Discovery of selective phosphatidylinositol 3-kinase inhibitors to treat hematological malignancies

Drug Discovery Today

Volumn 20, Issue 8, 2015, Pages 988-994

  Zhu, Jingyu ^a,b   Hou, Tingjun ^b   Mao, Xinliang ^a,c  

^a SOOCHOW UNIVERSITY   (China)

^b ZHEJIANG UNIVERSITY   (China)

^c MEDICAL COLLEGE OF SOOCHOW UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

2 (2 DIFLUOROMETHYLBENZIMIDAZOL 1 YL) 4,6 DIMORPHOLINO 1,3,5 TRIAZINE; 2 (6 AMINO 9 PURINYLMETHYL) 5 METHYL 3 (2 METHYLPHENYL) 3H QUINAZOLIN 4 ONE; 2 MORPHOLINO 8 PHENYLCHROMONE; BUPARLISIB; IDELALISIB; INTERLEUKIN 6; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PRODRUG; SOMATOMEDIN C; SONOLISIB; WORTMANNIN; ANTINEOPLASTIC AGENT; PHOSPHATIDYLINOSITOL 3 KINASE; PROTEIN KINASE INHIBITOR;

ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CANCER INHIBITION; CELL PROLIFERATION; CHRONIC LYMPHATIC LEUKEMIA; COMPARATIVE MOLECULAR FIELD ANALYSIS; CONFORMATIONAL TRANSITION; HEMATOLOGIC MALIGNANCY; HIGH THROUGHPUT SCREENING; HUMAN; LARGE CELL LYMPHOMA; LYMPHATIC LEUKEMIA; MOLECULAR DYNAMICS; PHYSICAL CHEMISTRY; QUANTITATIVE STRUCTURE ACTIVITY RELATION; SIGNAL TRANSDUCTION; SMALL LYMPHOCYTIC LEUKEMIA; STATIC ELECTRICITY; ANIMAL; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DEVELOPMENT; DRUG EFFECTS; ENZYMOLOGY; HEMATOLOGIC NEOPLASMS; METABOLISM; MOLECULAR DOCKING; MOLECULARLY TARGETED THERAPY; PATHOLOGY; PROCEDURES; PROTEIN CONFORMATION;

ANIMALS; ANTINEOPLASTIC AGENTS; DRUG DISCOVERY; HEMATOLOGIC NEOPLASMS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MOLECULAR DOCKING SIMULATION; MOLECULAR TARGETED THERAPY; PHOSPHATIDYLINOSITOL 3-KINASE; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; QUANTITATIVE STRUCTURE-ACTIVITY RELATIONSHIP; SIGNAL TRANSDUCTION;

EID: 84940614812     PISSN: 13596446     EISSN: 18785832     Source Type: Journal    
DOI: 10.1016/j.drudis.2015.03.009     Document Type: Review

References (55)

