作用于不同结合区域PLK1抑制剂的研究进展
摘要
在人类肿瘤发生及肿瘤细胞的增殖过程中有多种蛋白激酶(如:PLKs激酶、Aurora激酶、CDKs激酶)异常表达,其中PLKs激酶在肿瘤细胞的DNA复制及有丝分裂的各阶段中都有着重要的调控作用。PLKs激酶在肿瘤细胞中的过度表达引起越来越多的关注。本文阐释了其中的PLK1抑制剂与激酶不同结合区域的作用机制和结合特点,以及目前各类抑制剂的研究进展。
引文
1崔学振,尚培中.PLK1和Aurora A在消化系统肿瘤中的研究进展[J].中国现代普通外科进展,2016,19(5):395-399
2 任静,蒋孝华.Plk1和Cdk1在细胞周期和肿瘤中的研究进展[J].现代医药卫生,2016,32(6):872-875
3 Andrysik Z,Bernstein W Z,Deng L,et al.The novel mouse Polo-like kinase 5responds to DNA damage and localizes in the nucleolus[J].Nucleic Acids Res,2010,38(9):2931-2943
4 Carcer G,Escobar B,Higuero A M,et al.Plk5,apolo box domain-only protein with specific roles in neurondifferentiation and glioblastoma suppression[J].Mol Cell Biol,31(6):1225-1239
5 Lowery D M,Lim D,Yaffe M B.Structure and function of Pololike kinases[J].Oncogene,2005,24(2):248-259
6 Golsteyn R M,Schultz S J,Bartek J,et al.Cell cycle analysis and chromosomal localization of human Plk1,aputative homologue of the mitotic kinases Drosophila polo and Saccharomyces cerevisiae Cdc5[J].J Cell Sci,1994,107(6):1509-1517
7 Barr F A,SilljéH H,Nigg E A,et al.Polo-like kinase and the orchestration of cell division[J].Nat Rev Mol Cell Biol,2004,5(6):429-440
8 周燕,唐运莲,甘润良,等.PLK1在肿瘤发生中的研究进展[J].医学研究杂志,2015,44(3):158-161
9 Kumar S,Sharma A R,Sharma G,et al.PLK-1:Angel or devil for cell cycle progression[J].Biochimica et Biophysica Acta,2016,190-203
10 卢帅,吴梦秋,颜婷婷,等.Polo样激酶1及其小分子抑制剂的研究进展[J].药学进展,2010,34(3):97-104
11 Hayashi M T,Karlseder J.DNA damage associated with mitosis and cytokinesis failure[J].Oncogene,2013,32(39):4593-4601
12 董宪,张鹏,毕明刚.丝/苏氨酸激酶PLK 1研究进展[J].中国药理学通报,2010,26(3):289-293
13 Hu K,Law J H,Fotovati A,et al.Small interfering RNA library screen identified polo-like kinase-1(PLK1)as a potential therapeutic target for breast cancer that uniquely eliminates tumor-initiating cells[J].Breast Cancer Res,2012,14(1):R22
14 Mehndirattaa S,Saprab S,Singhc G,et al.Quinazolines as Apoptosis Inducers and Inhibitors:A Review of Patent Literature[J].Recent Patents on Anti-Cancer Drug Discovery,2016,11(1):2-66
15 柏静,杨长福,黄高,等.小分子靶向抗肿瘤药物的研究进展[J].肿瘤药学,2015,5(3):168-173
16 赵润,于淼,季宇彬,等.有丝分裂激酶抑制剂研究[J].哈尔滨商业大学学报,2016,32(1):1-5
17 Rudolph D,Steegmaier M,Hoffmann M,et al.BI 6727,a Pololike kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity[J].Clin Cancer Res,2009,15(9):3094-3102
18 Sato Y,Onozaki Y,Sugimoto T,et al.Imidazopyridine derivatives as potent and selective Polo-like kinase(PLK)inhibitors[J].Bioorg Med Chem Lett,2009,19(6):4673-4678
19 Italo B,Dario B.Identification of 4,5-Dihydro-1H-pyrazolo[4,3 -h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1inhibitors[J].J Med Chem,2010,53(9):3532-3551
20 Raymond V F,Emily J H,Michael J R,et al.Design and synthesis of 2-amino-pyrazolo-pyridines as Polo-like kinase 1inhibitors[J].Bioorg Med Chem Lett,2008,18(20):5648-5652
21 Duffey M O,Vos T J,Adams R,et al.Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1(MLN0905)[J].J Med Chem,2012,55(1):197-208
22 Han X,Zhang J,Guo L,et al.A series of beta-carboline derivatives inhibit the kinase activity of PLKs[J].PLoS One,2012,7(10):e46546
23 Santamaria A,Neef R,Eberspcher U,et al.Use of the novel PLK1inhibitor ZK-thiazolidin-one to elucidate functions of PLK1in early and late stages of mitosis[J].Mol Biol Cell 2007,18(10):4024-4036
24 Gjertsen B T,Schffski P.Discovery and development of the pololike kinase inhibitor volasertib in cancer therapy[J].Leukemia,2015,29(1):1-19
