Discovery and characterization of a novel inhibitor of CDC25B, LGH00045

Acta Pharmacologica Sinica

Volumn 29, Issue 10, 2008, Pages 1268-1274

  Feng, Xu ^a   Wang, Li Na ^b   Zhou, Yue Yang ^b   Yu, Hai Ping ^b   Shen, Qiang ^b   Zang, Yi ^b   Zhou, Yu Bo ^b   Li, Jing Ya ^b   Zhang, Hai Xia ^a   Li, Jia ^b  

^a LANZHOU UNIVERSITY   (China)

^b SHANGHAI INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

Cell circle; Cell division cycle 25B; Cyclin dependent kinase 1; High throughput screening; Inhibitor; LGH00045

Indexed keywords

3 (2 CHLOROPHENYL) 6 [(2 FURAN 2 YL)VINYL) [1,2,4]TRIAZOLO[3,4 B][1,3,4]THIADIAZOLE); BETA ACTIN; COMPLEMENTARY DNA; CYCLIN B1; CYCLIN DEPENDENT KINASE; LGH 00045; PROTEIN TYROSINE PHOSPHATASE; PROTEIN TYROSINE PHOSPHATASE 1B INHIBITOR; PROTEIN TYROSINE PHOSPHATASE INHIBITOR; UNCLASSIFIED DRUG;

ARTICLE; CANCER INHIBITION; CELL CYCLE G2 PHASE; CELL CYCLE M PHASE; CELL CYCLE PROGRESSION; CELL PROLIFERATION; ENZYME SPECIFICITY; HELA CELL; HIGH THROUGHPUT SCREENING; IC 50; NONHUMAN;

CDC2 PROTEIN KINASE; CDC25 PHOSPHATASES; CELL LINE, TUMOR; CELL PROLIFERATION; CELL SURVIVAL; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; ENZYME INHIBITORS; GENE EXPRESSION REGULATION, ENZYMOLOGIC; HUMANS; PLASMIDS;

EID: 53749088462     PISSN: 16714083     EISSN: 17457254     Source Type: Journal    
DOI: 10.1111/j.1745-7254.2008.00841.x     Document Type: Article

References (26)

