Na1.7 inhibitors for the treatment of chronic pain.

Steven J McKerrall, Daniel P Sutherlin

Journal: Bioorganic & medicinal chemistry letters 2019;28(19):3141-3149

PMID: 30139550

Full Text on Elsevier Science View on PubMed

Abstract

The voltage gated sodium channel Na1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive efforts to discover potent, selective, and efficacious Na1.7 inhibitors for the treatment of chronic pain. This digest will introduce the structure and function of Na1.7 and highlight the wealth of recent developments on a diverse array of Na1.7 inhibitors, including optimization of their potency, selectivity, and PK/PD relationships.

Address: Discovery Chemistry, Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, USA. Electronic address: [email protected].; Discovery Chemistry, Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, USA.

DOI: 10.1016/j.bmcl.2018.08.007