Abstract
In contrast to single-pharmacophore DNA-encoded libraries, where only one chemical moiety is linked to DNA, dual-pharmacophore DNA-encoded chemical libraries feature the display of two independent small-molecules in close proximity. This, in principle, allows to explore adjacent epitopes on a pharmaceutical target of choice and hence the discovery of simultaneously binding pairs of fragments, by virtue of the chelate effect.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Acetazolamide / chemical synthesis
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Acetazolamide / pharmacology
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Antigens, Neoplasm / chemistry*
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Antigens, Neoplasm / metabolism
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Carbonic Anhydrase IX
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Carbonic Anhydrase Inhibitors / chemical synthesis
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Carbonic Anhydrase Inhibitors / pharmacology
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Carbonic Anhydrases / chemistry*
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Carbonic Anhydrases / metabolism
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Carcinoma, Renal Cell / drug therapy
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Carcinoma, Renal Cell / enzymology
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Carcinoma, Renal Cell / pathology
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Combinatorial Chemistry Techniques
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DNA / chemistry*
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DNA / metabolism
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Drug Discovery
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Fluorescent Dyes / chemistry
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Gene Expression
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Gene Library*
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Humans
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Kidney Neoplasms / drug therapy
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Kidney Neoplasms / enzymology
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Kidney Neoplasms / pathology
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Small Molecule Libraries / chemical synthesis
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Small Molecule Libraries / chemistry*
Substances
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Antigens, Neoplasm
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Antineoplastic Agents
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Carbonic Anhydrase Inhibitors
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Fluorescent Dyes
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Small Molecule Libraries
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DNA
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CA9 protein, human
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Carbonic Anhydrase IX
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Carbonic Anhydrases
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Acetazolamide