The development and therapeutic potential of protein kinase inhibitors

Current Opinion in Chemical Biology

Volumn 3, Issue 4, 1999, Pages 459-465

  Cohen, Philip ^a  

^a UNIVERSITY OF DUNDEE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN KINASE; PROTEIN KINASE INHIBITOR;

CELL MEMBRANE PERMEABILITY; CLINICAL TRIAL; DRUG SPECIFICITY; HUMAN; REVIEW; THERAPY;

EID: 0033178359     PISSN: 13675931     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1367-5931(99)80067-2     Document Type: Article

References (45)

1. Liu J, Farmer JD, Lane WS, Friedman J, Weissman I, Schreiber SL: Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell 1991, 66:807-815.
2. Jonuleit T, Peschel C, Schwab R, van der Kuip H, Buchdunger E, Fischer T, Huber C, Aulitzky WE: Bcr-Abl kinase promotes cell cycle entry of primary myeloid CML cells in the absence of growth factors. Br J Haematol 1998, 100:295-303. This paper shows that CGP 57148, a potent inhibitor of both the PDGF receptor and the Abl tyrosine kinase, corrects abnormal negative cell cycle control in Bcr-Abl-expressing leukaemic cells, without affecting cell cycle control in normal cells.
3. Carroll M, Ohno-Jones S, Tamura S, Buchdunger E, Zimmermann J, Lydon NB, Gilliland DG, Druker BJ: CGP 57148, a tyrosine kinase inhibitor, inhibits the growth of cells expressing BCR-ABL, TEL-ABL and TEL-PDGR fusion proteins. Blood 1997, 90:4947-4952.
4. Le Coutre P, Mologni L, Cleris L, Marchesi E, Buchdunger E, Giardini R, Formelli F, Gambacorti-Passerini C: In vivo eradication of human BCR/ABL-positive leukaemia cells with an ABL kinase inhibitor. J Natl Cancer Inst 1999, 91:163-168. This paper shows that the prolonged administration of CGP 57148B cures 87-100% of mice bearing tumours as a result of the injection of Bcr/Abl-positive human leukaemia cells.
5. Ruckemann K, Fairbanks LD, Carrey EA, Hawrylowicz CM, Richards DF, Kirschbaum B, Simmonds HA: Leflunomide inhibits pyrimidine de novo synthesis in mitogen-stimulated T-lymphocytes from healthy humans. J Biol Chem 1998, 34:21682-21691.
6. Shawver LK, Schwartz DP, Taylorson LT, Longhi MP, Jacobs JS, Powell TJ, Hirth KP: SU 101, a Potent Inhibitor of PDGF-mediated Signaling, Inhibits Growth of a Wide Variety of Tumor Types in Vivo. Abstract at the American Association for Cancer Research, 1996 April: Washington, DC, USA.
7. Woodburn JR, Morris CO, Kelly H, Laight A: EGF receptor tyrosine kinase inhibitors as anti-cancer agents: Pre-clinical and early clinical profile of ZD 1839. Cell Mol Biol Lett 1998, 3:348-349. A specific inhibitor of the EGF receptor that has entered human clinical trials.
8. Moyer JD, Barbacci EG, Iwada KK, Arnold L, Boman B, Cunningham A, DiOrio C, Doty J, Worin MJ, Moyer MP et al.: Induction of apoptosis and cell cycle arrest by CP-358774, an inhibitor of epidermal growth factor receptor tyrosine kinase. Cancer Res 1997, 57:4838-4848.
9. Meydan N, Grunberger T, Dadi H, Shahar M, Arpaia E, Lapidot Z, Leeder JS, Freedman M, Cohen A, Gazit A et al.: Inhibition of acute lymphoblastic leukaemia by a Jak-2 inhibitor. Nature 1996, 379:645-648.
10. Hanahan D, Folkman J: Patterns and emerging mechanisms of the angiogenic switch during tumorigenesis. Cell 1996, 86:353-364.
11. Fong TAT, Shawver LK, Sun L, Tang C, App H, Powell J, Kim YH, Schreck R, Wang X, Risau W et al.: SU5416 is a potent and selective inhibitor of the vascular endothelial growth factor receptor (Flk-1/KDR) that inhibits tyrosine kinase catalysis, tumour vacularisation and growth of multiple tumour types. Cancer Res 1999, 59:99-106. A specific inhibitor of the VEGF receptor tyrosine kinase that will enter Phase III clinical trials later this year.
12. Mohammadi M, Froum S, Hamby JM, Schroeder MC, Panek RL, Lu GH, Eliseenkova AV, Green D, Schlessinger J, Hubbard SR: Crystal structure of an angiogenesis inhibitor bound to the FGF receptor tyrosine kinase domain. EMBO J 1998, 17:5896-5904.
