是HT4细胞中多催化蛋白酶复合物（MPC； 20S蛋白酶体）的胰凝乳蛋白酶样活性抑制剂。
编号：172582
CAS号：158442-41-2
单字母：Z-I-E(OtBu)-AL-CHO
| 编号: | 172582 |
| 中文名称: | PSI | Proteasome Inhibitor 1、Z-Ile-Glu(O-t-butyl)-Ala-Leucinal |
| 英文名: | PSI | Proteasome Inhibitor 1、Z-Ile-Glu(O-t-butyl)-Ala-Leucinal |
| 英文同义词: | PSI peptide |
| CAS号: | 158442-41-2 |
| 单字母: | Z-I-E(OtBu)-AL-CHO |
| 三字母: | Cbz N端Cbz保护 -Ile异亮氨酸 -Glu(OtBu)侧链OtBu保护的谷氨酸 -Ala丙氨酸 -Leu亮氨酸 -CHOC端醛基化 |
| 氨基酸个数: | 4 |
| 分子式: | C32H50O8N4 |
| 平均分子量: | 618.76 |
| 精确分子量: | 618.36 |
| 等电点(PI): | - |
| pH=7.0时的净电荷数: | - |
| 平均亲水性: | -1.3666666666667 |
| 疏水性值: | 3.37 |
| 消光系数: | - |
| 来源: | 人工化学合成，仅限科学研究使用，不得用于人体。 |
| 盐体系: | 可选TFA、HAc、HCl或其它 |
| 储存条件: | 负80℃至负20℃ |
| 标签: | 醛肽 CBZ修饰肽 侧链保护基肽 |
Z-IE（OtBu）AL-CHO是HT4细胞中多催化蛋白酶复合物（MPC；20S蛋白酶体）的糜蛋白酶样活性的抑制剂。这是迄今为止报道的第一种可以导致神经元细胞中泛素化蛋白积累的抑制剂。此外，该化合物诱导小鼠白血病L1210细胞大量凋亡。因此，蛋白酶体抑制剂可能被认为是潜在的抗肿瘤药物。
Z-IE(OtBu)AL-CHO is an inhibitor of chymotrypsin-like activity of the multicatalytic proteinase complex (MPC; 20S proteasome) in HT4 cells. It is the first inhibitor reported so far which can cause accumulation of ubiquitinylated proteins in neuronal cells. Furthermore, this compound induced massive apoptosis in murine leukaemia L1210 cells. Therefore, proteasome inhibitors may be considered as potential anti-neoplastic agents.
PSI是一种阻断蛋白酶体作用的药物，蛋白酶体是降解不需要和受损蛋白质的蛋白质复合物。它在体外引起多巴胺能细胞死亡，并通过抑制IκB-α降解来阻止NF-κB对TNF-α和冈田酸的激活。
PSI is a drug that blocks the action of proteasomes, protein complexes that degrade unneeded and damaged proteins. It causes dopaminergic cell death in vitro and prevents activation of NF-κB in response to TNF-α and okadaic acid by inhibiting IκB-α degradation.
| DOI | 名称 | |
|---|---|---|
| 10.1128/AAC.46.6.2038-2040.2002 | Antitrypanosomal activities of proteasome inhibitors | 下载 |
| 10.1113/jphysiol.2002.018689 | Molecular adaptations of neuromuscular disease-associated proteins in response to eccentric exercise in human skeletal muscle | 下载 |
| 10.1016/s0014-5793(02)03874-7 | Ubiquitin binding proteins protect ubiquitin conjugates from disassembly | 下载 |
| 10.1023/a:1026470027387 | Apoptosis induced in L1210 leukaemia cells by an inhibitor of the chymotrypsin-like activity of the proteasome | 下载 |
| 10.1016/j.brainres.2007.07.072 | Effects of systemic PSI administration on catecholaminergic cells in the brain, adrenal medulla and carotid body in Wistar rats | 下载 |
| 10.1182/blood-2008-07-171389 | Green tea polyphenols block the anticancer effects of bortezomib and other boronic acid-based proteasome inhibitors | 下载 |
| 10.1046/j.1471-4159.1994.63041578.x | A new inhibitor of the chymotrypsin-like activity of the multicatalytic proteinase complex (20S proteasome) induces accumulation of ubiquitin-protein conjugates in a neuronal cell | 下载 |
