Sandbox WWC8: Difference between revisions
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Importin α is a mediator protein that interacts with hundreds of different proteins in eukaryotic cells to ensure transport across the nuclear envelope through the nuclear pores. During early stages of infection, the NP is largely concentrated in the nucleus, importing viral RNA scripts for transcription and replication. The entrance of NP into the nucleus is guaranteed by the NP interaction with Importin α [1]. | Importin α is a mediator protein that interacts with hundreds of different proteins in eukaryotic cells to ensure transport across the nuclear envelope through the nuclear pores. During early stages of infection, the NP is largely concentrated in the nucleus, importing viral RNA scripts for transcription and replication. The entrance of NP into the nucleus is guaranteed by the NP interaction with Importin α [1]. | ||
[[Image:NP functional subunits.jpg]] | [[Image:NP functional-subunits.jpg]] | ||
===NP-CRM1=== | ===NP-CRM1=== | ||
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====Inhibition at the RNA-binding grove==== | ====Inhibition at the RNA-binding grove==== | ||
The RNA binding grove is a central focus in recent efforts to find new antiviral drugs. Inhibiting the RNA-binding activity of NP directly hinders the protein to import and export viral RNA scripts, thus slowing or stopping the replication cycle. The large size of the RNA binding grove poses a challenge to find suitable functional regions for small molecule inhibition. By the use of high-throughput techniques, S-naproxen has been identified to have sufficient binding activity on NP. The inhibitory effect of S-naproxen has been confirmed in-vitro and in-vivo [8]. The binding pocket around S-naproxen is defined by aromatic residues Tyr 148 and Phe 498, Glu 149, and several Arg residues (150, 152, 355, 361) [8]. Current studies explore the development of better naproxen-dervied inhibitors for the defined binding pocket [9]. | The RNA binding grove is a central focus in recent efforts to find new antiviral drugs. Inhibiting the RNA-binding activity of NP directly hinders the protein to import and export viral RNA scripts, thus slowing or stopping the replication cycle. The large size of the RNA binding grove poses a challenge to find suitable functional regions for small molecule inhibition. By the use of high-throughput techniques, S-naproxen has been identified to have sufficient binding activity on NP. The inhibitory effect of S-naproxen has been confirmed in-vitro and in-vivo [8]. The binding pocket around S-naproxen is defined by aromatic residues Tyr 148 and Phe 498, Glu 149, and several Arg residues (150, 152, 355, 361) [8]. Current studies explore the development of better naproxen-dervied inhibitors for the defined binding pocket [9]. | ||
[[Image:zoom binding site.jpg]] | |||
<Structure load='2IQH Binding site.pdb' size='350' frame='true' align='right' caption='Insert caption here' scene='Insert optional scene name here' /> | <Structure load='2IQH Binding site.pdb' size='350' frame='true' align='right' caption='Insert caption here' scene='Insert optional scene name here' /> | ||
