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The next generation of PDE4 inhibitors.
Curr Opin Chem Biol 2001; 5(4):432-8CO

Abstract

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.

Authors+Show Affiliations

Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe Claire, Dorval, Quebec, H9R 4P8, Canada. zheng_huang@merck.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

11470607

Citation

Huang, Z, et al. "The Next Generation of PDE4 Inhibitors." Current Opinion in Chemical Biology, vol. 5, no. 4, 2001, pp. 432-8.
Huang Z, Ducharme Y, Macdonald D, et al. The next generation of PDE4 inhibitors. Curr Opin Chem Biol. 2001;5(4):432-8.
Huang, Z., Ducharme, Y., Macdonald, D., & Robichaud, A. (2001). The next generation of PDE4 inhibitors. Current Opinion in Chemical Biology, 5(4), pp. 432-8.
Huang Z, et al. The Next Generation of PDE4 Inhibitors. Curr Opin Chem Biol. 2001;5(4):432-8. PubMed PMID: 11470607.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The next generation of PDE4 inhibitors. AU - Huang,Z, AU - Ducharme,Y, AU - Macdonald,D, AU - Robichaud,A, PY - 2001/7/27/pubmed PY - 2001/9/21/medline PY - 2001/7/27/entrez SP - 432 EP - 8 JF - Current opinion in chemical biology JO - Curr Opin Chem Biol VL - 5 IS - 4 N2 - 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. SN - 1367-5931 UR - https://www.unboundmedicine.com/medline/citation/11470607/The_next_generation_of_PDE4_inhibitors_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S1367-5931(00)00224-6 DB - PRIME DP - Unbound Medicine ER -