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Under homeostatic conditions, NRF2 is sequestered in the cytoplasm through its interaction with the repressor protein KEAP1
Cambridge, MA, USA: 2014
Treatment of Leber's optic atrophy
As the most abundant subtype in the central nervous system, the stoichiometric ratio differences between ( 4 2 ) 2 2 and ( 4 2 ) 2 4 of 4 2 nAChR determine receptor sensitivity and functional characteristics toward nicotine: The ( 4 2 ) 2 2 subtype exhibits high agonist affinity, whereas the ( 4 2 ) 2 4 subtype demonstrates 34-fold enhanced activation efficacy despite lower affinity, establishing a dual regulatory paradigm of high-affinity and high-efficacy ( 4 or 2 subunits completely blocks nicotine-induced burst firing of VTA dopamine neurons and dopamine release in the nucleus accumbens, while mice expressing hypersensitive 4 mutants exhibit exaggerated rewarding responses to low-dose nicotine (Picciotto et al., 1998
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