13. Dudley DT, Pang L, Decker SJ, Bridges AJ, Saltiel AR: A synthetic inhibitor of the mitogen-activated protein kinase cascade. Proc Natl Acad Sci USA 1995, 92:7686-7689.
14. Alessi DR, Cuenda A, Cohen P, Dudley DT, Saltiel AR: PD 98059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem 1995, 270:27489-27494.
15. Favata MF, Horiuchi KY, Manos EJ, Daulerio AJ, Stradley DA, Feeser WS, Van Dyk De, Pitts WJ, Earl RA, Hobbs F et al.: Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem 1998, 273:18623-18632. The first paper describing UO126 as an inhibitor of MKK1.
16. DeSilva DR, Jones EA, Favata MF, Jaffee BD, Magolda RL, Trzaskos JM, Scherle PA: Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy. J Immun 1999, 160:4175-4181. This report demonstrates that UO126 blocks the proliferation of T cells.
17. Meijer L, Borgne A, Mulner O, Chong JPJ, Blow JJ, Inagaki N, Inagaki M, Delcros J-G, Moulinoux J-P: Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem 1997, 243:527-536.
18. Gray NS, Wodicka L, Thunnissen AWH, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L et al.: Exploiting chemical libraries, structure and genomics in the search for kinase inhibitors. Science 1998, 281:533-538. The first description of purvalanol, a potent and specific inhibitor of cyclin-dependent protien kinases.
19. Alessi DR, Cohen P: Mechanism of action and function of protein kinase B. Curr Opin Genet Dev 1998, 8:55-62.
20. Uehata M, Ishizaki T, Satoh H, Ono T, Kawahara T, Morishita T, Tamakawa H, Yamagami K, Inui J, Maekawa M, Narumiya S: Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature 1997, 389:990-994.
21. 2+-sensitization of smooth muscle. FEBS Lett 1998, 440:183-187.
22. Kimura K, Ito M, Amano M, Chihara K, Fukata Y, Nakafuku M, Yamamori B, Feng J, Nakano T, Okawa K et al.: Regulation of myosin phosphatase by Rho and Rho-associated kinase (Rho-kinase). Science 1996, 273:245-248.
23. Sahai E, Ishizaki T, Narumiya S, Treisman R: Transformation mediated by RhoA requires activity of ROCK kinases. Curr Biol 1999, 9:136-145. This paper exploits Y27632 to identify a role for ROCK in cell transformation.
24. Itoh K, Yoshioka K, Akedo H, Uehata M, Ishizaki T, Narumiya S: An essential part for Rho-associated kinase in the transcellular invasion of tumor cells. Nat Med 1999, 5:221-225. This report uses Y27632 to identify a role for ROCK in tumour cell invasion.
25. Niggli V: Rho-kinase in human neutrophils: A role in signalling for myosin light chain phosphorylation and cell migration. FEBS Lett 1999, 445:69-72. Exploitation of Y27632 to identify a role for ROCK in neutrophil chemotaxis.
26. Tominaga T, Barber DL: Na-H exchange acts downstram of RhoA to regulate integrin-induced cell adhesion and spreading. Mol Biol Cell 1998, 9:2287-2303. Identification of an essential role for ROCK in integrin-induced cell spreading through the use of Y27632.
27. Gallagher TF, Seibel GL, Kassis S, Laydon JT, Blumenthal MJ, Lee JC, Lee D, Boehm JC, Fier-Thompson SM, Abt JW et al.: Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase. Bioorg Med Chem 1997, 5:49-64.
28. Lee JC, Laydon JT, McDonnell PC, Gallagher TF, Kumar S, Green D, McNulty D, Blumenthal MJ, Heys JR, Landvatter SW et al.: A protein kinase involved in the regulation of inflammatory cytokine biosynthesis. Nature 1994, 372:739-746.
29. Badger AM, Bradbeer JN, Votta B, Lee JC, Adama JL, Griswold DE: Pharmacological profile of SB 203580, a selective inhibitor of cytokine suppressive binding protein/p38 kinase in animal models of arthritis, bone resorption, endotoxin shock and immune function. J Pharmacol Exp Ther 1996, 279:1453-1461.
