Chemically programmed antibodies as HIV-1 attachment Inhibitors

Shinichi Sato, Tsubasa Inokuma, Nobumasa Otsubo, Dennis R. Burton, Carlos F. Barbas

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)


Herein, we describe the design and application of two small-molecule anti-HIV compounds for the creation of chemically programmed antibodies. N-Acyl-β-lactam derivatives of two previously described molecules BMS-378806 and BMS-488043 that inhibit the interaction between HIV-1 gp120 and T-cells were synthesized and used to program the binding activity of aldolase antibody 38C2. Discovery of a successful linkage site to BMS-488043 allowed for the synthesis of chemically programmed antibodies with affinity for HIV-1 gp120 and potent HIV-1 neutralization activity. Derivation of a successful conjugation strategy for this family of HIV-1 entry inhibitors enables its application in chemically programmed antibodies and vaccines and may facilitate the development of novel bispecific antibodies and topical microbicides.

Original languageEnglish
Pages (from-to)460-465
Number of pages6
JournalACS Medicinal Chemistry Letters
Issue number5
Publication statusPublished - 2013 May 9
Externally publishedYes


  • Bioconjugation
  • anti-HIV agent
  • chemically programmed antibody
  • entry inhibitor
  • microbicide

ASJC Scopus subject areas

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry


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