-Drapalo, A.
    Horban, A.
    Chang, L.
    Zhang, Y.
    Sampeur, P.
    Najera, I.
    Shulman, N.
    Smith, P.
    Tran, J.
    [J]. JOURNAL OF HEPATOLOGY, 2010, 52 : S16 - S17
  • [8] In vitro synergistic antiviral activity of ITMN-191, an orally active inhibitor of the hepatitis C virus (HCV) NS3/4A protease, in combination with PEG-Interferon alfa-2A
    Tan, Hua
    Seiwert, Scott D.
    Blatt, Lawrence M.
    [J]. HEPATOLOGY, 2006, 44 (04) : 534A - 534A
  • [9] COMBINATION OF THE NS3/4A PROTEASE INHIBITOR ITMN-191 WITH THE ALLOSTERIC NS5B POLYMERASE INHIBITOR ITMN-8020 ENHANCES REPLICON CLEARANCE AND REDUCES THE EMERGENCE OF DRUG RESISTANT VARIANTS
    Tan, H.
    Wang, G.
    Moy, C.
    Kossen, K.
    Rajagopalan, R.
    Misialek, S.
    Ruhrmund, D.
    Hooi, L.
    Snarskaya, N.
    Stoycheva, A.
    Buckman, B.
    Seiwert, S.
    Beigelman, L.
    [J]. JOURNAL OF HEPATOLOGY, 2009, 50 : S340 - S341
  • [10] Additive to synergistic antiviral effects of an NS3/4A protease inhibitor (ITMN-191) and an NS5B RNA-dependent RNA polymerase inhibitor (R1479) in an HCV replicon system
    Seiwert, S. D.
    Tan, H.
    Blatt, L. M.
    [J]. JOURNAL OF HEPATOLOGY, 2007, 46 : S167 - S167