Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases

doi:10.3389/fphar.2018.01048

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药理学第一研究室

	Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases
	Li, Heng 3,4; Zuo, Jianping1,3 ; Tang, Wei2,3,4
刊名	FRONTIERS IN PHARMACOLOGY
	2018-10-17
卷号	9
关键词	phosphodiesterase-4 psoriasis atopic dermatitis inflammatory airway diseases inflammatory bowel disease roflumilast apremilast crisaborole
ISSN号	1663-9812
DOI	10.3389/fphar.2018.01048
文献子类	Review
英文摘要	Phosphodiesterase-4 (PDE4), mainly present in immune cells, epithelial cells, and brain cells, manifests as an intracellular non-receptor enzyme that modulates inflammation and epithelial integrity. Inhibition of PDE4 is predicted to have diverse effects via the elevation of the level of cyclic adenosine monophosphate (cAMP) and the subsequent regulation of a wide array of genes and proteins. It has been identified that PDE4 is a promising therapeutic target for the treatment of diverse pulmonary, dermatological, and severe neurological diseases. Over the past decades, numerous PDE4 inhibitors have been designed and synthesized, among which roflumilast, apremilast, and crisaborole were approved for the treatment of inflammatory airway diseases, psoriatic arthritis, and atopic dermatitis, respectively. It is regrettable that the dramatic efficacies of a drug are often accompanied by adverse effects, such as nausea, emesis, and gastrointestinal reactions. However, substantial advances have been made to mitigate the adverse effects and obtain better benefit-to-risk ratio. This review highlights the dialectical role of PDE4 in drug discovery and the disquisitive details of certain PDE4 inhibitors to provide an overview of the topics that still need to be addressed in the future.
资助项目	National Science & Technology Major Project Key New Drug Creation and Manufacturing Program, China[2018ZX09711002-006-011]
WOS关键词	OBSTRUCTIVE PULMONARY-DISEASE ; CRISABOROLE TOPICAL OINTMENT ; MODERATE ATOPIC-DERMATITIS ; SELECTIVE PDE4 INHIBITOR ; SEVERE PLAQUE PSORIASIS ; IN-VITRO ; KAPPA-B ; ANTIINFLAMMATORY ACTIVITY ; BEHCETS-SYNDROME ; BETA(2)-ADRENOCEPTOR AGONIST
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	FRONTIERS MEDIA SA
WOS记录号	WOS:000447502000001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279530]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Zuo, Jianping; Tang, Wei
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Lab Immunopharmacol, Shanghai, Peoples R China; 2.Pilot Natl Lab Marine Sci & Technol, Open Studio Druggabil Res Marine Nat Prod, Qingdao, Peoples R China 3.Univ Chinese Acad Sci, Sch Pharm, Beijing, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, Lab Antiinflammat, Shanghai, Peoples R China;
推荐引用方式 GB/T 7714	Li, Heng,Zuo, Jianping,Tang, Wei. Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases[J]. FRONTIERS IN PHARMACOLOGY,2018,9.
APA	Li, Heng,Zuo, Jianping,&Tang, Wei.(2018).Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases.FRONTIERS IN PHARMACOLOGY,9.
MLA	Li, Heng,et al."Phosphodiesterase-4 Inhibitors for the Treatment of Inflammatory Diseases".FRONTIERS IN PHARMACOLOGY 9(2018).