Protein structure: Discovering selective protein kinase inhibitors

Drug Discovery Today: TARGETS

Volumn 2, Issue 3, 2003, Pages 101-108

  Buchanan, Sean G ^a  

^a ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [4 METHYL 2 (2 OXO 3 INDOLINYLMETHYLIDENYL) 3 PYRROLYL]PROPIONIC ACID; 4 AMINO 1 TERT BUTYL 3 (4 METHYLPHENYL)PYRAZOLO[3,4]PYRIMIDINE; 7 HYDROXYSTAUROSPORINE; CANERTINIB; DORAMAPIMOD; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; ERLOTINIB; GEFITINIB; IMATINIB; LAPATINIB; LFM A 13; MIDOSTAURIN; PROTEIN KINASE INHIBITOR; SB 242235; SEMAXANIB; STAUROSPORINE DERIVATIVE; SU 4984; TRASTUZUMAB; UNCLASSIFIED DRUG;

ALKYLATION; AMINO ACID SEQUENCE; BREAST CANCER; CARBOXY TERMINAL SEQUENCE; CATALYSIS; CRYSTAL STRUCTURE; DRUG ACTIVITY; DRUG RESEARCH; ENZYME ACTIVE SITE; ENZYME INHIBITION; ENZYME STRUCTURE; GENE MUTATION; GENOMICS; HUMAN; NONHUMAN; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN DOMAIN; PROTEIN FAMILY; PROTEIN PHOSPHORYLATION; REVIEW; RNA INTERFERENCE; SEQUENCE HOMOLOGY; STRUCTURE ACTIVITY RELATION;

EID: 15744399378     PISSN: 17418372     EISSN: None     Source Type: Journal    
DOI: 10.1016/s1477-3627(03)02320-1     Document Type: Review

References (64)

