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A-kinase anchoring proteins (AKAPs) are a group of proteins, which bind the regulatory subunits (RI and RII) of protein kinase A (PKA), anchoring it to specific locations within the cell. AKAPs play a central role in the regulation of signal transduction.
|Cat. No.||Product Name / Activity|
|AKAP disruptor; selectively binds PKA-RI with high affinity and blocks its interaction with AKAP; cell permeable|
|Inhibits PKA/AKAP interactions; cell permeable|
|AKAP disruptor; selectively binds PKA-RII and blocks its interaction with AKAP; cell permeable|
A-kinase anchoring proteins (AKAPs) are a group of proteins, which bind the regulatory subunits (RI and RII) of protein kinase A (PKA), anchoring it to specific locations within the cell. To date 30 genes with at least 50 members have been identified. Most of the identified AKAPs bind the RII region of PKA while several have been shown to bind RI. Some dual-AKAPs bind both RI and RII (D-AKAP1 and D-AKAP2 respectively). All AKAPs contain a PKA-anchoring domain, have unique localization signals and have the ability to complex with other signalling molecules. The AKAPs PKA-anchoring domain (an amphipathic helix) binds the N-terminal dimerization and docking domain of the regulatory subunit dimer of PKA.
Although initially classified by their ability to bind and tether PKA, AKAPs bind and anchor a wide variety of proteins, including phosphodiesterases (PDEs) protein kinase C (PKC), actin and MAPK. Spatio-temporal activation and termination of cellular signaling is pivotal to precise cellular function. AKAPs are able to regulate signaling events by tethering specific molecules in response to upstream cues. These molecules are usually tethered close to substrate proteins, allowing for efficient spatial and temporal control of cellular signaling. AKAPs allow for PKA to colocalize with other signaling proteins that propagate or terminate signal transduction.
AKAPs bring together kinase, phosphatases, phosphodiesterases, ion channels and receptors, at specific sites with in a cell. This scaffolding function helps regulate the cell cycle, ion channel activity and membrane trafficking amongst other functions. For example, simultaneous anchoring of PKA, PP2B and PKC generate an important locus for the integration of second messenger signals at the postsynaptic membrane.
Tocris offers the following scientific literature for A-Kinase-Anchoring Proteins to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.