Discovery of evodiamine derivatives as highly selective PDE5 inhibitors targeting a unique allosteric pocket
T Zhang, Z Lai, S Yuan, YY Huang… - Journal of medicinal …, 2020 - ACS Publications
Clinical use of phosphodiesterase-5 (PDE5) inhibitors is limited by several side effects due
to weak isoform selectivity. Herein, a unique allosteric pocket of PDE5 is identified by …
to weak isoform selectivity. Herein, a unique allosteric pocket of PDE5 is identified by …
Use of structure based design to increase selectivity of pyridyl-cinnoline phosphodiesterase 10A (PDE10A) inhibitors against phosphodiesterase 3 (PDE3)
E Hu, RK Kunz, S Rumfelt, KL Andrews, C Li… - Bioorganic & medicinal …, 2012 - Elsevier
We report our successful effort to increase the PDE3 selectivity of PDE10A inhibitor pyridyl
cinnoline 1 using a combination of computational modeling and structural–activity …
cinnoline 1 using a combination of computational modeling and structural–activity …
Drug repurposing and structure-based discovery of new PDE4 and PDE5 inhibitors
J Liu, X Zhang, G Chen, Q Shao, Y Zou, Z Li… - European Journal of …, 2023 - Elsevier
Abstract Phosphodiesterase-4 (PDE4) and PDE5 responsible for the hydrolysis of
intracellular cAMP and cGMP, respectively, are promising targets for therapeutic intervention …
intracellular cAMP and cGMP, respectively, are promising targets for therapeutic intervention …
[HTML][HTML] Phosphodiesterase 5 (PDE5): Structure-function regulation and therapeutic applications of inhibitors
Abstract Phosphodiesterase 5 (PDE5) is one of the most well-studied phosphodiesterases
(PDEs) that specifically targets cGMP typically generated by nitric oxide (NO)-mediated …
(PDEs) that specifically targets cGMP typically generated by nitric oxide (NO)-mediated …
[HTML][HTML] PDE4 inhibitors: Profiling hits through the multitude of structural classes
J Jin, F Mazzacuva, L Crocetti, MP Giovannoni… - International Journal of …, 2023 - mdpi.com
Cyclic nucleotide phosphodiesterases 4 (PDE4) are a family of enzymes which specifically
promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been …
promote the hydrolysis and degradation of cAMP. The inhibition of PDE4 enzymes has been …
Rational design of 2-chloroadenine derivatives as highly selective phosphodiesterase 8A inhibitors
Y Huang, XN Wu, Q Zhou, Y Wu, D Zheng… - Journal of Medicinal …, 2020 - ACS Publications
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 …
selective phosphodiesterase 8A (PDE8A) inhibitors, we identified a series of 2 …
The molecular biology of phosphodiesterase 4 enzymes as pharmacological targets: an interplay of isoforms, conformational states, and inhibitors
The phosphodiesterase 4 (PDE4) enzyme family plays a pivotal role in regulating levels of
the second messenger cAMP. Consequently, PDE4 inhibitors have been investigated as a …
the second messenger cAMP. Consequently, PDE4 inhibitors have been investigated as a …
[HTML][HTML] Advancements in phosphodiesterase 5 inhibitors: unveiling present and future perspectives
Phosphodiesterase 5 (PDE5) inhibitors presented themselves as important players in the
nitric oxide/cGMP pathway, thus exerting a profound impact on various physiological and …
nitric oxide/cGMP pathway, thus exerting a profound impact on various physiological and …
The discovery of novel, potent and selective PDE5 inhibitors
Y Bi, P Stoy, L Adam, B He, J Krupinski… - Bioorganic & medicinal …, 2001 - Elsevier
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Insight into binding of phosphodiesterase-9A selective inhibitors by crystal structures and mutagenesis
H Wang, X Luo, M Ye, J Hou… - Journal of medicinal …, 2010 - ACS Publications
PDE9 inhibitors have been studied as therapeutics for treatment of cardiovascular diseases,
diabetes, and neurodegenerative disorders. To illustrate the inhibitor selectivity, the crystal …
diabetes, and neurodegenerative disorders. To illustrate the inhibitor selectivity, the crystal …