title: Metal-bis(2-picolyl)amine complexes as state 1(T) inhibitors of activated Ras protein.
abstract: Allosteric interactions: Metal(II) cyclens inhibit Ras-effector interactions by stabilizing a weak effector-binding state of Ras, state 1(T), and binding directly in the active site. The novel state (1T) inhibitor Zn(2+)-BPA (BPA = bis(2-picolyl)amine) binds outside the nucleotide binding pocket but nevertheless allosterically stabilizes state 1(T) and thus inhibits the Ras-Raf interaction.
authors.affiliation: Institut für Biophysik und Physikalische Biochemie, Universität Regensburg, Universitätsstrasse 31, 93053 Regensburg, Germany.
authors.forename: Ina C
authors.initials: IC
authors.lastname: Rosnizeck
authors.forename: Michael
authors.initials: M
authors.lastname: Spoerner
authors.forename: Tobias
authors.initials: T
authors.lastname: Harsch
authors.forename: Sandra
authors.initials: S
authors.lastname: Kreitner
authors.forename: Daniel
authors.initials: D
authors.lastname: Filchtinski
authors.forename: Christian
authors.initials: C
authors.lastname: Herrmann
authors.forename: Daniel
authors.initials: D
authors.lastname: Engel
authors.forename: Burkhard
authors.initials: B
authors.lastname: König
authors.forename: Hans Robert
authors.initials: HR
authors.lastname: Kalbitzer
mesh_terms: D000588:Amines / Q000737:chemistry*; D001665:Binding Sites; D056831:Coordination Complexes / Q000737:chemistry*; D003300:Copper / Q000737:chemistry; D015195:Drug Design; D008958:Models, Molecular; D010848:Picolinic Acids / Q000737:chemistry*; D015398:Signal Transduction; D015032:Zinc / Q000737:chemistry*; D018631:ras Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry* / Q000378:metabolism
chemical_list: C501847:2,2'-dipicolylamine; D000588:Amines; D056831:Coordination Complexes; D010848:Picolinic Acids; D003300:Copper; D018631:ras Proteins; D015032:Zinc