Esterases (Phosphodi-)
No less than eleven sub-types of the enzyme family of phosphodiesterases (PDE; EC 3.1.4.-) are known to date, many of which exist as splice variants[1]. They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. Roughly, the sub-types can be divided into 3 groups: one group of enzymes specifically degrades cyclic adenosine monophosphate (cAMP; PDE4, 7 and 8), another group specifically targets cyclic guanosine monophosphate (cGMP; PDE5, 6, and 9), whereas the third group of enzymes (including PDE1, 2, 3, 10, and 11) are non specific towards either cAMP or cGMP. PDEs influence a vast array of pharmacological processes, including pro-inflammatory mediator production and action, ion channel function, muscle contraction, learning, differentiation, apoptosis, lipogenesis, glycogenolysis and gluconeogenesis. Recent advances in molecular pharmacology of PDE isoenzymes resulted in identification of new potential applications of PDE inhibitors in various therapeutic areas, including dementia, depression and schizophrenia[2].
[1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. Bolger G. B. Cell. Signal. 1994, 6, 851–859.
[2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. Y. H. Jeon,Y. -S. Heo, C. M. Kim,Y. -L. Hyun, T. G. Lee, S. Ro and J. M. Cho. Cell. Mol. Life Sci. Vol. 2005, 62, 1198.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
1957 | Apremilast | PDE4 inhibitor | €105.00 | |
1178 | BAY 19-8004 | PDE4 inhibitor | €135.00 | |
2281 | FIPI hydrochloride | Phospholipase D (PLD) inhibitor that blocks phosphatidic acid (PA) production in vivo | €100.00 | |
2218 | Gisadenafil besylate | Potent and selective inhibitor of PDE5 | €105.00 | |
1127 | L 454560 | PDE4 inhibitor | €165.00 | |
1168 | Olprinone hydrochloride | PDE3 inhibitor | €119.00 | |
1482 | Parogrelil | PDE3 inhibitor | €125.00 | |
1709 | PDE5 inhibitor 42 | PDE5 inhibitor | €125.00 | |
2825 | PDE9A inhibitor C33(S) | Potent and selective PDE9A inhibitor | €135.00 | |
2148 | PF 04447943 | Selective, brain penetrant PDE9A inhibitor | €105.00 | |
1911 | RAD51 inhibitor B02 | Inhibitor of RAD51 | €95.00 | |
1885 | RI-1 | Inhibitor of the central recombination protein RAD51 | €95.00 | |
2352 | Roflumilast | First specific PDE4 inhibitor licensed for treatment of COPD | €90.00 | |
1212 | Rolipram | PDE4 inhibitor | €65.00 | |
1229 | Rolipram, (R)-(-)- | PDE4 inhibitor | €110.00 |