1. Manning, G. et al. (2002) The protein kinase complement of the human genome. Science 298, 1912-1934
2. Blume-Jensen, P. and Hunter, T. (2001) Oncogenic kinase signalling. Nature 411, 355-365
3. Capdeville, R. et al. (2002) Glivec (STI571, imatinib), a rationally developed, targeted anticancer drug. Nat. Rev. Drug. Discov. 1, 493-502
4. Twombly, R. (2002) Despite concerns. FDA panel backs EGFR inhibitor. J. Natl. Cancer Inst. 94, 1596-1597
5. Baselga, J. et al. (2002) Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types. J. Clin. Oncol. 20, 4292-4302
6. Wakeling, A.E. et al. (2002) ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy. Cancer Res. 62, 5749-5754
7. Taylor, S.S. et al. (1992) Structural framework for the protein kinase family. Annu. Rev. Cell Biol. 8, 429-462
8. Liu, Y. et al. (1999) Structural basis for selective inhibition of Src family kinases by PP1. Chem. Biol. 6, 671-678
9. Ruegg, U.T. and Burgess, G.M. (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases. Trends Pharmacol. Sci. 10, 218-220
10. Waltenberger, J. et al. (1999) A dual inhibitor of platelet-derived growth factor beta-receptor and Src kinase activity potently interferes with motogenic and mitogenic responses to PDGF in vascular smooth muscle cells. A novel candidate for prevention of vascular remodeling. Circ. Res. 85, 12-22
11. Carlomagno, F. et al. (2002) The kinase inhibitor PP1 blocks tumorigenesis induced by RET oncogenes. Cancer Res. 62, 1077-1082
12. Tatton, L. et al. (2003) The Src-selective kinase inhibitor PP1 also inhibits kit and Bcr-Abl tyrosine kinases. J. Biol. Chem. 278, 4847-1853
13. Shah, N. et al. (2002) Multiple BCR-ABL kinase domain mutations confer polyclonal resistance to the tyrosine kinase inhibitor imatinib (STI571) in chronic phase and blast crisis chronic myeloid leukemia. Cancer Cell 2, 117-125
14. Zimmermann, J. et al. (1997) Potent and selective inhibitors of the ABL-kinase: phenylaminopyrimidine (PAP) derivatives. Bioorg. Med. Chem. Lett. 7, 187-192
15. Sawyers, C.L. (2002) Finding the next Gleevec: FLT3 targeted kinase inhibitor therapy for acute myeloid leukemia. Cancer Cell 1, 413-415
16. Regan, J. et al. (2002) Pyrazole urea-based inhibitors of p38 MAP kinase: from lead compound to clinical candidate. J. Med. Chem. 45, 2994-3008
17. Davies, S.P. et al. (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351, 95-105
18. Adams, J. et al. (2002) A strategy for the design of multiplex inhibitors for kinase-mediated signalling in angiogenesis. Curr. Opin. Chem. Biol. 6, 486-492
19. Pargellis, C. et al. (2002) Inhibition of p38 MAP kinase by utilizing a novel allosteric binding site. Nat. Struct. Biol. 9, 268-272
20. Nagar, B. et al. (2003) Structural Basis for the Autoinhibition of c-Abl Tyrosine Kinase. Cell 112, 859-871
21. Hantschel, O. et al. (2003) A Myristoyl/phosphotyrosine switch regulates c-Abl. Cell 112, 845-857
22. Chang, C.I. et al. (2002) Crystal structures of MAP kinase p38 complexed to the docking sites on its nuclear substrate MEF2A and activator MKK3b. Mol. Cell 9, 1241-1249
23. Parang, K. et al. (2001) Mechanism-based design of a protein kinase inhibitor. Nat. Struct. Biol. 8, 37-41
24. Ripka, A.S. and Rich, D.H. (1998) Peptidomimetic design. Curr. Opin. Chem. Biol. 2, 441-452
25. de Bono, J.S. and Rowinsky, E.K. (2002) The ErbB receptor family: a therapeutic target for cancer. Trends Mol. Med. 8(Suppl 4), S19-26
26. Wilson, F.H. et al. (2001) Human hypertension caused by mutations in WNK kinases. Science 293, 1107-1112
27. Hanks, S.K. and Hunter, T. (1995) Protein kinases 6. The eukaryotic protein kinase superfamily: kinase (catalytic) domain structure and classification. FASEB J. 9, 576-596
28. Scapin, G. (2002) Structural biology in drug design: selective protein kinase inhibitors. Drug Discov. Today 7, 601-611
29. Toledo, L.M. et al. (1999) The structure-based design of ATP-site directed protein kinase inhibitors. Curr. Med. Chem. 6, 775-805
30. Mahajan, S. et al. (1999) Rational design and synthesis of a novel antileukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13. J. Biol. Chem. 274, 9587-9599
31. Singh, J. et al. (1997) Structure-based design of a potent, selective, and irreversible inhibitor of the catalytic domain of the erbB receptor subfamily of protein tyrosine kinases. J. Med. Chem. 40, 1130-1135
32. Bridges, A.J. (2001) Chemical inhibitors of protein kinases. Chem. Rev. 101, 2541-2572
