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Frizzled receptors(FZDs)in Wnt signaling:potential therapeutic targets for human cancers

摘要Frizzled receptors(FZDs)are key contributors intrinsic to the Wnt signaling pathway,activation of FZDs triggering the Wnt signaling cascade is frequently observed in human tumors and intimately associated with an aggressive carcinoma phenotype.It has been shown that the abnormal expression of FZD receptors contributes to the manifestation of malignant characteristics in human tumors such as enhanced cell proliferation,metastasis,chemotherapy resistance as well as the acquisition of cancer stemness.Given the essential roles of FZD receptors in the Wnt signaling in human tumors,this review aims to consolidate the prevailing knowledge on the specific status of FZD receptors(FZD1-10)and elucidate their respective functions in tumor progression.Furthermore,we delineate the structural basis for binding of FZD and its co-receptors to Wnt,and provide a better theoretical foundation for subsequent studies on related mechanisms.Finally,we describe the existing biological classes of small molecule-based FZD inhibitors in detail in the hope that they can provide useful assistance for design and development of novel drug candidates targeted FZDs.

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作者 Hui-yu Liu [1] Xiao-jiao Sun [2] Si-yu Xiu [2] Xiang-yu Zhang [2] Zhi-qi Wang [2] Yan-lun Gu [3] Chu-xiao Yi [2] Jun-yan Liu [1] Yu-song Dai [1] Xia Yuan [2] Hua-peng Liao [4] Zhen-ming Liu [2] Xiao-cong Pang [3] Tian-cheng Li [5] 学术成果认领
作者单位 Department of Otorhinolaryngology Head and Neck Surgery,Peking University First Hospital,Beijing 100034,China [1] State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University,Beijing 100191,China [2] Department of Pharmacy,Peking University First Hospital,Beijing 100034,China [3] Yizhang County People's Hospital,Chenzhou 424200,China [4] Department of Otorhinolaryngology Head and Neck Surgery,Peking University First Hospital,Beijing 100034,China;Department of Otorhinolaryngology Head and Neck Surgery,Beijing Chaoyang Hospital,Capital Medical University,Beijing 100034,China [5]
栏目名称 Review Article
DOI 10.1038/s41401-024-01270-3
发布时间 2024-08-22
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中国药理学报(英文版)

中国药理学报(英文版)

2024年45卷8期

1556-1570页

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