title: An aptamer to the MAP kinase insert region.
abstract: Targeting functional, non-catalytic domains of protein kinases or other proteins is an emerging field in chemical biology research. Non-ATP competitive kinase inhibitors allow for the investigation of active-site independent functions, e.g., the biological role of protein-protein interactions. These inhibitors also serve as a starting point for developing novel therapeutic strategies. However, the identification of such inhibitors by means of conventional low molecular weight compounds represents a great challenge in modern drug discovery. Employing the mitogen-activated protein (MAP) kinase Erk2, we show that RNA aptamers have the capacity to be a novel, promising class of protein kinase inhibitors that can be applied to target individual subdomains and block domain specific functions without affecting kinase activity per se.
authors.affiliation: Life and Medical Sciences Institute , Gerhard-Domagk-Str.1, 53121 Bonn, Germany.
authors.forename: Sabine
authors.initials: S
authors.lastname: Lennarz
authors.forename: Elena
authors.initials: E
authors.lastname: Heider
authors.forename: Michael
authors.initials: M
authors.lastname: Blind
authors.forename: Günter
authors.initials: G
authors.lastname: Mayer
mesh_terms: D052157:Aptamers, Nucleotide / Q000737:chemistry / Q000494:pharmacology; D001483:Base Sequence; D001665:Binding Sites; D055808:Drug Discovery; D004926:Escherichia coli / Q000235:genetics; D006801:Humans; D019950:Mitogen-Activated Protein Kinase 1 / Q000037:antagonists & inhibitors* / Q000235:genetics; D008958:Models, Molecular; D008969:Molecular Sequence Data; D011485:Protein Binding; D047428:Protein Kinase Inhibitors / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins
chemical_list: D052157:Aptamers, Nucleotide; D047428:Protein Kinase Inhibitors; D011994:Recombinant Proteins; C535150:MAPK1 protein, human; D019950:Mitogen-Activated Protein Kinase 1