title: A potent transactivation domain mimic with activity in living cells.
abstract: Transcriptional coactivator-binding peptoids were isolated from a large combinatorial library. One of these molecules is shown to function as a potent activation domain surrogate in mammalian cells. Up to a 900-fold increase in expression of a Gal4-responsive reporter gene is observed when a steroid conjugate of the peptoid is incubated with HeLa cells expressing a Gal4 DNA-binding domain (DBD)-glucocorticoid receptor ligand-binding domain (GRLBD) fusion protein.
authors.affiliation: Departments of Internal Medicine and Molecular Biology and Center for Biomedical Inventions, University of Texas Southwestern Medical Center, 5323 Harry Hines Boulevard, Dallas, TX 75390, USA.
authors.forename: Bo
authors.initials: B
authors.lastname: Liu
authors.forename: Prasanna G
authors.initials: PG
authors.lastname: Alluri
authors.forename: Peng
authors.initials: P
authors.lastname: Yu
authors.forename: Thomas
authors.initials: T
authors.lastname: Kodadek
mesh_terms: D000818:Animals; D040761:Biomimetic Materials / Q000737:chemistry / Q000378:metabolism; D050882:CREB-Binding Protein; D002463:Cell Membrane Permeability; D020650:Combinatorial Chemistry Techniques; D003907:Dexamethasone / Q000737:chemistry / Q000378:metabolism; D006801:Humans; D009687:Nuclear Proteins / Q000737:chemistry* / Q000378:metabolism; D009842:Oligopeptides / Q000737:chemistry* / Q000378:metabolism; D017434:Protein Structure, Tertiary; D011965:Receptors, Glucocorticoid / Q000819:agonists; D011993:Recombinant Fusion Proteins / Q000737:chemistry / Q000378:metabolism; D015534:Trans-Activators / Q000737:chemistry* / Q000378:metabolism
chemical_list: D009687:Nuclear Proteins; D009842:Oligopeptides; D011965:Receptors, Glucocorticoid; D011993:Recombinant Fusion Proteins; D015534:Trans-Activators; D003907:Dexamethasone; D050882:CREB-Binding Protein; C494363:CREBBP protein, human