Abstract
The transient receptor potential vanilloid 5 (TRPV5) channel is a highly calcium selective ion channel that regulates systemic calcium homeostasis by acting as a critical gate for calcium reabsorption in the kidney. Human polymorphisms of this channel have exemplified the importance of TRPV5 in disorders of calcium homeostasis, but atomic level information regarding this channel had remained unknown. To address this gap, we utilized cryo‐electron microscopy (cryo‐EM) to understand the gating and modulation of TRPV5. Moreover, this newly obtained structural information coupled with structure‐based virtual screening allowed us to uncover novel inhibitors of TRPV5 and revealed unique mechanisms of TRPV5 inhibition. These studies have thus expanded the base of understanding of TRPV5 at the atomic level and laid the foundation for future rational drug design.Support or Funding InformationNIGMS R01GM103899; NIGMS R01GM129357
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