Cysteine proteases play multiple roles in basically all aspects of physiology and development. Furthermore, they are engaged in signalling pathways and in the response to biotic and abiotic stresses[3]. Aloxistatin is a specific and potent inhibitor of cysteine proteinases isolated from a culture of Aspergillus japonicus[3]. Aloxistatin at a series of concentrations was able to enter the intact platelet and inhibit the protease activity in lysed platelets when incubated for 5 min[4]. After a brief preincubation with the membrane-permeable, Aloxistatin (10 mg/ml) blunted PTH-induced (parathyroid hormone) cell proliferation in sub-confluent cultures and also attenuated proliferation and inhibited differentiation in longer-term confluent cultures[5]. Aloxistatin(100 mg/kg, p.o.) inhibited the activity of cathepsin B&L in skeletal muscle, heart, and liver of hamsters[6].
作用机制
Aloxistatin reacts irreversibly with the thiol group at the active site.
E-64d/阿洛司他丁 细胞实验
Cell Line
Concentration
Treated Time
Description
References
SH-SY5Y cells
10 µM
2 weeks
To study the inhibitory effect of E-64d on autophagy
Cell Death Dis. 2012 May 24;3(5):e312.
WT or patient fibroblast cells
10 μM
30 min
To evaluate the effect of E-64d on lysosomal function in fibroblasts. Results showed that pretreatment with E-64d significantly reduced the activity of lysosomes labeled with BMV109.
JCI Insight. 2022 Jul 8;7(13):e158457.
293T cells
10 μM
2 h
In CD9KO cells, E-64d significantly reduced MERS pseudovirus entry, indicating the necessity of CD9 in TTSP-mediated early virus entry.
PLoS Pathog. 2017 Jul 31;13(7):e1006546.
Huh-7 cells
6 mM
6 h
Used to measure autophagic degradation capability, results showed that lysosomal proteolytic activity was markedly reduced in the absence of VTRNA1-1.
Autophagy. 2022 Jan;18(1):191-203.
Hepa1-6 cells
10 µM
15 min
To determine the proportion of intracellular sporozoites that had productively invaded the cells, rather than those in the process of migrating.
J Exp Med. 2011 Feb 14;208(2):341-56.
Huh7 cells
0.14, 0.42, 1.23, 3.7, 11.1, and 33.3 μM
24 h
E-64d significantly inhibited SARS-CoV-2 pseudovirus infection with low cytotoxicity.
Signal Transduct Target Ther. 2021 Mar 27;6(1):134.
Arabidopsis protoplasts
20 µM
12 h
E-64d inhibited the degradation of FBA8, indicating its role in autophagy-associated vacuolar degradation
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