Proteomics

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Charting the interactome of PDE3A in human cells using an IBMX based chemical proteomics approach


ABSTRACT: We attempt to study the interactome of PDEs by synthesizing a broad spectrum PDE-capturing resin based on the non-selective PDE inhibitor 3-isobutyl-1-methylxanthine (IBMX). Chemical proteomics characterization of this resin in HeLa cell lysates led to the capture of several different PDEs. Combining the IBMX-resin with in-solution competition with other available, more selective PDE inhibitors, namely cilostamide and papaverine, allowed us to selectively probe the interactome of PDE3A in HeLa cells.

INSTRUMENT(S): TripleTOF 5600, LTQ Orbitrap Elite, Q Exactive

ORGANISM(S): Homo Sapiens (human)

TISSUE(S): Cell Culture

SUBMITTER: Eleonora Corradini  

LAB HEAD: Albert J.R. Heck

PROVIDER: PXD001781 | Pride | 2016-05-25

REPOSITORIES: Pride

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Charting the interactome of PDE3A in human cells using an IBMX based chemical proteomics approach.

Corradini Eleonora E   Klaasse Gruson G   Leurs Ulrike U   Heck Albert J R AJ   Martin Nathaniel I NI   Scholten Arjen A  

Molecular bioSystems 20151001 10


In the cell the second messenger cyclic nucleotides cAMP and cGMP mediate a wide variety of external signals. Both signaling molecules are degraded by the superfamily of phosphodiesterases (PDEs) consisting of more than 50 different isoforms. Several of these PDEs are implicated in disease processes inspiring the quest for and synthesis of selective PDE inhibitors, that unfortunately have led to very mixed successes in clinical trials. This may be partially caused by their pharmacological action  ...[more]

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