生物来源
human liver
质量水平
形式
solution
比活
≥0.5 units/mg protein
技术
activity assay: suitable
pH值范围
4.5—5.5
UniProt登记号
应用
pharmaceutical
运输
dry ice
储存温度
−20°C
基因信息
human ... CTSL1(1514)
一般描述
组织蛋白酶 L（CTSL）基因定位于人类染色体 9q21.33。它编码一种属于肽酶 C1 家族的溶酶体半胱氨酸蛋白酶。该酶是由二硫键连接的重链（175 个氨基酸）和轻链（42 个氨基酸）的一个二聚体。
应用
来自人类肝脏的组织蛋白酶 L（CTSL）已用于：
- 体外消化突变转化生长因子β-诱导的（TGFBIp）和 LC3（自噬体标记）蛋白
- 消化黑色素体前蛋白（Pmel17）重复结构域（RPT）异构体的 pH 依赖性原纤维，并通过色氨酸荧光研究 pH 对 sRPT 聚集动力学的影响
- 在无细胞系统中分析小分子或药物对 CTSL 的抑制作用
生化/生理作用
组织蛋白酶 L（CTSL）表现出内肽酶活性，并破坏与芳香残基的肽键。该酶在 pH 3.0–6.5 下与硫醇化合物一起发挥作用。弹性蛋白、胶原蛋白和 α-1 蛋白酶抑制剂作为组织蛋白酶 L（CTSL）的底物。CTSL 切割多种蛋白质，包括酶、受体和转录因子。它参与抗原肽的产生并控制 B 细胞的稳态。它与肌原纤维坏死和肿瘤进展有关。CTSL 表达增加促进肿瘤转移，与肿瘤患者预后不良有关。在癌症中观察到 CTSL 的表达增加。CTSL 与多形性胶质母细胞瘤（GBM）、中东呼吸综合征（MERS）、牙龈过度生长和严重急性呼吸综合征冠状病毒 2 型（SARS-CoV-2）有关。它在多种生理蛋白质底物的降解中具有比组织蛋白酶 B 和 H 更高的比活性。
单位定义
一个酶活性单位将在pH 5.5、25℃下，每分钟水解1.0 μmole的Z-Phe-Arg-AFC。
外形
溶于20mM丙二酸溶液，pH 5.5，含有1 mM EDTA和400 mM NaCl。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
常规特殊物品
Gustavo E Chavarria et al.
European journal of medicinal chemistry, 58, 568-572 (2012-11-22)
Kinetic analysis of the mode of inhibition of cathepsin L by KGP94, a lead compound from a privileged library of functionalized benzophenone thiosemicarbazone derivatives, demonstrated that it is a time-dependent, reversible, and competitive inhibitor of the enzyme. These results are
M Kathryn Liszewski et al.
Immunity, 39(6), 1143-1157 (2013-12-10)
Complement is viewed as a critical serum-operative component of innate immunity, with processing of its key component, C3, into activation fragments C3a and C3b confined to the extracellular space. We report here that C3 activation also occurred intracellularly. We found
Dexter N Dean et al.
Biochimica et biophysica acta. Proteins and proteomics, 1867(10), 961-969 (2019-02-05)
The pre-melanosomal protein (Pmel17) aggregates within melanosomes to form functional amyloid fibrils that facilitate melanin polymerization. The repeat domain (RPT) of Pmel17 fibrillates under strict acidic melanosomal pH. Alternative splicing results in a shortened repeat domain (sRPT), which also forms
Bailey Miller et al.
Journal of natural products, 77(1), 92-99 (2013-12-25)
A number of marine natural products are potent inhibitors of proteases, an important drug target class in human diseases. Hence, marine cyanobacterial extracts were assessed for inhibitory activity to human cathepsin L. Herein, we have shown that gallinamide A potently
Stefan Tholen et al.
Cellular and molecular life sciences : CMLS, 71(5), 899-916 (2013-07-03)
Endolysosomal cysteine cathepsins functionally cooperate. Cathepsin B (Ctsb) and L (Ctsl) double-knockout mice die 4 weeks after birth accompanied by (autophago-) lysosomal accumulations within neurons. Such accumulations are also observed in mouse embryonic fibroblasts (MEFs) deficient for Ctsb and Ctsl.
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