评估 HTLV-1 蛋白酶的反式-反式抑制剂作为竞争性抑制剂。
Evaluating a Retro-Inverso Type Inhibitor of HTLV-1 Protease as a Competitive Inhibitor.
机构信息
Department of Medicinal Chemistry, Kyoto Pharmaceutical University.
Center for Instrumental Analysis, Kyoto Pharmaceutical University.
出版信息
Chem Pharm Bull (Tokyo). 2024;72(3):309-310. doi: 10.1248/cpb.c23-00879.
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. IC values of the RI-modified inhibitor and pepstatin A, a standard inhibitor of aspartic proteases, were nearly equivalent.
研究了一种含有羟乙基胺二肽等排体的反式-反式（RI）抑制剂对人 T 细胞白血病病毒 1 型（HTLV-1）蛋白酶的抑制模式。对含有 D-allo-Ile 残基的 RI 修饰抑制剂的酶促评估表明，HTLV-1 受到竞争性抑制。RI 修饰抑制剂和 pepstatin A（天冬氨酸蛋白酶的标准抑制剂）的 IC 值几乎相当。
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