2. Academic Validation
  3. Advances in the Development of Phosphodiesterase-4 Inhibitors

Advances in the Development of Phosphodiesterase-4 Inhibitors

  • J Med Chem. 2020 Oct 8;63(19):10594-10617. doi: 10.1021/acs.jmedchem.9b02170.
Ting Peng 1,  Baowen Qi 2,  Jun He 3,  Hengming Ke 4,  Jianyou Shi 1
Affiliations

Affiliations

  • 1 Personalized Drug Therapy Key Laboratory of Sichuan Province, Sichuan Academy of Medical Science & Sichuan Provincial People's Hospital, School of Medicine of University of Electronic Science and Technology of China, Chengdu 610072, China.
  • 2 Center for Nanomedicine and Department of Anesthesiology, Brigham and Women's Hospital, Harvard Medical School, Boston, Massachusetts 02115, United States.
  • 3 Cancer Center, Collaborative Innovation Center for Biotherapy, West China Hospital, Sichuan University, Sichuan 610041, China.
  • 4 Department of Biochemistry and Biophysics, and Lineberger Comprehensive Cancer Center, University of North Carolina, Chapel Hill, North Carolina 27599, United States.
PMID: 32255344 DOI: 10.1021/acs.jmedchem.9b02170
Abstract

Cyclic nucleotide phosphodiesterase 4 (PDE4) specifically hydrolyzes cyclic adenosine monophosphate (cAMP) and plays vital roles in biological processes such as Cancer development. To date, PDE4 inhibitors have been widely studied as therapeutics for the treatment of various diseases such as chronic obstructive pulmonary disease, and many of them have progressed to clinical trials or have been approved as drugs. Herein, we review the advances in the development of PDE4 inhibitors in the past decade and will focus on their pharmacophores, PDE4 subfamily selectivity, and therapeutic potential. Hopefully, this analysis will lead to a strategy for development of novel therapeutics targeting PDE4.

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