title: Optimization of a Class of Tryptophan Dendrimers That Inhibit HIV Replication Leads to a Selective, Specific, and Low-Nanomolar Inhibitor of Clinical Isolates of Enterovirus A71.
abstract: Tryptophan dendrimers that inhibit HIV replication by binding to the HIV envelope glycoproteins gp120 and gp41 have unexpectedly also proven to be potent, specific, and selective inhibitors of the replication of the unrelated enterovirus A71. Dendrimer 12, a consensus compound that was synthesized on the basis of the structure-activity relationship analysis of this series, is 3-fold more potent against the BrCr lab strain and, surprisingly, inhibits a large panel of clinical isolates in the low-nanomolar/high-picomolar range.
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain Instituto de Tecnología Química (UPV-CSIC), Valencia, Spain.
authors.forename: Eva
authors.initials: E
authors.lastname: Rivero-Buceta
authors.affiliation: KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
authors.forename: Liang
authors.initials: L
authors.lastname: Sun
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain.
authors.forename: Belén
authors.initials: B
authors.lastname: Martínez-Gualda
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain Centro de Química Orgánica Manuel Lora Tamayo, Madrid, Spain.
authors.forename: Elisa G
authors.initials: EG
authors.lastname: Doyagüez
authors.affiliation: KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
authors.forename: Kim
authors.initials: K
authors.lastname: Donckers
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain.
authors.forename: Ernesto
authors.initials: E
authors.lastname: Quesada
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain.
authors.forename: María-José
authors.initials: MJ
authors.lastname: Camarasa
authors.affiliation: KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
authors.forename: Leen
authors.initials: L
authors.lastname: Delang
authors.affiliation: Instituto de Química Médica (CSIC), Madrid, Spain anarosa@iqm.csic.es johan.neyts@kuleuven.be.
authors.forename: Ana
authors.initials: A
authors.lastname: San-Félix
authors.affiliation: KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium anarosa@iqm.csic.es johan.neyts@kuleuven.be.
authors.forename: Johan
authors.initials: J
authors.lastname: Neyts
authors.affiliation: KU Leuven-University of Leuven, Department of Microbiology and Immunology, Rega Institute for Medical Research, Laboratory of Virology and Chemotherapy, Leuven, Belgium.
authors.forename: Pieter
authors.initials: P
authors.lastname: Leyssen
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D004770:Enterovirus / Q000187:drug effects*; D015699:HIV Envelope Protein gp120 / Q000235:genetics / Q000378:metabolism; D015700:HIV Envelope Protein gp41 / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects*
chemical_list: D019380:Anti-HIV Agents; D015699:HIV Envelope Protein gp120; D015700:HIV Envelope Protein gp41