Abstract
Encoded self-assembling chemical (ESAC) libraries are characterized by the covalent display of chemical moieties at the extremity of self-assembling oligonucleotides carrying a unique DNA sequence for the identification of the corresponding chemical moiety. We have used ESAC library technology in a two-step selection procedure for the identification of novel inhibitors of stromelysin-1 (MMP-3), a matrix metalloproteinase involved in both physiological and pathological tissue remodeling processes, yielding novel inhibitors with micromolar potency.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Carbonic Anhydrase II / antagonists & inhibitors
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / pharmacology
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Carboxypeptidases A / antagonists & inhibitors
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Catalysis
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Chromatography, Affinity
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Cloning, Molecular
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DNA / genetics*
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Drug Design
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Gene Library
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Humans
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Matrix Metalloproteinase 3 / chemistry
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Matrix Metalloproteinase 3 / genetics*
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Matrix Metalloproteinase Inhibitors*
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Oligonucleotides / chemical synthesis
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Oligonucleotides / chemistry
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Protease Inhibitors / chemical synthesis*
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Protease Inhibitors / chemistry
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Protease Inhibitors / pharmacology*
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Protein Binding
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Reverse Transcriptase Polymerase Chain Reaction
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Spectrometry, Mass, Electrospray Ionization
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Urokinase-Type Plasminogen Activator / antagonists & inhibitors
Substances
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Carbonic Anhydrase Inhibitors
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Indicators and Reagents
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Matrix Metalloproteinase Inhibitors
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Oligonucleotides
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Protease Inhibitors
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DNA
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Carboxypeptidases A
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Urokinase-Type Plasminogen Activator
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Matrix Metalloproteinase 3
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Carbonic Anhydrase II