Non disponible en dehors du Royaume-Uni et de l'Irlande

Application

Useful for the study of enzyme kinetics, screening inhibitors, and selectivity profiling.

Biochem/physiol Actions

PDE8 (phosphodiesterase 8) are cAMP-specific enzymes, and they play a role in various processes such as in T-cell activation regulation, chemotaxis of activated lymphocytes, control of testosterone synthesis in Leydig cells, initiation of glucose-induced biphasic insulin response, steroidogenesis, and excitation–contraction coupling. rs2304418 variant in this gene is linked with lower mRNA expression of PDE8A, which in turn is linked with reduced HIV-1 (human immunodeficiency virus) replication. The expression of this protein is significantly high in macrophages, and is controlled by miR-145-5p. PDE8A promotes HIV-1 replication in macrophages and this is controlled at the level of reverse transcription.

General description

PDE8A (phosphodiesterase 8A) is one of the two subfamilies of PDE8 protein family, the other being PDE8B. PDE8 shows wide range of tissue expression, and is especially abundant in testis. PDE8A contains a Per, ARNT and Sim (PAS) signaling domain in its N-terminal. PDE8s contain receiver (REC) domain, N-glycosylation, N-myristoylation, amidation consensus sites, and potential kinase substrate sites for PKC (protein kinase), PKA and casein kinase.Human PDE8A1 (GenBank Accession No. NM_002605), full length with N-terminal GST tag, MW = 119kDa, expressed in a Baculovirus infected Sf9 cell expression system.

Physical form

Formulated in 25 mM Tris-HCl, pH 8.0, 100 mM NaCl, 0.05% Tween-20, 50% glycerol and 3 mM DTT.

Preparation Note

Thaw on ice. Upon first thaw, briefly spin tube containing enzyme to recover full content of the tube. Aliquot enzyme into single use aliquots. Store remaining undiluted enzyme in aliquots at -70°C. Note: Enzyme is very sensitive to freeze/thaw cycles.

Unit Definition

One unit is defined as the amount of enzyme that will convert 1 pmole of 3′, 5′-cAMP to 5′ AMP per min at 37°C