Biochemical characterization of recombinant influenza A polymerase heterotrimer complex: Endonuclease activity and evaluation of inhibitors

PLoS One. 2017 Aug 15;12(8):e0181969. doi: 10.1371/journal.pone.0181969. eCollection 2017.

Abstract

Influenza polymerase is a heterotrimer composed of polymerase acidic protein A (PA) and basic proteins 1 (PB1) and 2 (PB2). The endonuclease active site, located in the PA subunit, cleaves host mRNA to prime viral mRNA transcription, and is essential for viral replication. To date, the human influenza A endonuclease activity has only been studied on the truncated active-site containing N-terminal domain of PA (PAN) or full-length PA in the absence of PB1 or PB2. In this study, we characterized the endonuclease activity of recombinant proteins of influenza A/PR8 containing full length PA, PA/PB1 dimer, and PA/PB1/PB2 trimer, observing 8.3-, 265-, and 142-fold higher activity than PAN, respectively. Using the PA/PB1/PB2 trimer, we developed a robust endonuclease assay with a synthetic fluorogenic RNA substrate. The observed Km (150 ± 11 nM) and kcat [(1.4 ± 0.2) x 10-3s-1] values were consistent with previous reports using virion-derived replication complex. Two known influenza endonuclease phenylbutanoic acid inhibitors showed IC50 values of 10-20 nM, demonstrating the utility of this system for future high throughput screening.

MeSH terms

  • Endonucleases / antagonists & inhibitors*
  • Endonucleases / chemistry
  • Endonucleases / metabolism*
  • Enzyme Activation / drug effects
  • Enzyme Inhibitors / pharmacology*
  • Influenza A virus / drug effects*
  • Influenza A virus / enzymology*
  • Inhibitory Concentration 50
  • RNA, Messenger / metabolism
  • RNA-Dependent RNA Polymerase / antagonists & inhibitors
  • RNA-Dependent RNA Polymerase / chemistry
  • RNA-Dependent RNA Polymerase / metabolism*
  • Viral Proteins / antagonists & inhibitors
  • Viral Proteins / chemistry
  • Viral Proteins / metabolism

Substances

  • Enzyme Inhibitors
  • PB2 protein, Influenzavirus A
  • RNA, Messenger
  • Viral Proteins
  • influenza virus polymerase basic protein 1
  • RNA-Dependent RNA Polymerase
  • Endonucleases

Grants and funding

Gilead Sciences, Inc. provided support in the form of salaries for all authors, but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. The specific roles of these authors are articulated in the ‘author contributions’ section.