Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor

Chem Pharm Bull (Tokyo). 2024;72(3):309-310. doi: 10.1248/cpb.c23-00879.

Abstract

The inhibition mode of a retro-inverso (RI) inhibitor containing a hydroxyethylamine dipeptide isostere against the human T-cell leukemia virus type-1 (HTLV-1) protease was examined. Enzymatic evaluation of the RI-modified inhibitor containing a D-allo-Ile residue revealed that HTLV-1 was competitively inhibited. IC50 values of the RI-modified inhibitor and pepstatin A, a standard inhibitor of aspartic proteases, were nearly equivalent.

Keywords: competitive inhibitor; human T-cell leukemia virus type-1 protease; retro-inverso conversion.

MeSH terms

  • Amino Acid Sequence
  • Aspartic Acid Endopeptidases* / chemistry
  • Aspartic Acid Endopeptidases* / metabolism
  • Dipeptides
  • Human T-lymphotropic virus 1* / metabolism
  • Humans
  • Protease Inhibitors / pharmacology

Substances

  • HTLV-1 protease
  • Aspartic Acid Endopeptidases
  • Dipeptides
  • Protease Inhibitors