Phosphodiesterases
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
- ↑ Swiss Institute of Bioinformatics (SIB): PROSITE documentation PDOC00116. Retrieved September 20, 2011 .
- ^ V Boswell-Smith, D Spina, C. Page: Phosphodiesterase inhibitors. In: Br J Pharmacol . , 147 (Suppl 1), 2006, pp. S252-257, PMID 16402111 .
- ↑ 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 .