1. Cao S, Foster C, Brisson M, Lazo JS, Kingston DG. Halenaquinone and xestoquinone derivatives, inhibitors of CDC25B phosphatase from a Xestospongia sp. Bioorg Med Chem 2005 13 : 999 1003.
2. Mailand N, Falck J, Lukas C, Syljuåsen RG, Welcker M, Lukas J. Rapid destruction of human CDC25A in response to DNA damage. Science 2000 288 : 1425 9.
3. Nilsson I, Hoffmann I. Cell cycle regulation by the CDC25 phosphatase family. Prog Cell Cycle Res 2000 4 : 107 14.
4. Turowski P, Franckhauser C, Morris MC, Vaglio P, Fernandez A, Lamb NJ. Functional CDC25C dual-specificity phosphatase is required for S-phase entry in human cells. Mol Biol Cell 2003 14 : 2984 98.
5. Lyon MA, Ducret AP, Wipf P, Lazo JS. Dual-specificity phosphatases as targets for antineoplastic agents. Nat Rev Drug Discov 2002 1 : 961 76.
6. Cangi MG, Cukor B, Soung P, Signoretti S, Moreira G Jr., Ranashinge M, et al. Role of the CDC25A phosphatase in human breast cancer. J Clin Invest 2000 106 : 753 61.
7. Broggini M, Buraggi G, Brenna A, Riva L, Codegoni AM, Torri V, et al. Cell cycle-related phosphatases CDC25A and B expression correlates with survival in ovarian cancer patients. Anticancer Res 2000 20 : 4835 40.
8. Ngan ES, Hashimoto Y, Ma ZQ, Tsai MJ, Tsai SY. Overexpression of CDC25B, an androgen receptor coactivator, in prostate cancer. On-cogene 2003 22 : 734 9.
9. Sasaki H, Yukiue H, Kobayashi Y, Tanahashi M, Moriyama S, Na-kashima Y, et al. Expression of the CDC25B gene as a prognosis marker in non-small cell lung cancer. Cancer Lett 2001 173 : 187 92.
10. Talvinen K, Tuikkala J, Grönroos J, Huhtinen H, Kronqvist P, Aittokallio T, et al. Biochemical and clinical approaches in evaluating the prognosis of colon cancer. Anticancer Res 2006 26 : 4745 51.
11. Sato Y, Sasaki H, Kondo S, Fukai I, Kiriyama M, Yamakawa Y, et al. Expression of the CDC25B mRNA correlated with that of N-myc in neuroblastoma. Jpn J Clin Oncol 2001 31 : 428 31.
12. Galaktionov K, Lee AK, Eckstein J, Draetta G, Meckler J, Loda M, et al. CDC25 phosphatases as potential human oncogenes. Science 1995 269 : 1575 7.
13. Ma ZQ, Chua SS, DeMayo FJ, Tsai SY. Induction of mammary gland hyperplasia in transgenic mice over-expressing human CDC25B. Oncogene 1999 18 : 4564 76.
14. Yao Y, Slosberg ED, Wang L, Hibshoosh H, Zhang YJ, Xing WQ, et al. Increased susceptibility to carcinogeninduced mammary tumors in MMTV- CDC25B transgenic mice. Oncogene 1999 18 : 5159 66.
15. Millar JB, Blevitt J, Gerace L, Sadhu K, Featherstone C, Russell P. p55CDC25 is a nuclear phosphoprotein required for the initiation of mitosis in human cells. Proc Natl Acad Sci USA 1991 88 : 10 500 4.
16. Lammer C, Wagerer S, Saffrich R, Mertens D, Ansorge W, Hoffmann I. The CDC25B phosphatase is essential for the G2/M phase transition in human cells. J Cell Sci 1998 111 : 2445 53.
17. Gabrielli BG, De Souza CP, Tonks ID, Clark JM, Hayward NK, El-lem KA. Cytoplasmic accumulation of CDC25B phosphatase in mitosis triggers centrosomal microtubule nucleation in HeLa cells. J Cell Sci 1996 109 : 1081 93.
18. Hoffman I, Draetta I, Karsenti G. Activation of the phosphatase activity of human CDC25 A by a CDK2-cyclin E dependent phosphory-lation at the Gl/S transition. EMBO J 1994 13 : 4302 10.
19. Jinno S, Suto K, Nagata A, Igarashi M, Kanaoka Y, Nojima H, et al. CDC25A is a novel phosphatase functioning early in the cell cycle. EMBO J 1994 13 : 1549 56.
20. Boutros R, Lobjois V, Ducommun B. CDC25 phosphatases in cancer cells: key players Good targets? Nature Reviews Cancer 2005 7 : 495 507.
21. Kar S, Wang M, Ham SW, Carr BI. H32, a nonquinone sulfone analog of vitamin K3, inhibits human hepatoma cell growth by inhibiting Cdc25 and activating ERK. Cancer Biol Ther 2006 5 : 1340 7.
22. Wrobel J, Sredy J, Moxham C, Dietrich A, Li Z, Sawicki DR, et al. PTP 1B inhibition and antihyperglycemic activity in the ob/ob mouse model of novel ll-arylbenzo[b]naphtho[2, 3-d]furans and ll-arylbenzo[b]naphtho[2, 3-d]thiophenes. J Med Chem 1999 42 : 3199 202.
23. Cheon HG, Kim SM, Yang SD, Ha JD, Choi JK. Discovery of a novel protein tyrosine phosphatase-IB inhibitor, KR61639: potential development as an antihyperglycemic agent. Eur J Pharmacol 2004 485 : 333 9.
24. Shi L, Yu HP, Zhou YY, Du JQ, Shen Q, Li JY, et al. Discovery of a novel competitive inhibitor of PTP1B by high-throughput screening. Acta Pharmacol Sin 2008 29 : 278 84.
25. Brezak MC, Quaranta M, Contour-Galcera MO, Lavergne O, Mondesert O, Auvray P, et al. Inhibition of human tumor cell growth in vivo by an orally bioavailable inhibitor of CDC25 phosphatases. Mol Cancer Ther 2005 4 : 1378 87.
26. Brisson M, Nguyen T, Vogt A, Yalowich J, Giorgianni A, Tobi D, et al. Discovery and characterization of novel small molecule inhibitors of human CDC25B dual specificity phosphatase. Mol Pharmacol 2004 66 : 824 33.