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

Chiyuki Awahara; Daiki Oku; Kazuya Kobayashi; Yasunao Hattori

doi:10.1248/cpb.c23-00879

Note

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

Chiyuki Awahara, Daiki Oku, Kazuya Kobayashi, Yasunao Hattori

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

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Supplementary material

2024 Volume 72 Issue 3 Pages 309-310

DOI https://doi.org/10.1248/cpb.c23-00879

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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.

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