Ahn, DR Yu, JH 2024-01-21T05:33:13Z 2024-01-21T05:33:13Z 2021-09-03 2005-02-15 0968-0896 https://pubs.kist.re.kr/handle/201004/136732 An approach is described to the design of neomycin-dipeptide conjugates as ligands for Rev responsive element (RRE) RNA, which effectively inhibit Rev-RRE interaction. A library of 256 neomycin-dipeptide conjugates was constructed on TentaGel beads using a split-and-pool combinatorial synthesis. Five conjugates were selected after screening the library with fluorescence linked RRE RNA, and they were identified after sequencing by MALDI-TOF mass spectrometer. The heteroconjugates bind to RRE RNA with moderately improved affinities and highly improved specificity, compared to neomycin as determined by means of fluorescence anisotropy and surface plasmon resonance (SPR) experiments. This strategy, synthesis of the neomycin-peptide heteroconjugate library and selection against RNA target, could provide an efficient way to develop inhibitors against pathogenic RNA. (C) 2004 Elsevier Ltd. All rights reserved. English PERGAMON-ELSEVIER SCIENCE LTD SPECIFICITY AMINOGLYCOSIDES INHIBITION POTENT Library construction of neomycin-dipeptide heteroconjugates and selection against RRE RNA Article 10.1016/j.bmc.2004.11.021 1 BIOORGANIC & MEDICINAL CHEMISTRY, v.13, no.4, pp.1177 - 1183 BIOORGANIC & MEDICINAL CHEMISTRY 13 4 1177 1183 scie scopus 000226967900025 2-s2.0-12844268189 Biochemistry & Molecular Biology Chemistry, Medicinal Chemistry, Organic Biochemistry & Molecular Biology Pharmacology & Pharmacy Chemistry Article SPECIFICITY AMINOGLYCOSIDES INHIBITION POTENT RNA target aminoglycoside-dipeptide heteroconjugate RRE