Nav1.7 inhibitors for the treatment of chronic pain |
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Authors: | Steven J. McKerrall Daniel P. Sutherlin |
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Affiliation: | Discovery Chemistry, Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, USA |
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Abstract: | The voltage gated sodium channel Nav1.7 plays an essential role in the transmission of pain signals. Strong human genetic validation has motivated extensive efforts to discover potent, selective, and efficacious Nav1.7 inhibitors for the treatment of chronic pain. This digest will introduce the structure and function of Nav1.7 and highlight the wealth of recent developments on a diverse array of Nav1.7 inhibitors, including optimization of their potency, selectivity, and PK/PD relationships. |
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Keywords: | SCN9A Voltage gated sodium channel Pain |
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