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Rational Design of 2-Chloroadenine Derivatives as Highly Selective Phosphodiesterase 8A Inhibitors.

Huang Y, Wu XN, Zhou Q, Wu Y, Zheng D, Li Z, Guo L, Luo HB
J Med Chem 63 15852-15863 (2020)
Related entries: 7cwa, 7cwf

Cited: 3 times
EuropePMC logo PMID: 33291877

Abstract

To validate the hypothesis that Tyr748 is a crucial residue to aid the discovery of highly selective phosphodiesterase 8A (PDE8A) inhibitors, we identified a series of 2-chloroadenine derivatives based on the hit clofarabine. Structure-based design targeting Tyr748 in PDE8 resulted in the lead compound

Reviews citing this publication (1)

  1. The Role of PDE8 in T Cell Recruitment and Function in Inflammation. Epstein PM, Basole C, Brocke S. Front Cell Dev Biol 9 636778 (2021)

Articles citing this publication (2)

  1. Structure-based discovery of orally efficient inhibitors via unique interactions with H-pocket of PDE8 for the treatment of vascular dementia. Wu XN, Zhou Q, Huang YD, Xie X, Li Z, Wu Y, Luo HB. Acta Pharm Sin B 12 3103-3112 (2022)
  2. Discovery of novel phosphodiesterase-1 inhibitors for curing vascular dementia: Suppression of neuroinflammation by blocking NF-κB transcription regulation and activating cAMP/CREB axis. Zhou Q, Le M, Yang Y, Wang W, Huang Y, Wang Q, Tian Y, Jiang M, Rao Y, Luo HB, Wu Y. Acta Pharm Sin B 13 1180-1191 (2023)


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