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Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice
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Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice
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Journal Article
Monoterpenoid aryl hydrocarbon receptor allosteric antagonists protect against ultraviolet skin damage in female mice
2023
Overview
The human aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor that is a pivotal regulator of human physiology and pathophysiology. Allosteric inhibition of AhR was previously thought to be untenable. Here, we identify carvones as noncompetitive, insurmountable antagonists of AhR and characterize the structural and functional consequences of their binding. Carvones do not displace radiolabeled ligands from binding to AhR but instead bind allosterically within the bHLH/PAS-A region of AhR. Carvones do not influence the translocation of ligand-activated AhR into the nucleus but inhibit the heterodimerization of AhR with its canonical partner ARNT and subsequent binding of AhR to the promoter of
CYP1A1
. As a proof of concept, we demonstrate physiologically relevant Ahr-antagonism by carvones in vivo in female mice. These substances establish the molecular basis for selective targeting of AhR regardless of the type of ligand(s) present and provide opportunities for the treatment of disease processes modified by AhR.
The aryl hydrocarbon receptor regulates the expression of genes involved in many cell processes and its dysregulation has been implicated in different diseases. Here, the authors identify dietary monoterpenoid carvone as an atypical non-competitive antagonist of human aryl hydrocarbon receptor and demonstrate that it can protect against ultraviolet skin damage in female mice.
Publisher
Nature Publishing Group UK,Nature Publishing Group,Nature Portfolio
Subject
/ 13/1
/ 13/51
/ 13/95
/ 14
/ 14/63
/ 38
/ 38/109
/ 38/15
/ 38/77
/ 42
/ 64
/ 64/60
/ 692/4017
/ 82/29
/ 82/58
/ 96
/ Animals
/ Aryl Hydrocarbon Receptor Nuclear Translocator - genetics
/ Aryl Hydrocarbon Receptor Nuclear Translocator - metabolism
/ Binding
/ Carvone
/ Cytochrome P-450 CYP1A1 - genetics
/ Damage
/ Female
/ Females
/ Humanities and Social Sciences
/ Ligands
/ Mice
/ Receptors, Aryl Hydrocarbon - genetics
/ Receptors, Aryl Hydrocarbon - metabolism
/ Science
