scholarly journals Antiviral activity and molecular mechanism of an orally active respiratory syncytial virus fusion inhibitor

2005 ◽  
Vol 55 (3) ◽  
pp. 289-292 ◽  
Author(s):  
Christopher Cianci ◽  
Nicholas Meanwell ◽  
Mark Krystal
Keyword(s):  
Respiratory Syncytial Virus ◽  
Antiviral Activity ◽  
Molecular Mechanism ◽  
Fusion Inhibitor ◽  
Virus Fusion ◽  
Syncytial Virus ◽  
Orally Active

Respiratory syncytial virus fusion inhibitors. Part 3: Water-soluble benzimidazol-2-one derivatives with antiviral activity in vivo

2006 ◽  
Vol 16 (5) ◽  
pp. 1115-1122 ◽  
Author(s):  
Kuo-Long Yu ◽  
Xiangdong Alan Wang ◽  
Rita L. Civiello ◽  
Ashok K. Trehan ◽  
Bradley C. Pearce ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Antiviral Activity ◽  
Water Soluble ◽  
Fusion Inhibitors ◽  
Virus Fusion ◽  
Syncytial Virus

scholarly journals Pharmacological Characterization of TP0591816, a Novel Macrocyclic Respiratory Syncytial Virus Fusion Inhibitor with Antiviral Activity against F Protein Mutants

2020 ◽  
Vol 65 (1) ◽  
pp. e01407-20
Author(s):  
Ippei Yoshida ◽  
Kaho Arikawa ◽  
Yusuke Honma ◽  
Shoko Inatani ◽  
Mitsukane Yoshinaga ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Antiviral Activity ◽  
Heptad Repeat ◽  
Fusion Inhibitor ◽  
Rich Region ◽  
F Protein ◽  
Protein Mutants ◽  
Rsv Infection ◽  
Syncytial Virus ◽  
Tract Infections

ABSTRACTHuman respiratory syncytial virus (RSV) is a major cause of lower respiratory tract infections in early childhood. However, no vaccines have yet been approved for prevention of RSV infection, and the treatment options are limited. Therefore, development of effective and safe anti-RSV drugs is needed. In this study, we evaluated the antiviral activity and mechanism of action of a novel macrocyclic anti-RSV compound, TP0591816. TP0591816 showed significant antiviral activities against both subgroup A and subgroup B RSV, while exerting no cytotoxicity. Notably, the antiviral activity of TP0591816 was maintained against a known fusion inhibitor-resistant RSV strain with a mutation in the cysteine-rich region or in heptad repeat B. Results of a time-of-addition assay and a temperature shift assay indicated that TP0591816 inhibited fusion of RSV with the cell membrane during viral entry. In addition, TP0591816 added after cell infection also inhibited cell-cell fusion. A TP0591816-resistant virus strain selected by serial passage had an L141F mutation, but no mutation in the cysteine-rich region or in heptad repeat B in the fusion (F) protein. Treatment with TP0591816 reduced lung virus titers in a dose-dependent manner in a mouse model of RSV infection. Furthermore, the estimated effective dose of TP0591816 for use against F protein mutants was thought to be clinically realistic and potentially tolerable. Taken together, these findings suggest that TP0591816 is a promising novel candidate for the treatment of resistant RSV infection.

scholarly journals Therapeutic efficacy of a respiratory syncytial virus fusion inhibitor

2017 ◽  
Vol 8 (1) ◽  
Author(s):  
Dirk Roymans ◽  
Sarhad S Alnajjar ◽  
Michael B Battles ◽  
Panchan Sitthicharoenchai ◽  
Polina Furmanova-Hollenstein ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Therapeutic Efficacy ◽  
Fusion Inhibitor ◽  
Virus Fusion ◽  
Syncytial Virus

scholarly journals Antiviral Activity of TMC353121, a Respiratory Syncytial Virus (RSV) Fusion Inhibitor, in a Non-Human Primate Model

PLoS ONE ◽  
2015 ◽  
Vol 10 (5) ◽  
pp. e0126959 ◽  
Author(s):  
Gabriela Ispas ◽  
Anil Koul ◽  
Johan Verbeeck ◽  
Jennifer Sheehan ◽  
Brigitte Sanders-Beer ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Antiviral Activity ◽  
Fusion Inhibitor ◽  
Primate Model ◽  
Syncytial Virus ◽  
Human Primate

scholarly journals Antiviral and lung protective activity of a novel respiratory syncytial virus fusion inhibitor in a mouse model

2010 ◽  
Vol 38 (2) ◽  
pp. 401-408 ◽  
Author(s):  
W. Olszewska ◽  
G. Ispas ◽  
C. Schnoeller ◽  
D. Sawant ◽  
T. Van de Casteele ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Mouse Model ◽  
Fusion Inhibitor ◽  
Protective Activity ◽  
Virus Fusion ◽  
Syncytial Virus

scholarly journals Molecular mechanism of respiratory syncytial virus fusion inhibitors

2015 ◽  
Vol 12 (2) ◽  
pp. 87-93 ◽  
Author(s):  
Michael B Battles ◽  
Johannes P Langedijk ◽  
Polina Furmanova-Hollenstein ◽  
Supranee Chaiwatpongsakorn ◽  
Heather M Costello ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Molecular Mechanism ◽  
Fusion Inhibitors ◽  
Virus Fusion ◽  
Syncytial Virus
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