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Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses

David H. Drewry, Frances Potjewyd, Armin Bayati, Jeffery L. Smith, Rebekah J. Dickmander, Stefanie Howell, Sharon Taft-Benz, Sophia M. Min, Mohammad Anwar Hossain, Mark T. Heise, Peter S. McPherson, Nathaniel J. Moorman, Alison D. Axtman

2022Journal of Medicinal Chemistry22 citationsDOIOpen Access PDF

Abstract

disrupts multiple phases of the lifecycle of β-coronaviruses: viral replication and viral entry. The diverse antiviral roles of PIKfyve have not been previously probed comprehensively in a single study or using the same compound set. Our scaffold is a distinct chemotype that lacks the canonical morpholine hinge-binder of classical lipid kinase inhibitors and has a non-overlapping kinase off-target profile with known PIKfyve inhibitors. Our chemical probe set can be used by the community to further characterize the role of PIKfyve in virology.

Topics & Concepts

ChemistryChemical biologyBiochemistryDrug discoveryKinomeKinaseCell biologyComputational biologyCombinatorial chemistryBiologyCalcium signaling and nucleotide metabolismSARS-CoV-2 and COVID-19 ResearchCOVID-19 Clinical Research Studies
Identification and Utilization of a Chemical Probe to Interrogate the Roles of PIKfyve in the Lifecycle of β-Coronaviruses | Litcius