Phosphodiesterases

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Phosphodiesterases
Identifier
Gene name (s) PDE
Enzyme classification
EC, category 3.1.4.17 esterase
Response type Hydrolase
Substrate cAMP, cGMP, cdAMP, cIMP, cCMP
Occurrence
Parent taxon Vertebrates

Phosphodiesterases (PDE), more precisely 3 ', 5'-cyclonucleotide phosphodiesterases , are a group of enzymes in vertebrates that break down the second messenger cAMP and cGMP to AMP and GMP . A distinction is made between eleven isoenzymes which are localized differently in the tissues of the human organism. Phosphodiesterases can be inhibited non-specifically or specifically (a certain enzyme) by various drugs, so-called phosphodiesterase inhibitors . A widely used, non-selective phosphodiesterase inhibitor is caffeine .

Phosphodiesterase Isoenzymes

Isoenzymes Number of isoforms Substrate tissue Specific inhibitors
Type 1 8th Calcium and calmodulin stimulated Heart, brain, lungs, smooth muscles KS-505a
Type 2 - cGMP stimulated Adrenal gland, heart, lungs, liver, platelets; involved in learning and memory processes Erythro-9- (2-hydroxy-3-nonyl) adenine
Type 3 4th cGMP-inhibited, cAMP-selective Heart, smooth muscles of blood vessels, lungs, liver, platelets, adipose tissue, leukocytes Cilostamid, enoximon, milrinon , siguazodan
Type 4 20th cAMP-specific Lungs, testes, kidneys, brain, liver, leukocytes Rolipram , roflumilast , daxalipram
Type 5 3 cGMP specific smooth muscles of the blood vessels of the erectile tissue of the penis, lungs, platelets Sildenafil , Tadalafil , Vardenafil
Type 6 - cGMP specific PR of the eye Dipyridamole
Type 7 3 cAMP-specific, high affinity Skeletal muscles, heart, kidney, brain, pancreas, lymphocytes BRL-50481
Type 8 - cAMP-specific Testicles, eyes, liver, skeletal muscles, heart, kidneys, ovaries, brain, lymphocytes no specific inhibitor known
Type 9 4th cGMP specific Kidney, liver, lungs, brain BAY 73-6691
Type 10 2 cGMP sensitive, cAMP selective Testicles, brain no specific inhibitor known
Type 11 4th cGMP sensitive, dual specificity Skeletal muscles, prostate, kidney, liver, pituitary gland, salivary glands, testes no specific inhibitor known

literature

  • Siegel, Agranoff, Fisher: Basic Neurochemistry Molecular, Cellular and Medical Aspects . Sixth Edition. American Society for Neurochemistry, 1999

Individual evidence

  1. Swiss Institute of Bioinformatics (SIB): PROSITE documentation PDOC00116. Retrieved September 20, 2011 .
  2. ^ V Boswell-Smith, D Spina, C. Page: Phosphodiesterase inhibitors. In: Br J Pharmacol . , 147 (Suppl 1), 2006, pp. S252-257, PMID 16402111 .
  3. J. Tesarik, C. Mendoza, A. Carreras: Effects of phosphodiesterase inhibitors caffeine and pentoxifylline on spontaneous and stimulus-induced acrosome reactions in human sperm. In: Fertility and Sterility , Vol. 58, No. 6, 1992, pp. 1185-1190, PMID 1333994 .