25 Van den Bossche J,Lardon F,Deschoolmeester V,et al.Spotlight on Volasertib:Preclinical and Clinical Evaluation of a Promising Plk1Inhibitor[J].Medicinal Research Reviews,2016,36(4):749-786
26 孙善亮,张亮,刘海春,等.PLK1激酶域抑制剂的构效关系与作用模式[J].中国医药工业杂志,2013,44(10):1036-1046
27 姚爱红,常玉杰,江程,等.作用于Polo-box结构域的Polo样激酶1 抑制剂的研究进展[J].药学前沿,2016,47(1):1-8
28 Reddy M V,Mallireddigari M R,Cosenza S C,et al.Design,synthesis,and biological evaluation of(E)styrylbenzylsulfones as novel anticancer agents[J].J Med Chem,2008,51(1):86-100
29 Chen D X,Huang J,Liu M,et al.Design,synthesis,and evaluation of non-ATP-competitive small-molecule Polo-like kinase 1(Plk1)inhibitors[J].Arch Pharm,2015,348(1):2-9
30 Liu M,Huang J,Chen D X,et al.Identification of indole-3-carboxylic acids as non-ATP-competitive polo-like kinase 1(Plk1)inhibitors[J].Bioorg Med Chem Lett,2015,25(3):431-43431 Xu J,Shen C,Wang T,et al.Structural basis for the inhibition of polo-like kinase 1[J].Nat Struct Mol Biol,2013,20(9):1047-1053
32 Jang Y,Lin C Y,Ma S,et al.Functional studies on the role of the C-terminal domain of mammalian polo-like kinase[J].Proc Natl Acad Sci USA,2002,99(4):1984-1989
33 宗可昕,张晶,陈云雨,等.PLK1PBD靶向抗肿瘤抑制剂的筛选及活性研究[J].中国医药生物技术,2016,11(1):13-20
34 张智慧,张晶,刘伟等.以PLK1PBD为靶点的小分子抑制剂筛选及其抗癌活性研究[J].中国医药生物技术,2015,10(2):125-129
35 Ahn M,Han Y H,Park J E,et al.A new class of peptidomimetics targeting the polo-box domain of polo-like kinase 1[J].J Med Chem,2015,58(1):294-304
36 Murugan R N,Park J E,Lim D,et al.Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1[J].Bioorg Med Chem,2013,21(9):2623-2634
37 Angela Berg and Thorsten Berg.Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1[J].ChemBioChem,2016,17:650-656
38蒋思明,王朝霞.保罗样激酶PLK1与肿瘤预后及治疗研究进展[J].现代肿瘤医学,2013,21(3):650-653
2 任静,蒋孝华.Plk1和Cdk1在细胞周期和肿瘤中的研究进展[J].现代医药卫生,2016,32(6):872-875
3 Andrysik Z,Bernstein W Z,Deng L,et al.The novel mouse Polo-like kinase 5responds to DNA damage and localizes in the nucleolus[J].Nucleic Acids Res,2010,38(9):2931-2943
4 Carcer G,Escobar B,Higuero A M,et al.Plk5,apolo box domain-only protein with specific roles in neurondifferentiation and glioblastoma suppression[J].Mol Cell Biol,31(6):1225-1239
5 Lowery D M,Lim D,Yaffe M B.Structure and function of Pololike kinases[J].Oncogene,2005,24(2):248-259
6 Golsteyn R M,Schultz S J,Bartek J,et al.Cell cycle analysis and chromosomal localization of human Plk1,aputative homologue of the mitotic kinases Drosophila polo and Saccharomyces cerevisiae Cdc5[J].J Cell Sci,1994,107(6):1509-1517
7 Barr F A,SilljéH H,Nigg E A,et al.Polo-like kinase and the orchestration of cell division[J].Nat Rev Mol Cell Biol,2004,5(6):429-440
8 周燕,唐运莲,甘润良,等.PLK1在肿瘤发生中的研究进展[J].医学研究杂志,2015,44(3):158-161
9 Kumar S,Sharma A R,Sharma G,et al.PLK-1:Angel or devil for cell cycle progression[J].Biochimica et Biophysica Acta,2016,190-203
10 卢帅,吴梦秋,颜婷婷,等.Polo样激酶1及其小分子抑制剂的研究进展[J].药学进展,2010,34(3):97-104
11 Hayashi M T,Karlseder J.DNA damage associated with mitosis and cytokinesis failure[J].Oncogene,2013,32(39):4593-4601
12 董宪,张鹏,毕明刚.丝/苏氨酸激酶PLK 1研究进展[J].中国药理学通报,2010,26(3):289-293
13 Hu K,Law J H,Fotovati A,et al.Small interfering RNA library screen identified polo-like kinase-1(PLK1)as a potential therapeutic target for breast cancer that uniquely eliminates tumor-initiating cells[J].Breast Cancer Res,2012,14(1):R22
14 Mehndirattaa S,Saprab S,Singhc G,et al.Quinazolines as Apoptosis Inducers and Inhibitors:A Review of Patent Literature[J].Recent Patents on Anti-Cancer Drug Discovery,2016,11(1):2-66
