PDE

PDEδ was originally identified as a fourth subunit of rod-specific cGMP PDE. PDEδ is thought to be a specific soluble transport factor for certain prenylated (farnesyl) proteins and Arl2-GTP, a regulator of PDE-mediated transport. PDEδ sustains the spatial organization of KRAS by facilitating its diffusion in the cytoplasm. Conversely, PDEδ down-modulation randomizes RAS distributions to all membranes in the cell and suppresses regulated signaling through wild-type RAS and also constitutive oncogenic RAS signaling in cancer cells[1],[2].

Phosphodiesterases (PDE; EC 3.1.4.-) 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[3]. 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[4].

Phosphodiesterases listed: PDEPLCPLD


[1] A. Chandra et al. TheGDI-like solubilizing factor PDEδ sustains the spatial organization and signalling of Ras family proteins. Nat. Cell Biol. 2011, 14, 148-158.
[2] G. Zimmermann et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013, 497, 638-642. 
[3] G. Bolger. Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. B. Cell. Signal. 1994, 6,  851–859.
[4] Y. H. Jeon et al. Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. Cell. Mol. Life Sci. Vol. 2005, 62, 1198. 

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2284 Deltarasin trihydrochloride Inhibitor of the prenyl binding protein PDEδ and the KRAS–PDEδ interaction. €125.00

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