The global burden of respiratory syncytial virus (RSV) and severe associated disease is prodigious. RSV-specific vaccines have been launched recently but there is no antiviral medicine commercially available. RSV polymerase (L) protein is one of the promising antiviral targets, along with fusion and nucleocapsid proteins. During medicinal chemistry campaigns, two potent L-protein inhibitors (PC786 and PC751) were identified. Both compounds inhibited the RSV A/B-induced cytopathic effect in HEp-2 cells equally, but PC786 was more potent than PC751 in bronchial epithelial cells. Repeated treatment with escalating concentrations on RSV A2-infected HEp-2 cells revealed both inhibitors led to a Y1631H mutation in the L protein, but only PC786 induced a mutation in the M protein (V153A). By L protein fragment and M protein binding analysis, we showed that the M protein interacts with the 1392-1735 amino acid region of the L protein, where PC786 potentially binds. In addition, PC786 treatment or PC786-induced mutant RSV was found to increase M-protein nuclear localisation later in infection, concomitant with delayed fusion protein localisation at the budding viral filaments. As M protein is known to play a key role in virus assembly and budding late in infection, our data suggests that disrupting the interaction between the M and L proteins could provide a novel target for antiviral development.

Download full-text PDF

Source
http://dx.doi.org/10.3390/v16121881DOI Listing

Publication Analysis

Top Keywords

protein
10
respiratory syncytial
8
syncytial virus
8
hep-2 cells
8
mutation protein
8
protein pc786
8
rsv
5
pc786
5
interaction matrix
4
matrix protein
4

Similar Publications

Plant growth and development are tightly regulated by cell division, elongation, and differentiation. A visible plant phenotype at the tissue or organ level is coordinated at the cellular level. Among these cellular regulations (cell division, elongation and differentiation), cell division in plants follows the same universal mechanisms across kingdoms of life, and involves conserved cell cycle regulatory proteins (cyclins, cyclin-dependent kinase and cell cycle inhibitors).

View Article and Find Full Text PDF

Diabetic cardiomyopathy (DCM) is a major complication of type 2 diabetes mellitus (T2DM), but its effective prevention and treatment are still limited. We investigated the effects of GYY4137, a slow-releasing hydrogen sulfide donor, and its downstream mediator forkhead box protein O1 (FOXO1) on T2DM-associated DCM. , T2DM mice were induced by a high-fat diet coupled with streptozotocin injection.

View Article and Find Full Text PDF

Insect protein hydrolysates (PH) are emerging as valuable compounds with biological activity. The aim of the present study was to assess the potential cytoprotective effects of PH from the Black Soldier Fly (BPH, in the range 0.1-0.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!