33. Stamos, J. et al. (2002) Structure of the epidermal growth factor receptor kinase domain alone and in complex with a 4-anilinoquinazoline inhibitor. J. Biol. Chem. 277, 46265-46272
34. Mohammadi, M. et al. (1997) Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science 276, 955-960
35. Zhao, B. et al. (2002) Structural basis for Chk1 inhibition by UCN-01. J. Biol. Chem. 277, 46609-46615
36. Fox, T. et al. (1998) A single amino acid substitution makes ERK2 susceptible to pyridinyl imidazole inhibitors of p38 MAP kinase. Protein Sci. 7, 2249-2255
37. Wilson, K.P. et al. (1997) The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase. Chem. Biol. 4, 423-431
38. Lisnock, J. et al. (1998) Molecular basis forp38 protein kinase inhibitor specificity. Biochemistry 37, 16573-16581
39. Wang, Z. et al. (1998) Structural basis of inhibitor selectivity in MAP kinases. Structure 6, 1117-1128
40. Bishop, A.C. et al. (2001) Magic bullets for protein kinases. Trends Cell Biol. 11, 167-172
41. Schindler, T. et al. (2000) Structural mechanism for STI-571 inhibition of abelson tyrosine kinase. Science 289, 1938-1942
42. Shewchuk, L.M. et al. (2000) Structure of the Tie2 RTK domain: self-inhibition by the nucleotide binding loop, activation loop, and C-terminal tail. Structure Fold. Des. 8, 1105-1113
43. Wybenga-Groot, L.E. et al. (2001) Structural basis for autoinhibition of the Ephb2 receptor tyrosine kinase by the unphosphorylated juxtamembrane region. Cell 106, 745-757
44. Meng, W. et al. (2002) Structure of mitogen-activated protein kinase-activated protein (MAPKAP) kinase 2 suggests a bifunctional switch that couples kinase activation with nuclear export. J. Biol. Chem. 277, 37401-37405
45. Kobe, B. et al. (1996) Giant protein kinases: domain interactions and structural basis of autoregulation. EMBO J. 15, 6810-6821
46. Xu, W. et al. (1997) Three-dimensional structure of the tyrosine kinase c-Src. Nature 385, 595-602
47. Sicheri, F. et al. (1997) Crystal structure of the Src family tyrosine kinase Hck. Nature 385, 602-609
48. Mao, C. et al. (2001) Crystal structure of Bruton's tyrosine kinase domain suggests a novel pathway for activation and provides insights into the molecular basis of X-linked agammaglobulinemia. J. Biol. Chem. 276, 41435-41443
49. Taylor, S.S. and Radzio-Andzelm, E. (1997) Protein kinase inhibition: natural and synthetic variations on a theme. Curr. Opin. Chem. Biol. 1, 219-226
50. Russo, A.A. et al. (1996) Crystal structure of the p27Kip1 cyclin-dependent-kinase inhibitor bound to the cyclin A-Cdk2 complex. Nature 382, 325-331
51. Hubbard, S.R. et al. (1994) Crystal structure of the tyrosine kinase domain of the human insulin receptor. Nature 372, 746-754
52. Ogawa, A. et al. (2002) Structure of the carboxyl-terminal Src kinase, Csk. J. Biol. Chem. 277, 14351-14354
53. Huse, M. and Kuriyan, J. (2002) The conformational plasticity of protein kinases. Cell 109, 275-282
54. Nagar, B. et al. (2002) Crystal structures of the kinase domain of c-Abl in complex with the small molecule inhibitors PD173955 and imatinib (STI-571). Cancer Res. 62, 4236-4243
55. Hamuro, Y. et al. (2002) Phosphorylation driven motions in the COOH-terminal Src kinase, CSK, revealed through enhanced hydrogen-deuterium exchange and mass spectrometry (DXMS). J. Mol. Biol. 323, 871-881
56. Buchanan, S.G. (2002) Structural genomics: bridging functional genomics and structure-based drug design. Curr. Opin. Drug Discov. Devel. 5, 367-381
57. Burley, S.K. et al. (1999) Structural genomics: beyond the human genome project. Nat. Genet. 23, 151-157
58. Goulding, C.W. et al. (2002) The TB structural genomics consortium: providing a structural foundation for drug discovery. Curr. Drug Targets Infect. Disord. 2, 121-141
59. Ghosh, S. et al. (1999) Structure-based design of potent inhibitors of EGF-receptor tyrosine kinase as anti-cancer agents. Anticancer Drug Des. 14, 403-410
60. Sudbeck, E.A. et al. (1999) Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin. Cancer Res. 5, 1569-1582
61. Cheek, S. et al. (2002) Sequence and structure classification of kinases. J. Mol. Biol. 320, 855-881
62. Ikuta, M. et al. (2001) Crystallographic approach to identification of cyclin-dependent kinase 4 (CDK4)-specific inhibitors by using CDK4 mimic CDK2 protein. J. Biol. Chem. 276, 27548-27554
63. Zheng, J. et al. (1993) Crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MgATP and peptide inhibitor. Biochemistry 32, 2154-2161
64. Christopher, J. (1998) SPOCK: The Structural Properties Observation and Calculation Kit (Program Manual)., http://quorum.tamu.edu/spock/