Probing the Catalytic Sites and Activation Mechanism of Photoreceptor Phosphodiesterase Using Radiolabeled Phosphodiesterase Inhibitors
نویسندگان
چکیده
منابع مشابه
Regulation of photoreceptor phosphodiesterase catalysis by its non-catalytic cGMP-binding sites.
The photoreceptor 3':5'-cyclic nucleotide phosphodiesterase (PDE) is the central enzyme of visual excitation in rod photoreceptors. The hydrolytic activity of PDE is precisely regulated by its inhibitory gamma subunit (Pgamma), which binds directly to the catalytic site. We examined the inhibition of frog rod outer segment PDE by endogenous Pgamma, as well as by synthetic peptides corresponding...
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The phosphodiesterases (PDEs) are metal ion-dependent enzymes that regulate cellular signaling by metabolic inactivation of the ubiquitous second messengers cAMP and cGMP. In this role, the PDEs are involved in many biological and metabolic processes and are proven targets of successful drugs for the treatments of a wide range of diseases. However, because of the rapidity of the hydrolysis reac...
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Correspondence: *Inserm U408, Unité de Pneumologie de l'Hôpital Bichat, Paris, France. ** and Dept of Thoracic Medicine, National Heart and Lung Institute, London, UK. This issue of the European Respiratory Journal starts a series of short reviews based on a Satellite Meeting held during the European Respiratory Society Annual Meeting in Nice in October 1994. The symposium was supported by Byk ...
متن کاملStructural features of the noncatalytic cGMP binding sites of frog photoreceptor phosphodiesterase using cGMP analogs.
The cGMP-specific phosphodiesterase (PDE) of retinal photoreceptors is a central regulatory enzyme in the visual transduction pathway of vertebrate vision. Although the mechanism of activation of PDE by transducin is well understood, the role of the noncatalytic cGMP binding sites located on the catalytic subunits of PDE remains obscure. We report here for the first time the molecular basis of ...
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OBJECTIVE To compare the direct pulmonary vasodilating activity and specificity of phosphodiesterase-5 (zaprinast) and phosphodiesterase-3 (milrinone) inhibitors on the pulmonary vascular (PV) bed of the spontaneously breathing cat with an intact chest. DESIGN Prospective, randomized animal study. SETTING Laboratory of university hospital. SUBJECTS Experiments were performed in vivo in in...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 2009
ISSN: 0021-9258
DOI: 10.1074/jbc.m109.018606