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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Biomimetic Materials / chemistry
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Biomimetic Materials / metabolism
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CREB-Binding Protein
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Cell Membrane Permeability
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Combinatorial Chemistry Techniques
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Dexamethasone / chemistry
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Dexamethasone / metabolism
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Humans
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Nuclear Proteins / chemistry*
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Nuclear Proteins / metabolism
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Oligopeptides / chemistry*
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Oligopeptides / metabolism
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Protein Structure, Tertiary
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Receptors, Glucocorticoid / agonists
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Recombinant Fusion Proteins / chemistry
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Recombinant Fusion Proteins / metabolism
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Trans-Activators / chemistry*
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Trans-Activators / metabolism
Substances
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Nuclear Proteins
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Oligopeptides
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Receptors, Glucocorticoid
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Recombinant Fusion Proteins
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Trans-Activators
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Dexamethasone
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CREB-Binding Protein
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CREBBP protein, human