title: GPCR Activation and Endocytosis Induced by a 2D Material Agonist.
abstract: Agonist-induced activation and endocytosis of G protein-coupled receptors (GPCRs) are crucial for a number of physiological and pathological processes. However, tools that are available for probing GPCR endocytosis have been insufficient. Here, we developed a two-dimensional (2D) material agonist by supramolecular self-assembly between an endogenous agonist of κ-opioid receptor (KOR) and 2D molybdenum disulfide. The 2D material agonist has proven to be amenable for eliciting GPCR activation and endocytosis in cells stably expressing KOR rather than in those without KOR expression. Using super-resolution microscopy, we also show that the 2D material agonist colocalizes well with GFP-fused KOR intracellularly. Further, the endocytosed 2D material agonist can selectively produce reactive oxygen species in cells that overly express KOR, as controlled by light irradiation.
authors.affiliation: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, P. R. China.
authors.forename: Wei-Tao
authors.initials: WT
authors.lastname: Dou
authors.affiliation: National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 189 Guo Shoujing Road, Shanghai 201203, P. R. China.|University of Chinese Academy of Sciences, UCAS , No. 19A, Yuquan Road, Beijing 100049, P. R. China.
authors.forename: Ya
authors.initials: Y
authors.lastname: Kong
authors.affiliation: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, P. R. China.
authors.forename: Xiao-Peng
authors.identifier: http://orcid.org/0000-0002-8736-3511
authors.initials: XP
authors.lastname: He
authors.affiliation: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, P. R. China.
authors.forename: Guo-Rong
authors.initials: GR
authors.lastname: Chen
authors.affiliation: National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 189 Guo Shoujing Road, Shanghai 201203, P. R. China.|University of Chinese Academy of Sciences, UCAS , No. 19A, Yuquan Road, Beijing 100049, P. R. China.
authors.forename: Yi
authors.initials: Y
authors.lastname: Zang
authors.affiliation: National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 189 Guo Shoujing Road, Shanghai 201203, P. R. China.|University of Chinese Academy of Sciences, UCAS , No. 19A, Yuquan Road, Beijing 100049, P. R. China.
authors.forename: Jia
authors.initials: J
authors.lastname: Li
authors.affiliation: Key Laboratory for Advanced Materials & Institute of Fine Chemicals, School of Chemistry and Molecular Engineering, East China University of Science and Technology , 130 Meilong Road, Shanghai 200237, P. R. China.
authors.forename: He
authors.identifier: http://orcid.org/0000-0003-3547-7485
authors.initials: H
authors.lastname: Tian
mesh_terms: D004705:Endocytosis; D043562:Receptors, G-Protein-Coupled
chemical_list: D043562:Receptors, G-Protein-Coupled
keywords: 2D material; G protein-coupled receptor; endocytosis; fluorescence; imaging; ligand; peptide; photodynamic therapy