Abstract:
Wingless-related integration site (Wnt) signaling is one of the main oncogenic pathways in different malignancies. Therefore, targeting this pathway has been considered an exciting strategy in cancer treatment. Porcn is among the central enzymes in this pathway that has recently been considered for cancer-targeted therapy. As a membrane-bound O-acyltransferase, Porcn plays a critical role in wnt ligand palmitoylation and its subsequent secretion. In addition to Porcn\'s role in stem cell signaling and differentiation, recent findings have shown its role in developing and progressing colorectal, pancreatic, liver, head, and neck cancers. Developed small molecule inhibitors have also opened a promising window toward cancer treatment strategies. In this review, the structure and biological role of Porcn in different cancer-related signaling pathways and inhibitors used for inhibiting this enzyme are discussed.
摘要:
无翼相关整合位点(Wnt)信号是不同恶性肿瘤的主要致癌途径之一。因此,靶向这一途径被认为是癌症治疗中令人兴奋的策略.Porcn是该途径中的中心酶之一,最近被认为用于癌症靶向治疗。作为膜结合的O-酰基转移酶,Porcn在wnt配体棕榈酰化及其随后的分泌中起关键作用。除了Porcn在干细胞信号转导和分化中的作用,最近的研究结果表明它在结直肠的发展和进展中的作用,胰腺,肝脏,头部,和颈部癌症。开发的小分子抑制剂也为癌症治疗策略打开了一个有希望的窗口。在这次审查中,讨论了Porcn在不同癌症相关信号通路中的结构和生物学作用以及用于抑制该酶的抑制剂。