摘要
ROR蛋白家族包含受体酪氨酸激酶ROR1和ROR2,作为Wnt受体,它们对于非经典Wnt信号通路至关重要,并与癌细胞增殖存活、侵袭转移和治疗抵抗密切相关。ROR蛋白在大多数成人健康组织中几乎不表达,但在一些癌症中却有较高的表达水平。有趣的是,两种ROR蛋白可能在肿瘤中发挥不同的作用,ROR1主要促进肿瘤发生,而ROR2在不同类型的肿瘤中促进或抑制肿瘤进展。目前这两种受体作为潜在的治疗靶点已经引起了人们的兴趣,该文总结了ROR蛋白的结构学特征及其在不同组织中的表达情况。此外,该文还回顾了ROR蛋白调控的生物学过程和信号通路,解释了其在癌症中发挥的重要作用。最后汇总了目前处于临床试验阶段的靶向ROR蛋白的生物药包括单抗、双抗、抗体偶联药物等。
The ROR family contains ROR1 and ROR2,which are Wnt receptors that are critical for nonclassical Wnt signaling pathways and are associated with cancer cell proliferation,survival,invasion,metastasis,and treatment resistance.RORs are less expressed in healthy adult tissues,but are overexpressed in several type of cancers.Interestingly,the two RORs may play different roles in tumors,with ROR1 always promoting tumorigenesis and ROR2 promoting or inhibiting tumor progression in different tumor types.This review summarizes the structural characteristics of RORs and its expression in different tissues.In addition,it reviews the biological processes and signaling pathways regulated by RORs to explain its important role in cancer.Finally,the biological drugs of targeting RORs in clinical trials of cancer therapies were summarized,including monoclonal antibodies,bispecific antibody and antibody-drug conjugate,etc.
作者
赵鑫
丁琳
陈煜选
胡庆华
ZHAO Xin;DING Lin;CHEN Yu-Syuan;HU Qinghua(School of Pharmacy,China Pharmaceutical University,Nanjing 211198,China;Shanghai Henlius Biotech,Inc.,Shanghai Innovation Center,Shanghai 200233,China)
出处
《中国细胞生物学学报》
CAS
CSCD
2022年第12期2354-2365,共12页
Chinese Journal of Cell Biology
关键词
受体酪氨酸激酶样孤儿受体
癌症
抗体
肿瘤靶向治疗
receptor tyrosine kinase-like orphan receptors
cancer
antibody
targeted cancer therapy