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

Awahara, Chiyuki; Oku, Daiki; Kobayashi, Kazuya; Hattori, Yasunao

Awahara, Chiyuki; Oku, Daiki; Kobayashi, Kazuya; Hattori, Yasunao.

Afiliación

Awahara C; Department of Medicinal Chemistry, Kyoto Pharmaceutical University.
Oku D; Department of Medicinal Chemistry, Kyoto Pharmaceutical University.
Kobayashi K; Department of Medicinal Chemistry, Kyoto Pharmaceutical University.
Hattori Y; Center for Instrumental Analysis, Kyoto Pharmaceutical University.

Chem Pharm Bull (Tokyo) ; 72(3): 309-310, 2024.

Article en En | MEDLINE | ID: mdl-38479891

ABSTRACT

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.

Asunto(s)

Ácido Aspártico Endopeptidasas; Virus Linfotrópico T Tipo 1 Humano; Humanos; Secuencia de Aminoácidos; Ácido Aspártico Endopeptidasas/química; Ácido Aspártico Endopeptidasas/metabolismo; Virus Linfotrópico T Tipo 1 Humano/metabolismo; Dipéptidos; Inhibidores de Proteasas/farmacología

Palabras clave

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

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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Virus Linfotrópico T Tipo 1 Humano / Ácido Aspártico Endopeptidasas Límite: Humans Idioma: En Revista: Chem Pharm Bull (Tokyo) Año: 2024 Tipo del documento: Article Pais de publicación: Japón

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