Developing FGFR4 inhibitors as potential anti-cancer agents via in silico design, supported by in vitro and cell-based testing

Current Medicinal Chemistry

Volumn 20, Issue 10, 2013, Pages 1203-1217

  Ho, H K ^a,c   Nemeth G ^b   Ng, Y R ^a   Pang, E ^a   Szantai Kis C ^b   Zsakai L ^e   Breza, N ^b   Greff, Z ^b   Horvath Z ^b   Pato J ^b   Szabadkai, I ^b   Szokol, B ^b,e   Baska, F ^b,e   Orfi, L ^b,e   Ullrich, A ^d   Keri G ^b,e   Chua, B T ^a  

^a INSTITUTE OF MEDICAL BIOLOGY   (Singapore)

^b Vichem Chemie Research Ltd   (Hungary)

^c NATIONAL UNIVERSITY OF SINGAPORE   (Singapore)

^d MAX PLANCK INSTITUTE OF BIOCHEMISTRY   (Germany)

^e SEMMELWEIS UNIVERSITY   (Hungary)

Author keywords

FGFR4; Inhibitor; Phosphorylation; Tyrosine Kinase

Indexed keywords

1 TERT BUTYL 3 [6 (3,5 DIMETHOXYPHENYL) 2 (4 DIETHYLAMINOBUTYLAMINO)PYRIDO[2,3 D]PYRIMIDIN 7 YL]UREA; ANTINEOPLASTIC AGENT; FIBROBLAST GROWTH FACTOR INHIBITOR; FIBROBLAST GROWTH FACTOR RECEPTOR 4; PROTEIN TYROSINE KINASE INHIBITOR; UNCLASSIFIED DRUG; V 1170; V 1241; V 1261; V 1291; V 2066; V 2122; V 2128; V 2153; V 3011; V 3019; V 3022; V 3068; V 4002; V 4004; V 4007; V 4015;

AB INITIO CALCULATION; APOPTOSIS; ARTICLE; CANCER CELL CULTURE; CELL MIGRATION; CELL PROLIFERATION; CELL VIABILITY; COMPUTER MODEL; DRUG EFFECT; HUMAN; HUMAN CELL; IC 50; IMMUNOBLOTTING; LIVER CELL CARCINOMA; MOLECULAR DOCKING; PROTEIN PHOSPHORYLATION;

ANTINEOPLASTIC AGENTS; APOPTOSIS; BINDING SITES; CELL LINE, TUMOR; CELL MOVEMENT; CELL SURVIVAL; HUMANS; MOLECULAR DOCKING SIMULATION; PHOSPHORYLATION; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 1; RECEPTOR, FIBROBLAST GROWTH FACTOR, TYPE 4;

EID: 84877946494     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/0929867311320100001     Document Type: Article

References (42)

