title: Dual-pharmacophore DNA-encoded chemical libraries.
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.
authors.affiliation: ETH Zurich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, 8093 Zurich, Switzerland. Electronic address: joerg.scheuermann@pharma.ethz.ch.
authors.forename: Jörg
authors.initials: J
authors.lastname: Scheuermann
authors.affiliation: ETH Zurich, Department of Chemistry and Applied Biosciences, Institute of Pharmaceutical Sciences, 8093 Zurich, Switzerland. Electronic address: dario.neri@pharma.ethz.ch.
authors.forename: Dario
authors.initials: D
authors.lastname: Neri
mesh_terms: D000086:Acetazolamide / Q000138:chemical synthesis / Q000494:pharmacology; D000951:Antigens, Neoplasm / Q000737:chemistry* / Q000378:metabolism; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000071231:Carbonic Anhydrase IX; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D002256:Carbonic Anhydrases / Q000737:chemistry* / Q000378:metabolism; D002292:Carcinoma, Renal Cell / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D020650:Combinatorial Chemistry Techniques; D004247:DNA / Q000737:chemistry* / Q000378:metabolism; D055808:Drug Discovery; D005456:Fluorescent Dyes / Q000737:chemistry; D015870:Gene Expression; D015723:Gene Library; D006801:Humans; D007680:Kidney Neoplasms / Q000188:drug therapy / Q000201:enzymology / Q000473:pathology; D054852:Small Molecule Libraries / Q000138:chemical synthesis / Q000737:chemistry*
chemical_list: D000951:Antigens, Neoplasm; D000970:Antineoplastic Agents; D002257:Carbonic Anhydrase Inhibitors; D005456:Fluorescent Dyes; D054852:Small Molecule Libraries; D004247:DNA; C089226:CA9 protein, human; D000071231:Carbonic Anhydrase IX; D002256:Carbonic Anhydrases; D000086:Acetazolamide