A potent transactivation domain mimic with activity in living cells.
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.
Liu
Bo
B
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.
Alluri
Prasanna G
PG
Yu
Peng
P
Kodadek
Thomas
T
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
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