Akt medical abbreviation

The serine-threonine protein kinase AKT1 is catalytically inactive in serum-starved primary and immortalized fibroblasts.

Federal government websites often end in. The site is secure. Its activation is controlled by a multi-step process that involves phosphoinositidekinase PI3K. This triggers activation of PI3K and conversion by its catalytic domain of phosphatidylinositol 3,4 -bisphosphate PIP 2 lipids to phosphatidylinositol 3,4,5 -trisphosphate PIP 3. Full activation of Akt leads to additional substrate-specific phosphorylation events in both the cytoplasm and nucleus, including inhibitory phosphorylation of the pro-apoptotic FOXO proteins Guertin et al. Additional Perspectives on Signal Transduction available at www. As a library, NLM provides access to scientific literature.

Akt medical abbreviation

Journal of Biomedical Science volume 29 , Article number: 76 Cite this article. Metrics details. A Correction to this article was published on 25 January Growth factor signaling plays a pivotal role in diverse biological functions, such as cell growth, apoptosis, senescence, and migration and its deregulation has been linked to various human diseases. Akt kinase is a central player transmitting extracellular clues to various cellular compartments, in turn executing these biological processes. Since the discovery of Akt three decades ago, the tremendous progress towards identifying its upstream regulators and downstream effectors and its roles in cancer has been made, offering novel paradigms and therapeutic strategies for targeting human diseases and cancers with deregulated Akt activation. Unraveling the molecular mechanisms for Akt signaling networks paves the way for developing selective inhibitors targeting Akt and its signaling regulation for the management of human diseases including cancer. Cells respond to various extracellular clues, such as growth factors and cytokines for their proliferation and survival by engaging their cognate receptors. Deregulation of this pathway is associated with numerous types of human diseases, such as diabetes and cancers [ 1 , 2 ]. Class IA of the PI3K consists of the p85 regulatory subunit and p catalytic subunit that together form a heterodimer. By binding to the p catalytic subunit, the p85 regulatory subunit keeps PI3K in an inactive state until stimulated by growth factors or cytokines. In response to these physiological cues, the p85 subunit of PI3K is phosphorylated and relieves its inhibition on PI3K for its activation. The activated PI3K then triggers the formation of PIP3 phosphoinositol 3, 4, 5-triphosphate in the plasma membrane by phosphorylating PIP2 phosphoinositol 4, 5-biphosphate , a second messenger that interacts with the PH domain of Akt and recruits Akt to the plasma membrane for activation [ 1 , 2 ]. Akt contains the N-terminal pleckstrin homology PH domain , central catalytic domain and C-terminal regulatory region.

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Federal government websites often end in. The site is secure. They are stimulated by a large variety of extracellular stimuli. Individual AKT members have a widely diverse repertoire of downstream effects in different settings by targeting over different substrates 1. Further search in the literature resulted in the following findings:. Rhoads by K.

Federal government websites often end in. The site is secure. Targeted cancer therapies are used to inhibit the growth, progression, and metastasis of the tumor by interfering with specific molecular targets and are currently the focus of anticancer drug development. Protein kinase B, also known as Akt, plays a central role in many types of cancer and has been validated as a therapeutic target nearly two decades ago. This review summarizes the intracellular functions of Akt as a pivotal point of converging signaling pathways involved in cell growth, proliferation, apoptotis and neo-angiogenesis, and focuses on the drug design strategies to develop potent anticancer agents targeting Akt. The discovery process of Akt inhibitors has evolved from adenosine triphosphate ATP -competitive agents to alternative approaches employing allosteric sites in order to overcome the high degree of structural similarity between Akt isoforms in the catalytic domain, and considerable structural analogy to the AGC kinase family. This process has led to the discovery of inhibitors with greater specificity, reduced side-effects and lower toxicity.

Akt medical abbreviation

There are three different genes that encode isoforms of Protein kinase B. Akt1 is involved in cellular survival pathways, by inhibiting apoptotic processes. Akt1 is also able to induce protein synthesis pathways, and is therefore a key signaling protein in the cellular pathways that lead to skeletal muscle hypertrophy and general tissue growth. A mouse model with complete deletion of the Akt1 gene manifests growth retardation and increased spontaneous apoptosis in tissues such as testes and thymus. Akt1 was originally identified as the oncogene in the transforming retrovirus , AKT8. Akt2 is an important signaling molecule in the insulin signaling pathway.

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References Cantley LC. The "t" stands for ' thymoma '; the letter was added when a transforming retrovirus was isolated from the Ak mouse strain, which was termed "Akt-8". We suggest that targeting Skp2, an upstream regulator for Akt, can be another potential approach for human cancer treatment on the basis of the findings from our group and others that Skp2 is required for cancer development in diverse genetic tumor models [ 33 , 70 , , , ]. The intensive research efforts on studying Akt signaling during last two decades have significantly advanced our current understandings of how oncogenic Akt is activated and how it transmits the signal to downstream effectors to participate in various biological processes. Article Talk. Bibcode : Natur. In addition, Akt also undergoes O -linked N -acetylglucosamine glycosylations O -GlcNAcylation , which is a dynamic and reversible modification on serine and threonine residues leading to interfering the cellular signaling and function. Brunet A, et al. ONCO c-Akt. GSK-3beta regulates cyclin D1 expression: a new target for chemotherapy. It was shown that the activation occurs through phosphatidylinositol 3-kinase. Alessi DR, et al. Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression.

They are stimulated by a large variety of extracellular stimuli. Individual AKT members have a widely diverse repertoire of downstream effects in different settings by targeting over different substrates 1. Further search in the literature resulted in the following findings:.

PMID Apr 5, Thus, RhoA is a relevant downstream effector for Skp2-mediated cell migration and metastasis. Figure 1. More reference expression data. Most of its substrates remains to be determined what their functional relevance in Akt signaling is. Targeting activated Akt with GDC, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Google Scholar Chen Q, et al. Alteration in cell cycle regulation is believed to be a key driving force for cancer development. A PP2A regulatory subunit regulates C. Liu Z, et al. Ranieri C, et al. New York: Garland Science.