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Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc

Academic Article
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Overview

authors

  • Asano, S.
  • Gavrilyuk, J.
  • Burton, Dennis
  • Barbas III, Carlos

publication date

  • February 2014

journal

  • ACS Medicinal Chemistry Letters  Journal

abstract

  • CCR5 antagonists are among the most advanced approaches in HIV therapy and may also be relevant to treatment of graft-versus-host disease and Staphylococcus aureus infection. To expand the potential of the only approved CCR5 antagonist, Maraviroc, we studied derivatives that would enable functional linkage of Maraviroc to long-lived carriers. Through targeted synthesis, we discovered an effective linkage site on Maraviroc and demonstrate the potential of these derivatives to prepare potent chemically programmed antibodies and PEGylated derivatives. The resulting compounds effectively neutralized a variety of HIV-1 isolates. Both chemically programmed antibody and PEGylation approaches extend the neutralization activity of serum circulating Maraviroc. Derivation of a successful conjugation strategy for Maraviroc should further enable its use in chemically programmed vaccines, novel bispecific antibodies, and topical microbicides.
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Research

keywords

  • CCR5 antagonist
  • Maraviroc
  • PEGylation
  • chemically programmed antibody
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Identity

PubMed Central ID

  • PMC3927940

International Standard Serial Number (ISSN)

  • 1948-5875 (Print) 1948-5875 (Linking)

Digital Object Identifier (DOI)

  • 10.1021/ml400370w

PubMed ID

  • 24563723
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Additional Document Info

start page

  • 133

end page

  • 137

volume

  • 5

issue

  • 2

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