15 柏静,杨长福,黄高,等.小分子靶向抗肿瘤药物的研究进展[J].肿瘤药学,2015,5(3):168-173
16 赵润,于淼,季宇彬,等.有丝分裂激酶抑制剂研究[J].哈尔滨商业大学学报,2016,32(1):1-5
17 Rudolph D,Steegmaier M,Hoffmann M,et al.BI 6727,a Pololike kinase inhibitor with improved pharmacokinetic profile and broad antitumor activity[J].Clin Cancer Res,2009,15(9):3094-3102
18 Sato Y,Onozaki Y,Sugimoto T,et al.Imidazopyridine derivatives as potent and selective Polo-like kinase(PLK)inhibitors[J].Bioorg Med Chem Lett,2009,19(6):4673-4678
19 Italo B,Dario B.Identification of 4,5-Dihydro-1H-pyrazolo[4,3 -h]quinazoline derivatives as a new class of orally and selective Polo-like kinase 1inhibitors[J].J Med Chem,2010,53(9):3532-3551
20 Raymond V F,Emily J H,Michael J R,et al.Design and synthesis of 2-amino-pyrazolo-pyridines as Polo-like kinase 1inhibitors[J].Bioorg Med Chem Lett,2008,18(20):5648-5652
21 Duffey M O,Vos T J,Adams R,et al.Discovery of a potent and orally bioavailable benzolactam-derived inhibitor of Polo-like kinase 1(MLN0905)[J].J Med Chem,2012,55(1):197-208
22 Han X,Zhang J,Guo L,et al.A series of beta-carboline derivatives inhibit the kinase activity of PLKs[J].PLoS One,2012,7(10):e46546
23 Santamaria A,Neef R,Eberspcher U,et al.Use of the novel PLK1inhibitor ZK-thiazolidin-one to elucidate functions of PLK1in early and late stages of mitosis[J].Mol Biol Cell 2007,18(10):4024-4036
24 Gjertsen B T,Schffski P.Discovery and development of the pololike kinase inhibitor volasertib in cancer therapy[J].Leukemia,2015,29(1):1-19
25 Van den Bossche J,Lardon F,Deschoolmeester V,et al.Spotlight on Volasertib:Preclinical and Clinical Evaluation of a Promising Plk1Inhibitor[J].Medicinal Research Reviews,2016,36(4):749-786
26 孙善亮,张亮,刘海春,等.PLK1激酶域抑制剂的构效关系与作用模式[J].中国医药工业杂志,2013,44(10):1036-1046
27 姚爱红,常玉杰,江程,等.作用于Polo-box结构域的Polo样激酶1 抑制剂的研究进展[J].药学前沿,2016,47(1):1-8
28 Reddy M V,Mallireddigari M R,Cosenza S C,et al.Design,synthesis,and biological evaluation of(E)styrylbenzylsulfones as novel anticancer agents[J].J Med Chem,2008,51(1):86-100
29 Chen D X,Huang J,Liu M,et al.Design,synthesis,and evaluation of non-ATP-competitive small-molecule Polo-like kinase 1(Plk1)inhibitors[J].Arch Pharm,2015,348(1):2-9
30 Liu M,Huang J,Chen D X,et al.Identification of indole-3-carboxylic acids as non-ATP-competitive polo-like kinase 1(Plk1)inhibitors[J].Bioorg Med Chem Lett,2015,25(3):431-43431 Xu J,Shen C,Wang T,et al.Structural basis for the inhibition of polo-like kinase 1[J].Nat Struct Mol Biol,2013,20(9):1047-1053
32 Jang Y,Lin C Y,Ma S,et al.Functional studies on the role of the C-terminal domain of mammalian polo-like kinase[J].Proc Natl Acad Sci USA,2002,99(4):1984-1989
33 宗可昕,张晶,陈云雨,等.PLK1PBD靶向抗肿瘤抑制剂的筛选及活性研究[J].中国医药生物技术,2016,11(1):13-20
34 张智慧,张晶,刘伟等.以PLK1PBD为靶点的小分子抑制剂筛选及其抗癌活性研究[J].中国医药生物技术,2015,10(2):125-129
35 Ahn M,Han Y H,Park J E,et al.A new class of peptidomimetics targeting the polo-box domain of polo-like kinase 1[J].J Med Chem,2015,58(1):294-304
36 Murugan R N,Park J E,Lim D,et al.Development of cyclic peptomer inhibitors targeting the polo-box domain of polo-like kinase 1[J].Bioorg Med Chem,2013,21(9):2623-2634
37 Angela Berg and Thorsten Berg.Inhibitors of the Polo-Box Domain of Polo-Like Kinase 1[J].ChemBioChem,2016,17:650-656
38蒋思明,王朝霞.保罗样激酶PLK1与肿瘤预后及治疗研究进展[J].现代肿瘤医学,2013,21(3):650-653
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