AKT3

AKT3

A gene on chromosome 1q44 that encodes protein kinase B (PKB), a member of the serine-threonine protein kinase family, which regulate cell signalling in response to insulin and growth factors and are involved in an array of biological processes including cell proliferation, differentiation, apoptosis and tumourigenesis, as well as glycogen synthesis and glucose uptake. PKB is stimulated by platelet-derived growth factor (PDGF), insulin and insulin-like growth factor 1.
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In TNBC, Akt3-MAGI3 fusions have been reported to upregulate the expression of AKT3, while removing the PDZ [PSD95 (postsynaptic density protein), Dlg1 (Drosophila disc large tumor suppressor), and zo-1 (zonula occludens-1 protein)] domain of MAGI3, required for PTEN binding.
SNP rs14339964 at Gga3:36327458 is located in an intron region of AKT3 which is known to be regulators of cell signaling in response to insulin and growth factors and involved in a wide variety of biological processes.
Mutations in three genes, AKT3, PIK3R2 and PIK3CA, were also found to be associated with a constellation of disorders including cancer, hydrocephalus, epilepsy, autism, vascular anomalies and skin growth disorders.
AKT3, PIK3R2 and PIK3CA are present in all humans, but mutations in the genes are what lead to conditions including megalencephaly, cancer and other disorders.
Other less common aberrations found in melanomas include PI3K mutations, loss of heterozygosity of PTEN, amplification of AKT3, KIT mutations, and constitutive activating mutations of ERK.
AKT3 is also responsible for progression to a more aggressive melanoma.
Three members, AKT1, AKT2, and AKT3, have been identified in this subfamily and VQD-002 has been shown to inhibit all three isoforms.
A study of mutations across breast cancer subtypes identified recurrent aberrations in the CBFB [5] (core-binding factor, beta subunit) gene, deletions in its partner RUNX1 (runt-related transcription factor 1), and fusion of the MAGI3 (membrane associated guanylate kinase, WW and PDZ domain containing 3) gene with the AKT3 [v-akt murine thymoma viral oncogene homolog 3 (protein kinase B, gamma)] gene (i.
5] Human genes: CBFB, core-binding factor, beta subunit; RUNX1, runt-related transcription factor 1; MAGI3, membrane associated guanylate kinase, WW and PDZ domain containing 3; AKT3, v-akt murine thymoma viral oncogene homolog 3 (protein kinase B, gamma); MAGI3-AKT3, fusion of genes MAGI3 and AKT3; KRAS, v-Ki-ras2 Kirsten rat sarcoma viral oncogene homolog; CT-NNB1, catenin (cadherin-associated protein), beta 1, 88kDa; SMARCA4, SWI/ SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4; CREBBP, CREB-binding protein; WNT, wingless-type MMTV integration site family; BRAF, v-raf murine sarcoma viral oncogene homolog B1.
These compounds display nanomolar inhibitory activity and are >100-fold selective over AKT2, AKT3, and 96 other enzyme targets.