International Journal of Impotence Research

TABLE 1

FROM:

Phosphodiesterase 11: a brief review of structure, expression and function

A Makhlouf, A Kshirsagar and C Niederberger

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Table 1. Summary of PDE family characteristics1, 7, 8, 9

Figure and tables index
PDE
family 		Genes
(if multigene) 		Substrate Inhibitors, Ki or (IC 50) Regulation Tissue expression
 1PDE1AcAMP>cGMPVinpocetine (14 mu M) (+)Ca2+/CAM1A: Thyroid, testis, brain
 PDE1BcAMP>cGMPZaprinast (6 mu M)(-)PKA, CamKII1B: Brain, lymphocytes
 PDE1CcAMP=cGMPSildenafil (0.35 mu M) 1C: Blood vessels, testis
      
 2 cGMPgreater than or equal tocAMPEHNA (1 mu M) (+)cGMP, PKCBrain, heart, platelets, liver, thymocytes
   Bay 60-7550 (0.047 mu M)(+/-)N-terminal-targeting domain 
      
 3PDE3AcAMP>cGMPCilostamide (0.020 mu M) (+)PKA, PKB3A: Heart, blood vessels
 PDE3B Milrinone (0.150 mu M) (-)cGMP3B: Adipocytes, hepatocytes, lymphocytes
   Zardaverine (0.5–2 mu M)(+/-)N-terminal-targeting domain 
      
 4PDE4AcAMPRolipram (1 mu M) (+)PKA, ERK, phosphatidic acid4A: Lung, immune cells, brain, blood vessels
 PDE4B Roflumilast (0.8 nM)(-)ERK, caspases 
 PDE4C Cilomilast (120 nM)(+/-)N-terminal-targeting domains 
 PDE4D Zardaverine (0.8–4 mu M)  
      
 5 cGMPZaprinast (0.130 mu M) (+)cGMP, PKG, PKASmooth muscle, platelets, Purkinje cells, gastro-intestinal epithelium, pulmonary endothelium
   Sildenafil (0.10 mu M) (-)Caspases 
   Vardenafil (0.001 mu M)   
   Tadalafil (0.010 mu M)   
      
 6PDE6AcGMPZaprinast (0.400 mu M) (+)TransducinRetinal photoreceptors
 PDE6B Dipyridamole (0.125 mu M) (-)cGMP, gamma and delta subunits 
 PDE6C Sildenafil (0.050 mu M)   
   Vardenafil (0.011 mu M)  
   Tadalafil (2 mu M)  
      
 7PDE7AcAMPIBMX (4 mu M) (+/-)PKABrain, lymphocytes, kidney
 PDE7B Dipyridamole (0.6 mu M)   
      
 8PDE8AcAMPDipyridamole (9 mu M) PAS domainThyroid
 PDE8B    
      
 9 cGMPZaprinast (35 mu M) UnknownKidney
      
10 cGMP>cAMPDipyridamole (1 mu M) (-)cAMPTestis, brain
   Zaprinast (22 mu M)  
      
11 cAMP and cGMPZaprinast (12 mu M) UnknownSkeletal muscle, prostate, testis, corpus cavernosum, heart (but see text and Table 3)
   Dipyridamole (0.4 mu M)   

 CAM=calmodulin c; ERK=extracellular signal-regulated protein kinase; PAS=periodic acid-Schiff stain; PDE=phosphodiesterase; PKA=protein kinase A; PKC=protein kinase A; PKG=protein kinase G.

 Only some of the most commonly reported inhibitors for each PDE are listed. Tissue expression is representative of most reports and is not necessarily exhaustive.

Figure and tables index
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