30. Cuenda A, Rouse J, Doza YN, Meier R, Cohen P, Gallagher TF, Young PR, Lee JC: SB 203580 is a specific inhibitor of a MAP kinase homologue which is stimulated by cellular stresses and interleukin 1. FEBS Lett 1995, 364:229-233.
31. Cohen P: The search for physiological substrates of MAP and SAP kinases in mammalian cells. Trends Cell Biol 1997, 7:353-361.
32. Thomas G, Hall MM: TOR signalling and the control of cell growth. Curr Opin Cell Biol 1997, 9:782-787.
33. Mohammadi M, McMahon G, Sun L, Tang C, Hirth P, Yen BK, Hubbard SR, Schlessinger J: Structures of the tyrosine kinase domain of fibroblast growth factor receptor in complex with inhibitors. Science 1997, 276:955-960.
34. Tong L, Pav S, White DA, Rogers S, Crane KM, Cywin CL, Brown ML, Pargellis CA: A highly specific inhibitor of p38 MAP kinase binds in the ATP pocket Nat Struct Biol 1997, 4:311-316.
35. Wilson KP, McCaffrey PG, Hsiao K, Pazhanisamy S, Galullo V, Bemis GW, Fitzgibbon MJ, Caron PR, Murcko MA, Su MSS: The structural basis for the specificity of pyridinylimidazole inhibitors of p38 MAP kinase. Chem Biol 1997, 4:423-431.
36. de Azevedo WF, Leclerc S, Meijer L, Havlicek L, Strnad M, Kim SH: Inhibition of cyclin-dependent protein kinases by purine analogues: Crystal structure of human cdk2 complexed with roscovitine. Eur J Biochem 1997, 243:518-526.
37. Eyers PA, Craxton M, Morrice N, Cohen P, Goedert M: Conversion of SB 203580-insensitive MAP kinase family members to drug-sensitive forms by a single amino acid substitution. Chem Biol 1998, 5:321-328. This paper and [38] demonstrate that all MAP kinase family members can be converted from SB 203580-insensitive to SB 203580-sensitive forms by a single amino acid substitution.
38. Gum RJ, McLaughlin MM, Kumar S, Wang Z, Bower MJ, Lee JC, Adams JL, Livi GP, Goldsmith EJ, Young PR: Acquisition of sensitivity of stress-activated protein kinases to the p38 inhibitor, SB 203580, by alteration of one or more amino acids within the ATP-binding pocket J Biol Chem 1998, 273:15605-15610.
39. Borsch-Haubold AG, Pasquet S, Watson SP: Direct inhibition of cyclooxygenase-1 and -2 by the kinase inhibitors SB 203580 and PD 98059. J Biol Chem 1998, 273:28766-28772. This paper shows that SB 203580 inhibits two enzymes that are not protein kinases.
40. Standaert ML, Galloway L, Karnam P, Bandyopadhyay G, Moscat J, Farese RV: Protein kinase Cζ as a downstream effector of phosphatidylinositol 3-kinase during insulin stimulation in rat adipocytes. J Biol Chem 1997, 272:30075-30082.
41. Alessi DR: The protein kinase C inhibitors Ro 318220 and GF 109203X are equally potent inhibitors of MAPKAP kinase 1β (Rsk-2) and p70 S6 kinase. FEBS Lett 1997, 402:121-123.
42. Eyers PA, van den Ussel P, Quinlan R, Goedert M, Cohen P: Use of a drug-resistant mutant of SAPK2a/p38 to validate the in vivo specificity of SB 203580. FEBS Lett 1999, 451:191-196. This paper introduces a novel method for validating the In Vivo Specifities of Protein Kinase Inhibitors That May Be of General Utility.
43. Hoessel R, Leclerc S, Endicott JA, Nobel MEM, Lawrie A, Tunnah P, Leost M, Damiens E, Marie D, Marko D et al.: Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat Cell Biol 1999, 1:60-67. This paper shows that indirubin derivatives are potent inhibitors of CDKs and exhibit anti-proliferative activity leading to G2/M arrest in all cell types examined.
44. Frantz B, Klatt T, Pang M, Parsons J, Rolando A, Williams H, Tocci MJ, O'Keefe SJ, O'Neill EA: The activation state of p38 mitogen-activated protein kinase determines the efficiency of ATP competition for pyridinylimidazole inhibitor binding. Biochemsitry 1998, 37:13846-13853.
45. Sebolt-Leopold JS, Dudley DT, Herrera R, Bacelaere KV, Wiland A, Gowan RC, Tecle H, Barrett SD, Bridges A, Przybranowski S et al.: Blockade of the MAP kinase pathway suppresses growth of colon tumours in vivo. Nat Med 1999, 5:810-816.