Table 2.
Functional consequences of disrupting AKAP-dependent protein–protein interactions
| Type | Name | Target | Model system | Physiological effect |
|---|---|---|---|---|
| Peptide | Ht-31 | AKAP–PKA | Mouse oocytes | Stimulation of oocyte maturationa |
| Rat hearts (in vivo) | Increased β-AR-stimulated contractilityb | |||
| Hippocampal neurons | Reduced AMPA/kainate channel currentsc | |||
| CD4(+) T cells | Reduced antigen presentation, inhibition of TNF-α and IL-10 productiond | |||
| S-Ht31 | AKAP–PKA | Renal inner medullary collecting duct (IMCD) cells | Inhibition of forskolin-stimulated AQP-2 translocatione,f | |
| TAT-AKAD | AKAP–PKA | Cardiac myocytes | Reduced contractilityg | |
| Mouse hearts (ex vivo) | Negative effect on chronotropy, inotropy and lusitropyg | |||
| AKAP15-LZ | AKAP18 – L-type Ca2+ channel | Mouse skeletal muscle cells (MM14, DZ1A) | Inhibition of voltage-dependent potentiation of L-type Ca2+ channelh | |
| AKAP18δ-wt | AKAP–PKA | Rat neonatal cardiac myocytes | Reduced β-adrenoceptor-induced L-type Ca2+ currentsi | |
| Arg9-11-PLN | AKAP18δ–PLN | Rat neonatal and adult cardiac myocytes | Reduced adrenoceptor-induced Ca2+ reuptake into the SRj | |
| RIAD-Arg11 | AKAP–PKA (I) | T cells | Uncoupling of cAMP-mediated inhibition of T-cell functionk | |
| Mouse Y1 adrenocortical cells | Reduced ACTH-stimulated progesterone productionk | |||
| AKAP-IS | AKAP–PKA | HEK293 cells | Attenuation of GluR1 (AMPA receptor subunit) currentsl | |
| CD4(+) T cells, KG-1 dendritic progenitor cells | Reduced antigen presentationd,m | |||
| TAT-AKAP-IS | AKAP–PKA | INS-1 Pancreatic β-cells | Inhibition of glucagon-induced potentiation of insulin secretionn | |
| Superakap-IS | AKAP–PKA (II) | Hippocampal neurons | Attenuation of AMPA-responsive currentso | |
| Peptido-mimetic | Unnatural RIAD | AKAP–PKA (I) | in vitro | Not determinedp |
| Small molecule | FMP-API-1 | AKAP–PKA | Rat neonatal cardiac myocytes | Increased contractilityq |
| Rat hearts (ex vivo) | Increased contractilityq |
TAT-AKAD, TAT-conjugated A-kinase anchoring disruptor (PKA binding region of AKAP10); RIAD: RI-anchoring disruptor; ACTH, adrenocorticotropic hormone; LZ, leucine zipper.