Selective targeting of phosphodiesterases to develop potent antiparasitic drugs

Regulation of intracellular cyclic nucleotides to avoid homeostatic imbalances is achieved through catabolic activity of phosphodiesterases (PDEs). Recently, Ajiboye et al. reported validation of Cryptosporidium PDE1 (CpPDE1) as a viable drug target and identified optimized pyrazolopyrimidines with...

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Published in:Trends in parasitology 2024-12, Vol.40 (12), p.1075-1076
Main Authors: Khan, Shahbaz M., Mia, Md Mukthar, Witola, William H.
Format: Article
Language:English
Subjects:
Animals
Antiparasitic Agents - pharmacology
Antiparasitic Agents - therapeutic use
Cryptosporidium
Cryptosporidium - drug effects
Cryptosporidium - enzymology
cyclic-nucleotides
drug-target
Humans
phosphodiesterases
Phosphoric Diester Hydrolases - drug effects
Phosphoric Diester Hydrolases - metabolism
pyrazolopyrimidines
selective-inhibition
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creator Khan, Shahbaz M.
Mia, Md Mukthar
Witola, William H.
description Regulation of intracellular cyclic nucleotides to avoid homeostatic imbalances is achieved through catabolic activity of phosphodiesterases (PDEs). Recently, Ajiboye et al. reported validation of Cryptosporidium PDE1 (CpPDE1) as a viable drug target and identified optimized pyrazolopyrimidines with selective activity against CpPDE1 over human PDEs and with potent anticryptosporidial efficacy. Regulation of intracellular cyclic nucleotides to avoid homeostatic imbalances is achieved through catabolic activity of phosphodiesterases (PDEs). Recently, Ajiboye et al. reported validation of Cryptosporidium PDE1 (CpPDE1) as a viable drug target and identified optimized pyrazolopyrimidines with selective activity against CpPDE1 over human PDEs and with potent anticryptosporidial efficacy.
doi_str_mv 10.1016/j.pt.2024.11.001
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subjects Animals
Antiparasitic Agents - pharmacology
Antiparasitic Agents - therapeutic use
Cryptosporidium
Cryptosporidium - drug effects
Cryptosporidium - enzymology
cyclic-nucleotides
drug-target
Humans
phosphodiesterases
Phosphoric Diester Hydrolases - drug effects
Phosphoric Diester Hydrolases - metabolism
pyrazolopyrimidines
selective-inhibition
title Selective targeting of phosphodiesterases to develop potent antiparasitic drugs
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