Artificial nucleobase-amino acid conjugates: a new class of TAR RNA binding agents
Autor: | Jean-Patrick Joly, Maria Duca, Patrick Eldin, Laurence Briant, Guillaume Mata, Rachid Benhida, Fabien Fontaine-Vive |
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Přispěvatelé: | Institut de Chimie de Nice (ICN), Institut de Chimie du CNRS (INC)-Centre National de la Recherche Scientifique (CNRS)-Université Côte d'Azur (UCA)-Université Nice Sophia Antipolis (... - 2019) (UNS), COMUE Université Côte d'Azur (2015-2019) (COMUE UCA)-COMUE Université Côte d'Azur (2015-2019) (COMUE UCA), Institut de Recherche en Infectiologie de Montpellier (IRIM), Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Centre National de la Recherche Scientifique (CNRS)-Université Nice Sophia Antipolis (... - 2019) (UNS), Université Côte d'Azur (UCA)-Université Côte d'Azur (UCA), Centre d’études d’Agents Pathogènes et Biotechologies pour la Santé (CPBS), Institut de Chimie Radicalaire (ICR), Aix Marseille Université (AMU)-Centre National de la Recherche Scientifique (CNRS), Departamento de Matematicas y Computacion (Department of Mathematics and Computer Science), Universidad de La Rioja (UR), Commissariat à l'énergie atomique et aux énergies alternatives - Laboratoire d'Electronique et de Technologie de l'Information (CEA-LETI), Université Grenoble Alpes (UGA)-Direction de Recherche Technologique (CEA) (DRT (CEA)), Commissariat à l'énergie atomique et aux énergies alternatives (CEA)-Commissariat à l'énergie atomique et aux énergies alternatives (CEA), Université Nice Sophia Antipolis (... - 2019) (UNS), Université Côte d'Azur (UCA)-Université Côte d'Azur (UCA)-Centre National de la Recherche Scientifique (CNRS) |
Jazyk: | angličtina |
Rok vydání: | 2014 |
Předmět: |
MESH: Amino Acids
Anti-HIV Agents Base pair RNA-dependent RNA polymerase HIV Infections MESH: Base Sequence Virus Replication Catalysis Cell Line MESH: HIV-1 MESH: Gene Products tat Transcription (biology) MESH: RNA Humans Amino Acids MESH: Anti-HIV Agents ComputingMilieux_MISCELLANEOUS MESH: Humans Base Sequence Chemistry Organic Chemistry MESH: Virus Replication Cooperative binding RNA Nuclease protection assay General Chemistry MESH: Purines MESH: HIV Infections Non-coding RNA 3. Good health MESH: Cell Line Pyrimidines Biochemistry Purines RNA editing MESH: Pyrimidines Gene Products tat [SDV.MP.VIR]Life Sciences [q-bio]/Microbiology and Parasitology/Virology [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology HIV-1 |
Zdroj: | Chemistry-A European Journal Chemistry-A European Journal, Wiley-VCH Verlag, 2014, 20 (7), pp.2071-9. ⟨10.1002/chem.201303664⟩ Chemistry-A European Journal, Wiley-VCH Verlag, 2014, 20 (7), pp.2071-2079. ⟨10.1002/chem.201303664⟩ |
ISSN: | 0947-6539 1521-3765 |
DOI: | 10.1002/chem.201303664⟩ |
Popis: | International audience; The human immunodeficiency virus type-1 (HIV-1) Tat protein stimulates transcriptional elongation. Tat is involved in the transcription machinery by binding to the transactivation response region (TAR) RNA stem-loop structure, which is encoded by the 5′ leader sequence found in all HIV-1 mRNAs. Herein, we report the rational design, synthesis, and in vitro evaluation of new RNA binding agents that were conceived in order to bind strongly and selectively to the stem-loop structure of TAR RNA and, thus, inhibit the Tat/TAR interaction. We have demonstrated that the conjugation of modified nucleobases, able to interact specifically with an RNA base pair, and various amino acids allows these motifs to bind the target RNA selectively and in a cooperative manner that leads to the inhibition of viral replication in HIV-infected cells. |
Databáze: | OpenAIRE |
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