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Application of porcupine inhibitors in stem cell fate determination.
Chemical Biology & Drug Design ( IF 3 ) Pub Date : 2020-05-17 , DOI: 10.1111/cbdd.13704
Ashkan Kalantary-Charvadeh 1, 2, 3 , Vahid Hosseini 2 , Amir Mehdizadeh 4 , Masoud Darabi 1, 2
Affiliation  

Porcupine (Porcn), a membrane‐bound O ‐acyltransferase, is an endoplasmic reticulum‐located protein that has catalytic activity. Porcn is involved in post‐translational lipid modification of wingless‐Int (Wnt) proteins and serves as an indispensable step in the Wnt proper secretion and signaling. Small‐molecule inhibitors targeting Porcn catalytic function in vitro and in vivo are of great interest not only for treating cancer and fibrotic disorders but also in the field of regenerative medicine. Although a number of studies have been conducted, the exact role of Porcn in stem cell fate is not entirely clear. In some cases, Porcn inhibition declined differentiation rate, and in others, it induced stem cell differentiation toward specific lineages. In this review, we first elaborated the Porcn catalytic activity and its inhibitors. Then, we discussed about the recently reported results of Porcn inhibitors in stem cells self‐renewal and differentiation.

中文翻译:

豪猪抑制剂在干细胞命运测定中的应用。

豪猪(Porcn),膜结合的O酰基转移酶是一种内质网定位蛋白,具有催化活性。Porcn参与了无翅Int(Wnt)蛋白的翻译后脂质修饰,是Wnt正确分泌和信号传导中不可或缺的步骤。在体外和体内,靶向Porcn催化功能的小分子抑制剂不仅在治疗癌症和纤维变性疾病中,而且在再生医学领域都引起了极大的兴趣。尽管已进行了大量研究,但Porcn在干细胞命运中的确切作用尚不完全清楚。在某些情况下,Porcn抑制作用会降低分化速率,而在其他情况下,它会诱导干细胞向特定谱系分化。在这篇综述中,我们首先阐述了Porcn的催化活性及其抑制剂。然后,
更新日期:2020-06-23
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