摘要
Polo样激酶1(PLK1)作为polo样激酶家族的重要成员,对细胞有丝分裂具有重要调控作用,其过度表达与多种肿瘤密切相关。PLK1-PBD结构域可在有丝分裂的不同时期定位于不同的细胞结构,发挥相应的作用,可通过调控PLK1激酶的定位,导致有丝分裂紊乱,最终促进肿瘤细胞凋亡。研发人员通过模拟与PBD结合的磷酸化底物结构,报道了一系列多肽类抑制剂,本文对该类抑制剂的最新研究进展进行综述,并对其未来发展趋势予以展望。
Polo-like kinase 1(PLK1),an important polo-like kinase member,plays an important role in regulating cell mitosis,and its overexpression is closely related to a variety of tumors.The PLK1-PBD domain can locate in different cell structures at different mitotic periods.Also,it can regulate the location of PLK1 kinase,lead to mitotic disorders,and ultimately promote tumor cell apoptosis.A series of peptide inhibitors have been reported as phosphorylated substrates to bind with PBD.In this paper,the polypeptide PLK1-PBD inhibitors are classified according to the structure feathers,and the latest research progress and SARs are reviewed.
作者
黄道伟
杨晓聪
张越
张庆伟
李建其
HUANG Dao-wei;YANG Xiao-cong;ZHANG Yue;ZHANG Qing-wei;LI Jian-qi(College of Chemical and Pharmaceutical Engineering,Hebei University of Science and Technology,Shijiazhuang 050018,China;Hebei Pharmaceutical and Chemical Engineering Technology Innovation Center,Shijiazhuang 050018,China;Hebei Provincial Laboratory of Medicinal Molecular Chemistry,Shijiazhuang 050018,China;Novel Technology Center of Pharmaceutical Chemistry,Shanghai Institute of Pharmaceutical Industry Co.,Ltd.,China State Institute of Pharmaceutical Industry Co.,Ltd.,Shanghai 201203.China;Shanghai Engineering Research Center of Pharmaceutical Process,Shanghai 201203.China)
出处
《中国药物化学杂志》
CAS
CSCD
2022年第4期305-313,共9页
Chinese Journal of Medicinal Chemistry
基金
河北省自然科学基金青年基金项目(H2020208007)。
作者简介
黄道伟(1987-),男(汉族),河南信阳人,博士,讲师,硕士生导师,主要从事抗肿瘤新药研究,E-mail:huangdaowei321@163.com;通信作者:张越(1965-),女(汉族),河北石家庄人,教授,硕士生导师,主要从事抗肿瘤新药研发、药物及药物中间体的工艺研究,Tel:(0311)88632186,E-mail:yuezhang02@163.com;李建其(1957-),男(汉族),江苏南通人,研究员,博士生导师,主要从事创新药物及药物合成工艺研究,Tel:(021)55514600-288,E-mail:lijianqb@163.com。
