Glucocorticoid-regulated human serotonin transporter (5-HTT) expression is modulated by the 5-HTT gene-promotor-linked polymorphic region

J Neurochem. 2003 Sep;86(5):1072-8. doi: 10.1046/j.1471-4159.2003.01944.x.

Abstract

Mood, emotion and cognition are modulated by serotonergic neurotransmission, while the physiological function of serotonergic synapses depends on serotonin reuptake, which is mediated by the serotonin transporter (5-HTT). Allelic variation of 5-HTT expression in humans is caused by a functional gene-promoter polymorphism with two predominant variant alleles, which are associated with variations in anxiety measures as previously reported. Here we report that administration of dexamethasone, a potent glucocorticosteroid hormone, results in an increase in 5-HTT expression in immortalized human B-lymphoblastoid cells, which express the human 5-HTT. Functional reporter gene assays as well as 5-HT uptake and inhibitor binding measures revealed a genotype-dependent dose-response to glucocorticosteroid administration, which was antagonized by RU 38486, a non-specific glucocorticosteroid hormone antagonist. The allele-specific differences after administration of dexamethasone depended on the repetitive GC-rich sequence located approximately 1.4 kb upstream of the 5-HTT gene transcription site because of absence of a significant steroid effect after transfecting a deletional mutant reporter gene construct, which lacks this repetitive promoter sequence. Our findings may contribute to explain the vulnerability to stress-related disorders in susceptible individuals, in whom further clinical studies should follow up on these in vitro findings.

MeSH terms

  • B-Lymphocytes / drug effects
  • B-Lymphocytes / metabolism
  • Binding, Competitive / drug effects
  • Carrier Proteins / genetics*
  • Carrier Proteins / metabolism*
  • Cell Line
  • Choriocarcinoma / metabolism
  • Cocaine / analogs & derivatives*
  • Cocaine / pharmacokinetics
  • Dexamethasone / pharmacology
  • Dose-Response Relationship, Drug
  • Gene Expression Regulation / physiology*
  • Genes, Reporter
  • Glucocorticoids / metabolism*
  • Humans
  • Membrane Glycoproteins / genetics*
  • Membrane Glycoproteins / metabolism*
  • Membrane Transport Proteins*
  • Nerve Tissue Proteins*
  • Polymerase Chain Reaction
  • Promoter Regions, Genetic / physiology*
  • Serotonin Plasma Membrane Transport Proteins
  • Transfection

Substances

  • Carrier Proteins
  • Glucocorticoids
  • Membrane Glycoproteins
  • Membrane Transport Proteins
  • Nerve Tissue Proteins
  • SLC6A4 protein, human
  • Serotonin Plasma Membrane Transport Proteins
  • 2beta-carbomethoxy-3beta-(4-iodophenyl)tropane
  • Dexamethasone
  • Cocaine