1. A. Hamilton, and et al. Targeted therapy in haematological malignancies J. Pathol. 220 2010 404 418
2. R.C. Muise-Helmericks, and et al. Cyclin D expression is controlled post-transcriptionally via a phosphatidylinositol 3-kinase/Akt-dependent pathway J. Biol. Chem. 273 1998 29864 29872
3. D.A. Fruman, and C. Rommel PI3Kdelta inhibitors in cancer: rationale and serendipity merge in the clinic Cancer Discov. 1 2012 562 572
4. L. So, and D.A. Fruman PI3K signalling in B- and T-lymphocytes: new developments and therapeutic advances Biochem. J. 442 2012 465 481
5. D. Mahadevan, and et al. Phase I pharmacokinetic and pharmacodynamic study of the pan-PI3K/mTORC vascular targeted pro-drug SF1126 in patients with advanced solid tumours and B-cell malignancies Eur. J. Cancer 48 2012 3319 3327
6. D.A. Fruman, and C. Rommel PI3K and cancer: lessons, challenges and opportunities Nat. Rev. Drug Discov. 13 2014 140 156
7. P. Liu, and et al. Targeting the phosphoinositide 3-kinase pathway in cancer Nat. Rev. Drug Discov. 8 2009 627 644
8. B.T. Hennessy, and et al. Exploiting the PI3K/AKT pathway for cancer drug discovery Nat. Rev. Drug Discov. 4 2005 988 1004
9. D.J. Rossi, and I.L. Weissman Pten, tumorigenesis, and stem cell self-renewal Cell 125 2006 229 231
10. J. Zhu, and et al. Targeting the phosphatidylinositol 3-kinase/AKT pathway for the treatment of multiple myeloma Curr. Med. Chem. 21 2014 3173 3187
11. A. Silva, and et al. PTEN posttranslational inactivation and hyperactivation of the PI3K/Akt pathway sustain primary T cell leukemia viability J. Clin. Invest. 118 2008 3762 3774
12. P. Sujobert, and et al. Essential role for the p110delta isoform in phosphoinositide 3-kinase activation and cell proliferation in acute myeloid leukemia Blood 106 2005 1063 1066
13. A. Gutierrez, and et al. High frequency of PTEN, PI3K, and AKT abnormalities in T-cell acute lymphoblastic leukemia Blood 114 2009 647 650
14. C. Billottet, and et al. Inhibition of class I phosphoinositide 3-kinase activity impairs proliferation and triggers apoptosis in acute promyelocytic leukemia without affecting atra-induced differentiation Cancer Res. 69 2009 1027 1036
15. Q. Xu, and et al. Survival of acute myeloid leukemia cells requires PI3 kinase activation Blood 102 2003 972 980
16. D. Chiron, and et al. Autocrine insulin-like growth factor 1 and stem cell factor but not interleukin 6 support self-renewal of human myeloma cells Blood Cancer J. 3 2013 e120
17. L. Zhang, and et al. Role of the microenvironment in mantle cell lymphoma: IL-6 is an important survival factor for the tumor cells Blood 120 2012 3783 3792
18. H. Ikeda, and et al. PI3K/p110{delta} is a novel therapeutic target in multiple myeloma Blood 116 2010 1460 1468
19. A. Markham Idelalisib: first global approval Drugs 74 2014 1701 1707
20. C.J. Vlahos, and et al. A specific inhibitor of phosphatidylnositol 3-kinase, 2-(4-morpholinyl)-8-phenyl-4h-1-benzopyran-4-one (Ly294002) J. Biol. Chem. 269 1994 5241 5248
21. E.H. Walker, and et al. Structural determinants of phosphoinositide 3-kinase inhibition by wortmannin, LY294002, quercetin, myricetin, and staurosporine Mol. Cell 6 2000 909 919
22. J.R. Garlich, and et al. A vascular targeted pan phosphoinositide 3-kinase inhibitor prodrug, SF1126, with antitumor and antiangiogenic activity Cancer Res. 68 2008 206 215
23. J.E. Bird, and et al. Bleeding response induced by anti-thrombotic doses of a phosphoinositide 3-kinase (PI3K)-beta inhibitor in mice Throm. Res. 127 2011 560 564
24. H. Tanaka, and et al. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations Clin. Cancer Res. 17 2011 3272 3281
25. F.I. Raynaud, and et al. Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases Cancer Res. 67 2007 5840 5850
26. T. Yamori, and et al. ZSTK474, a novel anticancer drug candidate targeted at phosphatidylinositol-3 kinase: identification of the molecular target using COMPARE analysis Clin. Cancer Res. 11 2005 9115 19115
27. S.M. Maira, and et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor Mol. Cancer Ther. 11 2012 317 328
28. M.P. Wymann, and et al. Wortmannin inactivates phosphoinositide 3-kinase by covalent modification of Lys-802, a residue involved in the phosphate transfer reaction Mol. Cell. Biol. 16 1996 1722 1733
