title: Formation, recognition and bioactivities of a novel G-quadruplex in the STAT3 gene.
abstract: G-Quadruplexes have been proved to exist in 5'-untranslated region (5'-UTR), promoter, intron and exon regions of many human genes. Here we report an intramolecular G-quadruplex formed by a G-rich sequence in the 3'-flanking region of signal transducers and activators of transcription 3 (STAT3) gene. The results showed that this G-rich sequence could affect the expression of STAT3. When the STAT3 G-quadruplex was stabilized by a novel non-planar ligand Cepharanthine (CEP), the decreased expression of STAT3 was observed in primary cultured cardiomyocytes. We also demonstrated that the down-regulation of STAT3 was most likely occurred at the transcriptional level. Our results provide a new clue for studying the G-quadruplex formation, recognition and function in the 3'-flanking region of gene.
authors.affiliation: Beijing National Laboratory for Molecular Sciences, Key Laboratory of Bioorganic Chemistry and Molecular Engineering of Ministry of Education, Department of Chemical Biology, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China.
authors.forename: Sen
authors.initials: S
authors.lastname: Lin
authors.forename: Sufang
authors.initials: S
authors.lastname: Li
authors.forename: Zan
authors.initials: Z
authors.lastname: Chen
authors.forename: Xiangwei
authors.initials: X
authors.lastname: He
authors.forename: Youyi
authors.initials: Y
authors.lastname: Zhang
authors.forename: Xiaojie
authors.initials: X
authors.lastname: Xu
authors.forename: Ming
authors.initials: M
authors.lastname: Xu
authors.forename: Gu
authors.initials: G
authors.lastname: Yuan
mesh_terms: D024509:3' Flanking Region / Q000502:physiology*; D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D044182:Benzylisoquinolines / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D002478:Cells, Cultured; D015536:Down-Regulation; D015195:Drug Design; D054856:G-Quadruplexes; D015870:Gene Expression; D005786:Gene Expression Regulation; D006801:Humans; D008024:Ligands; D008156:Luciferases / Q000235:genetics / Q000378:metabolism; D058990:Molecular Targeted Therapy; D032383:Myocytes, Cardiac / Q000378:metabolism; D009369:Neoplasms / Q000188:drug therapy / Q000503:physiopathology; D050796:STAT3 Transcription Factor / Q000235:genetics* / Q000378:metabolism; D052117:Benzodioxoles
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D044182:Benzylisoquinolines; D008024:Ligands; D008156:Luciferases; D050796:STAT3 Transcription Factor; C494086:STAT3 protein, human; C006947:cepharanthine; D052117:Benzodioxoles