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Akt-Targeted Library

12,000 Compounds

Akt kinase, which is also known as Protein Kinase B (PKB), is one of the key members of extended serine/threonine protein kinase family. This kinase plays a crucial role in multiple cellular processes such as glucose metabolism, cell proliferation, apoptosis, transcription and cell migration. However, it should be noted, that targeting the kinase activity has revealed itself to be a challenge due to non-selectivity of the compounds towards other kinases. To date, three main Akt isoforms (Akt1, Akt2, and Akt3) have been identified in human cells. The first member is deeply involved in cellular survival pathways by inhibiting apoptotic processes. It 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. Since it can block apoptosis, and thereby promote cell survival, Akt1 has been implicated as a major factor in many types of cancer. Akt (now also called Akt1) was originally identified as the oncogene in the transforming retrovirus AKT8. The second isoform, Akt2, is an important signaling molecule in the Insulin signaling pathway. It is required to induce glucose transport. The role of Akt3 is less clear, though it appears to be predominantly expressed in brain. Akt is associated with tumor cell survival, proliferation, and invasiveness. The activation of Akt is also one of the most frequent alterations observed in human cancer and tumor cells. Tumor cells that have constantly active Akt may depend on Akt for survival. Therefore, understanding Akt and its pathways is important for the creation of better therapies to treat a range of diseases, especially cancer. In the past decade, the upstream signals that lead to Akt activation, the downstream substrates that exert the effects of Akt, and the secondary binding proteins that regulate Akt activation have been well documented. Among them, phosphatidylinositol 3-kinase (PI3K) is the most studied enzyme and several PI3K inhibitors have reached clinical trials. For example, the constitutive activation of the PI3K/Akt pathway has been confirmed as an essential step toward cell transformation. Inhibition of Akt kinase restores DNA damage processing and Chk1 activation after irradiation in late G2 [1]. This data demonstrates a previously unrecognized role for Akt in cell cycle regulation of DNA repair and checkpoint activation. Because Akt/PKB is frequently activated in many tumor types, these findings have important implications for the evolution and therapy of such cancers. It has also been described that PKB plays a critical role in regulation of migration of various cell types [2].

PTPN Targeted Library Selection_examples of structure

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