Description
Several cyclic nucleotide phosphodiesterases (PDE2, -
5, -
6, -
10, and -
11) contain a tandem of GAF domains in their N-
terminal regulatory region that are thought to mediate cAMP-
or cGMP-
induced stimulation of adenylyl and guanylyl cyclases. Sp-
cyclic AMPS (Sp-
cAMPS) is a derivative of cAMP that binds the PDE10 GAF domain (EC
50 = 40 μM). It has been used to study GAF-
mediated stimulation of PDE10.
References
[1] dostmann w r, taylor s s, genieser h g, et al. probing the cyclic nucleotide binding sites of camp-dependent protein kinases i and ii with analogs of adenosine 3', 5'-cyclic phosphorothioates[j]. journal of biological chemistry, 1990, 265(18): 10484-10491.
[2] hanks s k, quinn a m, hunter t. the protein kinase family: conserved features and deduced phylogeny of the catalytic domains[j]. science, 1988, 241(4861): 42-52.
[3] spicuzza l, belvisi m g, birrell m a, et al. evidence that the anti‐spasmogenic effect of the β‐adrenoceptor agonist, isoprenaline, on guinea‐pig trachealis is not mediated by cyclic amp‐dependent protein kinase[j]. british journal of pharmacology, 2001, 133(8): 1201-1212.
