CDP840: A Novel Inhibitor of PDE-4

Cell Biochemistry and Biophysics

Volumn 29, Issue 1-2, 1998, Pages 113-132

  Perry, M J ^a   O'Connell, J ^a   Walker, C ^a   Crabbe, T ^a   Baldock, D ^a   Russell, A ^a   Lumb, S ^a   Huang, Z ^b   Howat, D ^a   Allen, R ^a   Merriman, M ^a   Walls, J ^a   Daniel, T ^a   Hughes, B ^a   Laliberte, F ^b   Higgs, G A ^a   Owens, R J ^a  

^a UCB PHARMA   (Belgium)

^b MERCK FROSST CENTRE FOR THERAPEUTIC RESEARCH   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

2 PYRROLIDONE DERIVATIVE; 3',5' CYCLIC NUCLEOTIDE PHOSPHODIESTERASE; 4 [2 [3 (CYCLOPENTYLOXY) 4 METHOXYPHENYL] 2 PHENYLETHYL]PYRIDINE; CYCLIC AMP; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE IV; PYRIDINE DERIVATIVE; ROLIPRAM; TRITIUM;

ANIMAL; ARTICLE; BINDING COMPETITION; BIOSYNTHESIS; BRAIN; CATALYSIS; CHEMISTRY; COMPARATIVE STUDY; DRUG ANTAGONISM; DRUG EFFECT; ENZYMOLOGY; GENETICS; GUINEA PIG; HUMAN; MALE; METABOLISM; MOUSE; PROTEIN BINDING;

3',5'-CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE; ANIMALS; BINDING, COMPETITIVE; BRAIN; CATALYSIS; CYCLIC AMP; GUINEA PIGS; HUMANS; MALE; MICE; PHOSPHODIESTERASE INHIBITORS; PROTEIN BINDING; PYRIDINES; PYRROLIDINONES; ROLIPRAM; TRITIUM;

EID: 0031616075     PISSN: 10859195     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF02737831     Document Type: Article

References (34)

