title: Synthesis of a quinazoline derivative: a new α₁-adrenoceptor ligand for conjugation to quantum dots to study α₁-adrenoceptors in living cells.
abstract: Quantum dots (QDs) that are conjugated to small molecule derivatives of drugs and endogenous ligands may be useful tools to study the distribution and dynamic of membrane bound receptors, ion channels and transporters in live cells. In order to use these tools, it is necessary to functionalize QDs with bioactive ligands. In this paper, we successfully synthesized a ligand of α(1)-adrenoceptor that could be conjugated to QDs. In addition, the conjugation of the ligands to QDs and their biological activity were evaluated through binding assay with 30 nM QD conjugates in living human embryonic kidney 293 cells.
authors.affiliation: School of Chemistry and Chemical Engineering, Shandong University, Shanda Nanlu 27, 250100 Jinan, Shandong Province, PR China.
authors.forename: Guoheng
authors.initials: G
authors.lastname: Zhou
authors.forename: Lei
authors.initials: L
authors.lastname: Wang
authors.forename: Yudao
authors.initials: Y
authors.lastname: Ma
authors.forename: Liping
authors.initials: L
authors.lastname: Wang
authors.forename: Youyi
authors.initials: Y
authors.lastname: Zhang
authors.forename: Wei
authors.initials: W
authors.lastname: Jiang
mesh_terms: D058668:Adrenergic alpha-1 Receptor Antagonists / Q000378:metabolism; D001681:Biological Assay; D001710:Biotin / Q000378:metabolism; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D057809:HEK293 Cells; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D008970:Molecular Weight; D010879:Piperazines / Q000378:metabolism; D011092:Polyethylene Glycols / Q000378:metabolism; D011224:Prazosin / Q000031:analogs & derivatives* / Q000737:chemistry / Q000378:metabolism; D011485:Protein Binding; D045663:Quantum Dots; D011799:Quinazolines / Q000737:chemistry* / Q000378:metabolism; D018340:Receptors, Adrenergic, alpha-1 / Q000378:metabolism*
chemical_list: C547713:ADRA1A protein, human; D058668:Adrenergic alpha-1 Receptor Antagonists; D008024:Ligands; D010879:Piperazines; D011799:Quinazolines; D018340:Receptors, Adrenergic, alpha-1; D011092:Polyethylene Glycols; C050977:2-(1-piperazinyl)-4-amino-6,7-dimethoxyquinazoline; D001710:Biotin; C015568:urapidil; D011224:Prazosin