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

by | Mar 14, 2024 | Publications

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.

PMID:38479891 | DOI:10.1248/cpb.c23-00879

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