1. Eswarakumar V.P. Lax I. Schlessinger J. Cytokine Growth Factor Rev 2005 16 (2) 139-149.
2. Cappellen D. De Oliveira C. Ricol D. de Medina S. Bourdin J. Sastre-Garau X. Chopin D. Thiery J.P. Radvanyi F. Nat Genet 1999 23 (1) 18-20.
3. Morgan G.J. Walker B.A. Davies F.E. Nature reviews. Cancer 2012 12 (5) 335-348.
4. Kobrin M.S. Yamanaka Y. Friess H. Lopez M.E. Korc M. Cancer Res 1993 53 (20) 4741-4744.
5. Onose H. Emoto N. Sugihara H. Shimizu K. Wakabayashi I. Eur J Endocrinol 1999 140 (2) 169-173.
6. Qiu W.H. Zhou B.S. Chu P.G. Chen W.G. Chung C. Shih J. Hwu P. Yeh C. Lopez R. Yen Y. World J Gastroenterol 2005 11 (34) 5266-5272.
7. Ho H.K. Pok S. Streit S. Ruhe J.E. Hart S. Lim K.S. Loo H.L. Aung M.O. Lim S.G. Ullrich A. J.Hepatol. 2009 50 (1) 118-127.
8. Shah R.N. Ibbitt J.C. Alitalo K. Hurst H.C. Oncogene 2002 21 (54) 8251-8261.
9. Ye Y.W. Zhou Y. Yuan L. Wang C.M. Du C.Y. Zhou X.Y. Zheng B.Q. Cao X. Sun M.H. Fu H. Shi Y.Q. Cancer.
10. Roidl A. Foo P. Wong W. Mann C. Bechtold S. Berger H.J. Streit S. Ruhe J.E. Hart S. Ullrich A. Ho H.K. Oncogene 29 (10) 1543-1552.
11. Bange J. Prechtl D. Cheburkin Y. Specht K. Harbeck N. Schmitt M. Knyazeva T. Muller S. Gartner S. Sures I. Wang H. Imyanitov E. Haring H.U. Knayzev P. Iacobelli S. Hofler H. Ullrich A. Cancer Res 2002 62 (3) 840-847.
12. da Costa Andrade V.C. Parise O. Hors C.P. de Melo Martins P.C. Silva A.P. Garicochea B. Exp Mol Pathol 2007 82 (1) 53-57.
13. Streit S. Bange J. Fichtner A. Ihrler S. Issing W. Ullrich A. Int J Cancer 2004 111 (2) 213-217.
14. Thussbas C. Nahrig J. Streit S. Bange J. Kriner M. Kates R. Ulm K. Kiechle M. Hoefler H. Ullrich A. Harbeck N. J Clin Oncol 2006 24 (23) 3747-3755.
15. Xu W. Li Y. Wang X. Chen B. Wang Y. Liu S. Xu J. Zhao W. Wu J. Eur J Cancer 46 (18) 3332-3338.
16. Wang J. Yu W. Cai Y. Ren C. Ittmann M.M. Neoplasia 2008 10 (8) 847-856.
17. Seitzer N. Mayr T. Streit S. Ullrich A. Cancer Res 70 (2) 802-812.
18. Zhu X. Zheng L. Asa S.L. Ezzat S. Am J Pathol 177 (6) 2860-2869.
19. Ezzat S. Huang P. Dackiw A. Asa S.L. Clin Cancer Res 2005 11 (3) 1336-1341.
20. Koziczak M. Hynes N.E. J Biol Chem 2004 279 (48) 50004-50011.
21. Keri G. Szekelyhidi Z. Banhegyi P. Varga Z. Hegymegi-Barakonyi B. Szantai-Kis C. Hafenbradl D. Klebl B. Muller G. Ullrich A. Eros D. Horvath Z. Greff Z. Marosfalvi J. Pato J. Szabadkai I. Szilagyi I. Szegedi Z. Varga I. Waczek F. Orfi L. Assay Drug Dev Technol 2005 3 (5) 543-551.
22. Mologni L. Current medicinal chemistry 2011 18 (2) 162-175.
23. Ye Y.W. Zhou Y. Yuan L. Wang C.M. Du C.Y. Zhou X.Y. Zheng B.Q. Cao X. Sun M.H. Fu H. Shi Y.Q. Cancer 117 (23) 5304-5313.
24. Hadari Y.R. Gotoh N. Kouhara H. Lax I. Schlessinger J. Proc Natl Acad Sci U S A 2001 98 (15) 8578-8583.
25. Roidl A. Foo P. Wong W. Mann C. Bechtold S. Berger H.J. Streit S. Ruhe J.E. Hart S. Ullrich A. Ho H.K. Oncogene 2010 29 (10) 1543-1552.
26. Roidl A. Berger H.J. Kumar S. Bange J. Knyazev P. Ullrich A. Clin Cancer Res 2009 15 (6) 2058-2066.
27. Bavetsias V. Crumpler S. Sun C. Avery S. Atrash B. Faisal A. Moore A.S. Kosmopoulou M. Brown N. Sheldrake P.W. Bush K. Henley A. Box G. Valenti M. de Haven Brandon A. Raynaud F.I. Workman P. Eccles S.A. Bayliss R. Linardopoulos S. Blagg J. Journal of medicinal chemistry 2012 55 (20) 8721-8734.
28. Groundwater P.W. Solomons K.R. Drewe J.A. Munawar M.A. Prog Med Chem 1996 33 233-329.
29. Sun L. Tran N. Liang C. Tang F. Rice A. Schreck R. Waltz K. Shawver L.K. McMahon G. Tang C. J Med Chem 1999 42 (25) 5120-5130.
30. Kania R.S. Bender S.L. Borchardt A.J. Braganza J.F. Cripps S.J. Hua Y. Johnson M.D. Johnson T.O. Luu H.T. Palmer C.L. Reich S.H. Tempczyk-russell A.M. Teng M. Thomas C. Varney M.D. Wallace M.B. Indazole compounds and pharmaceutical compositions for inhibiting protein kinases and methods for their use. 2001.
31. Levitzki A. Gilon C. Trends Pharmacol Sci 1991 12 (5) 171-174.
32. Bavetsias V. MacDonald E. Linardopoulos S. Preparation of imidazopyridines as enzyme inhibitors especially Aurora kinase inhibitors for treating cell proliferative diseases. 2007.
33. Bavetsias V. MacDonald E. Linardopoulos S. Preparation of imidazopyridine derivatives useful as enzyme inhibitors for the treatment of cell proliferative and autoimmune diseases. 2009.
34. Liu M. Wang S. Clampit J.E. Gum R.J. Haasch D.L. Rondinone C.M. Trevillyan J.M. Abad-Zapatero C. Fry E.H. Sham H.L. Liu G. Bioorg Med Chem Lett 2007 17 (3) 668-672.
35. Heath W.F.H.J. McDonald J.H.I. Brasca M.G. Orzi F. Crugnola A. Ballinari D. Mariani M. Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents. 2005.
36. Mohammadi M. Froum S. Hamby J.M. Schroeder M.C. Panek R.L. Lu G.H. Eliseenkova A.V. Green D. Schlessinger J. Hubbard S.R. EMBO J 1998 17 (20) 5896-5904.
37. Chohan Z.H. Supuran C.T. Ben Hadda T. Nasim F.U. Khan K.M. J Enzyme Inhib Med Chem 2009 24 (3) 859-870.
38. Fritzen E.L. Brightwell A.S. Erickson L.A. Romero D.L. Bioorg Med Chem Lett 2000 10 (7) 649-652.
39. Ido M. Nagao Y. Higashigawa M. Shibata T. Taniguchi K. Hamazaki M. Sakurai M. Br J Cancer 1991 64 (6) 1103-1107.
40. Zhang N. Wu B. Eudy N. Wang Y. Ye F. Powell D. Wissner A. Feldberg L.R. Kim S.C. Mallon R. Kovacs E.D. Toral-Barza L. Kohler C.A. Bioorg Med Chem Lett 2001 11 (11) 1407-1410.
41. Toullec D. Pianetti P. Coste H. Bellevergue P. Grand-Perret T. Ajakane M. Baudet V. Boissin P. Boursier E. Loriolle F. et al. J Biol Chem 1991 266 (24) 15771-15781.
42. Boschelli D.H. Ye F. Wang Y.D. Dutia M. Johnson S.L. Wu B. Miller K. Powell D.W. Yaczko D. Young M. Tischler M. Arndt K. Discafani C. Etienne C. Gibbons J. Grod J. Lucas J. Weber J.M. Boschelli F. J Med Chem 2001 44 (23) 3965-3977.