1. Palfreyman, M. N. and Souness, J. E. (1996) Phosphodiesterase type IV inhibitors. Prog. Med. Chem. 33, 1-52.
2. Torphy, T. J., Livi, G., and Christensen, S. (1993) Novel phosphodiesterase inhibitors for the therapy of asthma. Drug News Perspect. 6, 203-214.
3. Torphy, T. J. and Undem, B. J. (1991) Phosphodiesterase inhibitors new opportunities for the treatment of asthma. Thorax. 46, 512-523.
4. Saletu, B. (1992) EEG mapping and psychopharmacology with denbufylline in SDAT and MID. Biol. Psychiatry 32, 668-681.
5. Brunne, T., Engelstatter, R., Steinijans, V. W., and Kunkel, G. (1992) Bronchodilator effects of inhaled Zardaverine, a phosphodiesterase 3 and 4 inhibitor in patients with asthma. Eur. Respir. J. 5, 982-985.
6. Hebenstrieb, G. H. (1989) Rolipram in major depressive disorders results of a double blind comparative study with imipramine. Pharmacol. Psychiatr. 22, 156-160.
7. Swinnen, J. V., Joseph D. R., and Conti, M. (1989) Molecular cloning of rat homologues of the Urosophilia melanogaster dunce cAMP phosphodiesterase. Proc. Natl. Acad. Sci. USA 86, 5325-5329.
8. Bolger, G., Michaeli, T., Martins, T., St John, T., Steiner, B., Rodgers, L. Riggs, M., and Ferguson, K. (1993) A family of human phosphodiesterases homologous to the dunce learning and memory gene product of Drosophila melanogaster are potential targets for antidepressant drugs. Mol Cell Biol. 13, 6558-6571.
9. Hughes, B., Owens, R. J., Perry, M. J., Warrellow, G., and Allen, R. (1997) PDE 4 inhibitors: the use of molecular cloning in the design and development of novel drugs. Drug Disc. Today 2, 89-101.
10. Huston, E., Pooley, L. Julien, P., Scotland, G., McPhee, I., Sullivan, M., Bolger, G., and Houslay, M. D. (1996) The human cyclic AMP-specific phosphodiesterase PDE 46 (HSPDE4A4B) expressed in transfected COS7 cells occurs as both particulate and cytosolic species that exhibit distinct kinetics of inhibition by the anti-depressant rolipram. J. Biol. Chem. 271, 31,334-31,344.
11. O'Connell, J. C., McCallum, J. F., McPhee, I., Wakefield, J., Houslay, E. S., Wishart, W., Bolger, G., Frames, M., and Houslay, M. D. (1996) The SH3 domain of SRC tyrosyl protein kinase interacts with the N-terminal splice region of the PDE 4A cAMP-specific phosphodiesterase RPDE-6 (RNPDE 45). Biochem. J. 318, 255-262.
12. Alvarez, R., Sette, C., Yang., D., Eglen, R. M., Wilhelm, R., Shelton, E. R., and Conti, M. (1995) Activation and selective inhibition of a cyclic AMP-specific phosphodiesterase, PDE 4D3. Mol. Pharm. 48, 616-622.
13. Sette, C. and Conti, M. (1996) Phosphorylation and activation of a cAMP-specific phosphodiesterase by the cAMP-dependent protein kinase. Involvement of serine 54 in the enzyme activation. J. Biol. Chem. 271, 16,526-16,534.
14. Torphy, T. J., Stadel, J. M., Burman, M., Cieslinski, L. B., McLaughlin, M. M., White, J. R., and Livi, G. P. (1992) Co-expression of human cAMP-specific phosphodiesterase activity and high affinity rolipram binding in yeast. J. Biol. Chem. 267, 1798-1804.
15. McLaughlin, M., Cieslinski, L., Burman, M., Torphy, T., and Livi, G. P. (1993) A low-Km rolipram-sensitive, cAMP-specific phosphodiesterase from human brain. J. Biol. Chem. 268, 6470-6476.
16. Schneider, H. H., Schmiechen, R., Brezinski, M., and Seidler, J. (1986) Stereospecific binding of the anti-depressant rolipram to brain protein structures. Eur. J. Pharm. 127, 105-115.
17. Souness, J. E., Griffin, M., Maslen, C., Ebsworth, K., Scott, L. C., Pollock, K., Palfreyman, M. N., and Karlsson, J. A. (1996) Evidence that cyclic AMP phosphodiesterase inhibitors suppress TNF-alpha generation from human monocytes by interacting with a low-affinity phosphodiesterase 4 conformer. Br. J. Pharm. 118, 649-658.
18. Barnette, M. S., Bartus, J. O. L., Burman, M., Christensen, S. B., Cieslinski, L. B., Esser, K. M., Prabhakar, V. S., Rush, J. A., and Torphy, T. J. (1996) Association of the anti-inflammatory activity of phosphodiesterase 4 (PDE 4) inhibitors with either inhibition of PDE 4 catalytic activity or competition for [H-3] rolipram binding. Bioch. Pharm. 51, 949-956.
