Atg
The Atg proteins involved in autophagosome formation consist of several functional units: Atg1 kinase and its regulators, the PI3K complex, Atg9, the Atg2-Atg18 complex, and two ubiquitin-like conjugation systems.Mammals contain counterparts for most yeast Atg proteins as well as some additional factors that are specific to higher eukaryotes. During canonical autophagy, Atg1 associates with Atg13, Atg17, Atg29 and Atg31. In contrast, during the Cvt pathway, Atg1 interacts with Atg11, Atg13, Atg20, Atg24 and Vac8. the mTORC1-dependent regulation of the ULK1–ATG13–FIP200–ATG101 complex has been deciphered. Under nutrient-rich conditions, mTORC1 associates with the ULK1–ATG13–FIP200–ATG101 complex and phosphorylates ULK1 and ATG13. Under starvation conditions or upon treatment with mTOR inhibitors, mTORC1 dissociates from this mega-complex, and the inhibitory mTOR-dependent phospho-sites within ULK1 and ATG13 become dephosphorylated. Active ULK1 then autophosphorylates and phosphorylates ATG13 and FIP200, ultimately leading to the initiation of autophagosome formation.The phospho-status of the ULK1–ATG13–FIP200–ATG101 complex is central for the regulation of autophagic processes. In general, global phosphorylation of ULK1 and ATG13 is decreased under starvation conditions and FIP200 phosphorylation is decreased under fed conditions.
References
1.Mizushima N,et al. Annu Rev Cell Dev Biol. 2011;27:107-32. 2.Sebastian Wesselborg,et al. Cell Mol Life Sci. 2015; 72: 4721–4757.
References
1.Mizushima N,et al. Annu Rev Cell Dev Biol. 2011;27:107-32. 2.Sebastian Wesselborg,et al. Cell Mol Life Sci. 2015; 72: 4721–4757.
Autophagy
Atg
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LV-320
产品货号 : M16930
cas no: ——
LV-320 (LV320) 是一种新型强效、细胞活性、自噬相关半胱氨酸蛋白酶 ATG4B 的变构抑制剂,在 ATG4B 裂解试验中 IC50 为 24.5 uM。 -
NSC 185058
产品货号 : M14346
cas no: 39122-38-8
NSC 185058 (NSC185058, NSC-185058, 2-Pyridinecarbothioamide) 是一种新型 ATG4B 拮抗剂,可抑制自噬,IC50 为 50 uM,对 mTOR 和 PI3K 活性没有影响。 -
NSC 377071
产品货号 : M13794
cas no: 26097-80-3
NSC 377071 (NSC-377071, NSC377071, Cambendodium) 是一种新型 ATG4B 拮抗剂,可抑制自噬,对 mTOR 和 PI3K 活性没有影响;直接抑制饥饿或雷帕霉素诱导的细胞 ATG4B 活性,并抑制饥饿反应中 LC3B 的脂化和自噬体形成,抑制 Saos-2 骨肉瘤体内生长。 -
FMK-9a
产品货号 : M13062
cas no: 1955550-51-2
FMK-9a (FMK9a) 是一种有效的、选择性的、ATG4B (Autophagin-1) 共价拟肽抑制剂,TR-FRET 测定中的 IC50 为 80 nM;对天冬氨酸蛋白酶、丝氨酸蛋白酶、金属蛋白酶和 20S 蛋白酶体没有活性,抑制组织蛋白酶 B 和钙蛋白酶,IC50 为亚微摩尔 (0.1-0.2 uM);与 Cys74 共价结合并灭活 ATG4B 蛋白水解活性,在细胞 LRA 测定中的 IC50 为 15 nM。 -
S130
产品货号 : M10558
cas no: 1160852-22-1
S130(ATG4B抑制剂S130)是一种有效的、特异性的ATG4B抑制剂,IC50为3.24 uM,具有很强的亲和力(Kd=4 uM)并特异性抑制ATG4B的活性。