肽基 O-酰基异羟肟酸酯：组织蛋白酶 B 的强效新型失活剂。
Peptidyl O-acyl hydroxamates: potent new inactivators of cathepsin B.
作者信息
Smith R A, Coles P J, Spencer R W, Copp L J, Jones C S, Krantz A
机构信息
Syntex Research, Mississauga, Ontario, Canada.
出版信息
Biochem Biophys Res Commun. 1988 Sep 30;155(3):1201-6. doi: 10.1016/s0006-291x(88)81267-1.
Peptidyl O-acyl hydroxamates having appropriate active-site recognition features are very potent time-dependent inhibitors of the cysteine proteinase cathepsin B. The inhibition is irreversible, and the inactivation rate is strongly dependent on peptide structure and correct positioning of the P1 amino acid carbonyl group. Lipophilic O-acyl groups provide the most rapid inactivators, as exemplified by the inhibitor O-mesitoyl N-benzyloxycarbonyl-L-phenylalanyl-L-alanine hydroxamate (kmax/Ki = 640,000 M-1s-1).
具有适当活性位点识别特征的肽基O-酰基异羟肟酸酯是半胱氨酸蛋白酶组织蛋白酶B非常有效的时间依赖性抑制剂。这种抑制是不可逆的，失活速率强烈依赖于肽结构和P1氨基酸羰基的正确定位。亲脂性O-酰基提供了最快的失活剂，例如抑制剂O-均三甲苯甲酰基-N-苄氧羰基-L-苯丙氨酰-L-丙氨酸异羟肟酸酯（kmax/Ki = 640,000 M-1s-1）。
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