29. N.T. Ihle, and et al. Molecular pharmacology and antitumor activity of PX-866, a novel inhibitor of phosphoinositide-3-kinase signaling Mol. Cancer Ther. 3 2004 763 772
30. T.D. Le Cras, and et al. Inhibition of PI3K by PX-866 prevents transforming growth factor-alpha-induced pulmonary fibrosis Am. J. Path. 176 2010 679 686
31. K. Yu, and et al. PWT-458, a novel pegylated-17-hydroxywortmannin, inhibits phosphatidylinositol 3-kinase signaling and suppresses growth of solid tumors Cancer Biol. Ther. 4 2005 538 545
32. C. Sadhu, and et al. Essential role of phosphoinositide 3-kinase delta in neutrophil directional movement J. Immunol. 170 2003 2647 2654
33. B.J. Lannutti, and et al. CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability Blood 117 2011 591 594
34. I. Angulo, and et al. Phosphoinositide 3-kinase delta gene mutation predisposes to respiratory infection and airway damage Science 342 2013 866 871
35. C. Garcia-Echeverria, and W.R. Sellers Drug discovery approaches targeting the PI3K/Akt pathway in cancer Oncogene 27 2008 5511 5526
36. P. Workman, and et al. Drugging the PI3 kinome: from chemical tools to drugs in the clinic Cancer Res. 70 2010 2146 2157
37. R.H. Shoemaker The NCI60 human tumour cell line anticancer drug screen Nat. Rev. Cancer 6 2006 813 823
38. D. Kong, and T. Yamori JFCR39, a panel of 39 human cancer cell lines, and its application in the discovery and development of anticancer drugs Bioorg. Med. Chem. 20 2012 1947 1951
39. S. Yaguchi, and et al. Antitumor activity of ZSTK474, a new phosphatidylinositol 3-kinase inhibitor J. Natl. Cancer Inst. 98 2006 545 556
40. D.X. Kong, and T. Yamori ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor identified using the JFCR39 drug discovery system Acta Pharm. Sin. 31 2010 1189 1197
41. C. Albanese, and et al. IKKalpha regulates mitogenic signaling through transcriptional induction of cyclin D1 via Tcf Mol. Biol. Cell 14 2003 585 599
42. J.F. Gera, and et al. AKT activity determines sensitivity to mammalian target of rapamycin (mTOR) inhibitors by regulating cyclin D1 and c-myc expression J. Biol. Chem. 279 2004 2737 2746
43. X. Mao, and et al. A small-molecule inhibitor of D-cyclin transactivation displays preclinical efficacy in myeloma and leukemia via phosphoinositide 3-kinase pathway Blood 117 2011 1986 1997
44. K. Han, and et al. Identification of a promising PI3K inhibitor for the treatment of multiple myeloma through the structural optimization J. Hematol. Oncol. 7 2014 9
45. S.Q. Yin, and et al. Preparation of S14161 and its analogues and the discovery of 6-bromo-8-ethoxy-3-nitro-2H-chromene as a more potent antitumor agent in vitro Bioorg. Med. Chem. Lett. 23 2013 3314 3319
46. T. Crabbe Exploring the potential of PI3K inhibitors for inflammation and cancer Biochem. Soc. Trans. 35 2007 253 256
47. K.A. Giuliano, and et al. Advances in high content screening for drug discovery Assay Drug Dev. Tech. 1 2003 565 577
48. M. Wolff, and et al. Automated high content screening for phosphoinositide 3 kinase inhibition using an AKT1 redistribution assay Comb. Chem. High Thr. Scr. 9 2006 339 350
49. T.J. Hou, and X.J. Xu Recent development and application of virtual screening in drug discovery: an overview Curr. Pharm. Des. 10 2004 1011 1033
50. R. Frederick, and et al. Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening Bioorg. Med. Chem. Lett. 19 2009 5842 5847
51. S.J. Shuttleworth, and et al. Progress in the preclinical discovery and clinical development of class I and dual class I/IV phosphoinositide 3-kinase (PI3K) inhibitors Curr. Med. Chem. 18 2011 2686 2714
52. J. Tang, and et al. A virtual screen identified C96 as a novel inhibitor of phosphatidylinositol 3-kinase that displays potent preclinical activity against multiple myeloma in vitro and in vivo Oncotarget 5 2014 3836 3848
53. J. Zhu, and et al. A novel PI3K inhibitor PIK-C98 displays potent preclinical activity against multiple myeloma Oncotarget 6 2015 185 195
54. A.M. Doweyko 3D-QSAR illusions J. Comput. Aided Mol. Des. 18 2004 587 596
55. R. Safavi-Sohi, and J.B. Ghasemi Quasi 4D-QSAR and 3D-QSAR study of the pan class I phosphoinositide-3-kinase (PI3K) inhibitors Med. Chem. Res. 22 2013 1587 1596