title: Estradiol inhibits the activity of proton-coupled amino acid transporter PAT1 expressed in Xenopus oocytes.
abstract: Estrogen has great potential as a therapeutic agent in focal ischemic brain injury. Amino acids as energy resources and neurotransmitters in the central nervous system are crucial for proper neuronal function and excitability. The proton-coupled amino acid transporter PAT1 has clear potential in drug absorption. In this paper, human brain PAT1 was cloned and expressed in Xenopus oocytes. The effects of estradiol on the activity of PAT1 were investigated. Glycine-induced membrane currents mediated by PAT1 were measured using the two-electrode voltage clamp technique. The amplitude of the glycine-elicited current was decreased progressively with increasing concentrations of β-estradiol. A concentration-dependent outwards current of PAT1 was also detected by the presence of β-estradiol. We conclude that estrogen attenuates the activity of PAT1 by directly closing PAT1 channel. Our results may provide an additional mechanism for estrogen on neurotransmission and neuronal metabolism during ischemic injury.
authors.affiliation: Department of Physiology and Neurobiology, Xinxiang Medical University, Xinxiang, Henan, PR China.
authors.forename: Linlin
authors.initials: L
authors.lastname: Shan
authors.forename: Yujie
authors.initials: Y
authors.lastname: Yang
authors.forename: Jin
authors.initials: J
authors.lastname: Wang
authors.forename: Ji
authors.initials: J
authors.lastname: Zuo
authors.forename: Xianhong
authors.initials: X
authors.lastname: Dong
authors.forename: Chaokun
authors.initials: C
authors.lastname: Li
authors.forename: Dongliang
authors.initials: D
authors.lastname: Li
mesh_terms: D026905:Amino Acid Transport Systems / Q000037:antagonists & inhibitors* / Q000235:genetics* / Q000378:metabolism; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism / Q000502:physiology; D004553:Electric Conductivity; D055724:Electrophysiological Phenomena / Q000187:drug effects; D004958:Estradiol / Q000494:pharmacology*; D004967:Estrogens / Q000494:pharmacology*; D005260:Female; D015870:Gene Expression; D005998:Glycine / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D009865:Oocytes / Q000378:metabolism*; D027981:Symporters / Q000037:antagonists & inhibitors* / Q000235:genetics* / Q000378:metabolism; D014982:Xenopus laevis / Q000235:genetics*
chemical_list: D026905:Amino Acid Transport Systems; D004967:Estrogens; C475905:SLC36A1 protein, human; D027981:Symporters; D004958:Estradiol; D005998:Glycine