The next generation of PDE4 inhibitors
A number of highly potent PDE4 inhibitors are being developed for the treatment of asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis and Crohn's disease. Cilomilast (Ariflo ™, SB 207499, SmithKline Beecham), the most advanced member of the class in Phase II...
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| Veröffentlicht in: | Current Opinion in Chemical Biology 2001-08, Vol.5 (4), p.432-438 |
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| container_end_page | 438 |
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| container_issue | 4 |
| container_start_page | 432 |
| container_title | Current Opinion in Chemical Biology |
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| creator | Huang, Zheng Ducharme, Yves Macdonald, Dwight Robichaud, Annette |
| description | A number of highly potent PDE4 inhibitors are being developed for the treatment of asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, multiple sclerosis and Crohn's disease. Cilomilast (Ariflo
™, SB 207499, SmithKline Beecham), the most advanced member of the class in Phase III clinical trials, was reported to have a limited therapeutic window. Other inhibitors with improved profiles in preclinical models are entering into (or are in) clinical trials. The recent developments in understanding PDE4 catalysis, inhibitor binding and their emetic response should facilitate the design of the next generation of PDE4 inhibitors. |
| doi_str_mv | 10.1016/S1367-5931(00)00224-6 |
| format | Article |
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| ispartof | Current Opinion in Chemical Biology, 2001-08, Vol.5 (4), p.432-438 |
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| source | Elsevier ScienceDirect Journals Complete - AutoHoldings; MEDLINE |
| subjects | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors Antiemetics - pharmacology asthma CAMP cancer Catalysis COPD Cyclic Nucleotide Phosphodiesterases, Type 4 Cyclohexanecarboxylic Acids - pharmacology Cyclohexanecarboxylic Acids - therapeutic use emesis HIV Humans multiple sclerosis Nitriles PDE4 Phosphodiesterase Inhibitors - pharmacology Phosphodiesterase Inhibitors - therapeutic use rheumatoid arthritis |
| title | The next generation of PDE4 inhibitors |
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