19. Cohan, V. L., Showell, H. J., Fisher, D. A., Pazoles, C. J., Watson, J. W., Turner, C. R., and Cheng, J. B. (1996) In vitro pharmacology of the novel phosphodiesterase type 4 inhibitor CP-80633. J. Pharm. Exp. Ther. 278, 1356-1361.
20. Harbinson, P. L., MacLeod, D., Hawksworth, R., O'Toole, S., Sullivan, P. J., Heath P., Kilfeather, S., Page, C. P., Costello, J., Holgate, S. T., and Lee, T. H. (1997) The effect of a novel orally active selective PDE4 isoenzyme inhibitor (CDP840) on allergen-induced responses in asthmatic subjects. Eur. Respir. J. 10, 1008-1014.
21. Owens, R. J., Catterall, C., Batty, D., Jappy, J., Russell, A., Smith, B. J., O'Connell, J., and Perry, M. J. (1997) Human phosphodiesterase 4A; characterization of full-length and truncated enzymes expressed in COS cells. Biochem. J., in press.
22. Owens, R. J., Lumb, S., Rees-Milton, K., Russell, A., Baldock, D., Lang, V., Crabbe, T., Ballesterso, M., and Perry, M. J. (1997) Molecular cloning and expression of a human phosphodiesterase 4C. Cell. Signalling, in press.
23. Bolger, G. (1994) Molecular biology of the cAMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. Cell. Signalling, 6, 851-859.
24. Summers, M. D. and Smith, G. E. (1987) A manual of methods for baculovirus vectors and insect culture procedures. Texas Agricultural Experiment Station Bulletin no. 1555.
25. Hughes, B., Howat, D., Lisle, H., Holbrook, M., James, T., Gozzard, N., Blease, K., Hughes, P., Kingaby, R., Warrellow, G., Alexander, R., Head, J., Boyd, E., Eaton, M., Perry, M., Wales, M., Smith, B., Owens, R., Catterall, C., Lumb, S., Russell, A., Allen, R., Merriman, M., Bloxham, D., and Higgs, G. (1996) The inhibition of antigen-induced eosinophilia and bronchoconstriction by CDP840, a novel stereo-selective inhibitor of phosphodiesterase type 4. Br. J. Pharmacol. 118(5), 1183-1191.
26. Smith, B. J., Wales, M. R., Jappy, J. W. G., and Perry, M. J. (1993) A phosphodiesterase assay using Alumina Microcolumns. Anal. Biochem. 214, 335-357.
27. Kroegel, C., Giembycz, M. A., and Barnes, P. J. (1990) Characterisation of eosinophil cell activation by peptides. J. of Immunol. 145, 2581-2587.
28. Schmiechen, R., Schneider, H. H., and Wachtel, H. (1990) Close correlation between behavioural response and binding in vivo for inhibitors of the rolipram-sensitive phosphodiesterase. Psychopharmacol. 102, 17-20.
29. Dixon, M. (1953) The determination of enzyme inhibitor constants. Biochem. J. 55, 170-175.
30. Souness, J. E., Maslen, C., Webber, S., Foster, M., Raeburn, D., Palfreyman, M. N., Ashton, M. J., and Karlsson, J. A. (1995) Suppression of eosinophil function by RP73401, a potent and selective inhibitor of cyclic AMP-specific phosphodiesterase. Br. J. Pharmacol. 115, 39-46.
31. Kovala, T., Sanwal, B. D., and Ball, E. C. (1997) Recombinant expression of a Type IV cAMP-Specific Phosphodiesterase: Characterisation and Structure-function Studies of Deletion Mutants. Biochemistry 36, 2968-2976.
32. Wilson, M., Sullivan, M., Brown, N., and Houslay, M. D. (1994) Purification, characterization and analysis of rolipram inhibition of a human type-IVA cyclic AMP-specific phosphodiesterase expressed in yeast. Biochem. J. 304, 407-415.
33. Holbrook, M., Gozzard, N., James, T., Higgs, G., and Hughes, B. (1996) Inhibition of bronchospasm and ozone-induced airway hyperresponsiveness in the guinea-pig by CDP840, a novel phosphodiesterase type 4 inhibitor. Br. J. Pharmacol. 118(5), 1192-1200.
34. Gozzard, N., Elhashim, A., Herd, C. M., Blake, S. M., Holbrook, M., Hughes, B., Higgs, G. A., and Page, C. P. (1996) Effect of the glucocorticosteroid budesonide and a novel phosphodiesterase type 4 inhibitor, CDP840, on antigen-induced airway responses in neonatally immunised rabbits. Br. J. Pharmacol. 118(5), 1201-1208.