2021年6月10日 · Serotonin 5-HT receptor might activate dopaminergic neuron activity in a region-dependent manner via activating PI3K/Akt signaling through GPCR and extensively contributes to neurological functions. GPCR/PI3K/Akt signaling cascade is believed to be an important therapeutic target to understand neurodegenerative diseases .

2021年6月10日 · In this review, we focused on receptors, which activate PI3K/Akt pathway and its potential to treat Alzheimer's disease. Among several membrane receptors, GPCRs are the major drug targets for therapy, and GPCR signaling pathways are altered during Alzheimer's disease.

Among the signaling cascades regulated by GPCRs, the PI3K/AKT pathway intersects several vital cell functions, including apoptosis, proliferation, metabolism, growth, and glucose homeostasis (3 – 5). We utilized ovarian preantral GCs to elucidate how GPCRs can activate the PI3K/AKT pathway downstream of the IGF1R.

2021年12月16日 · In this review, we discuss the roles of the PI3K/Akt pathway in various cancer phenotypes, review the current statuses of different PI3K/Akt inhibitors, and introduce combination therapies...

The combined signaling by FcRγ (which couples to tyrosine kinases) and the LTB4 receptor (BLT1, a GPCR) preferentially required PI3Kβ, despite that stimulation with LTB4 alone activated PI3Kγ. These studies suggest that PI3K β serves a special function as a coincidence detector for signaling from RTKs and GPCRs.

2007年10月19日 · Akt plays an integral role in the phosphoinositide 3-kinase (PI3K) signaling pathways. PI3K pathways are activated in response to extracellular signals mediated by cell-surface receptors of the G protein-coupled receptor (GPCR), integrin and growth factor/receptor tyrosine kinase (RTK) superfamilies.

2021年8月27日 · Here, we report the architecture of the p110γ-p101 complex and a new mechanism of how it can be activated during GPCR signaling. Our cryo-EM structure of p110γ-p101 reveals important differences in the assembly of catalytic and regulatory subunits between class IA and class IB PI3Ks and provides novel insight into PI3K regulation.

2016年5月5日 · Therefore, it is possible that contact-dependent signaling between tumor cells and macrophages requires GPCR signaling through PI3Kβ. We also achieved partial rescue of p110β knockdown in T47D cells (PIK3CA mutant).

2019年3月1日 · The unusually complex regulation of PI3Kβ by small and trimeric G proteins and RTKs leads to a rich landscape of signaling responses at the cellular and organismic levels. This review focuses first on the regulation of PI3Kβ activity in vitro and in cells, and then summarizes the biology of PI3Kβ signaling in distinct tissues and in human ...

Phosphoinositide 3-kinase (PI3K) family members contain one of four different catalytic subunits and generate the second messenger PIP 3 in response to stimulation. Whereas some PI3K isoforms mediate signaling from receptor tyrosine kinases (RTKs) and one isoform mediates signals from GPCRs, PI3Kβ transduces signals from both receptor types.