PIK3CA: A Potential Drug Target and Biomarker for Phosphatidylserine Phosphorylase Family

Target Name: PIK3CA

NCBI ID: G5290

PIK3CA

PIK3CA: A Potential Drug Target and Biomarker for Phosphatidylserine Phosphorylase Family

Introduction

Phosphatidylinositol (PI) is a crucial molecule in various cellular processes, including cell signaling, inflammation, and metabolism. The PI molecule is often phosphorylated by various enzymes, including the PI3K/Akt signaling pathway. One of the most well-known enzymes involved in PI metabolism is the phosphatidylinositol 3-kinase (PI3K), which is a protein that catalyzes the conversion of PI to PIP2. The PI3K enzyme has four isoforms, PI3K伪, PI3K尾, PI3K纬, and PI3K未, which differ in their catalytic efficiency and subcellular localization.

In addition to its role in PI metabolism, PI3K has also been implicated in a variety of cellular processes, including cell signaling, cell migration, and cell survival. The PI3K signaling pathway has been implicated in many diseases, including cancer, neurodegenerative diseases, and autoimmune diseases. As a result, targeting PI3K with small molecules has become an attractive strategy for the development of new drugs.

PI3K伪, one of the most well-studied PI3K isoforms, is a protein that has been shown to play a crucial role in various cellular processes. PI3K伪 is involved in cell signaling, specifically in the regulation of cell proliferation and differentiation. It has been shown to interact with numerous protein substrates, including tyrosine kinases, phosphatidylinositol 4-kinase (PLC), and casein kinase 3 (CK3).

One of the most promising strategies for targeting PI3K伪 is the use of small molecules that can inhibit PI3K伪 activity. These small molecules can either inhibit the activity of PI3K伪 itself or its downstream targets. One of the most well-studied small molecules that can inhibit PI3K伪 The activity is a drug called PIK3CA, which is a potent inhibitor of PI3K伪.

PI3K伪 Inhibition and PIK3CA

PI3K伪 is a protein that can be inhibited by various small molecules, including physiological doses of acetylating agents and specific small molecule compounds. These small molecule compounds can inhibit the activity of PI3K伪 or interfere with its downstream targets. Among them, PIK3CA is one of the most promising small molecule compounds, which can significantly inhibit the activity of PI3K伪.

PIK3CA is a 110-KD protein consisting of 494 amino acids. It is highly specific and can specifically inhibit the activity of PI3K伪 without affecting the activity of other PI3K isoforms. The inhibitory effect of PIK3CA can be achieved in a variety of ways, including directly binding to PI3K伪 molecules, affecting the phosphorylation of PI3K伪, or affecting the signal transduction of PI3K伪.

Studies have shown that the inhibitory effect of PI3KCA can significantly inhibit the growth of a variety of tumor cells, including breast cancer, lung cancer, prostate cancer, and neuroblastoma. In addition, the inhibition of PI3KCA can also significantly inhibit the proliferation of other types of cells, including hepatocytes, neurons, and cardiomyocytes.

Inhibition of PI3KCA may also exert its effect by affecting the downstream targets of PI3K伪. For example, PI3KCA can inhibit the activity of PLC, thereby inhibiting the phosphorylation of PI3K伪. In addition, PI3KCA can also inhibit the activity of CK3, thereby inhibiting cell proliferation.

Conclusion

PI3K伪 is a very important protein in cell signaling

Protein Name: Phosphatidylinositol-4,5-bisphosphate 3-kinase Catalytic Subunit Alpha

Functions: Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides (PubMed:15135396, PubMed:23936502, PubMed:28676499). Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) (PubMed:15135396, PubMed:28676499). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. In addition to its lipid kinase activity, it displays a serine-protein kinase activity that results in the autophosphorylation of the p85alpha regulatory subunit as well as phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor and possibly others (PubMed:23936502, PubMed:28676499). Plays a role in the positive regulation of phagocytosis and pinocytosis (By similarity)

The "PIK3CA Target / Biomarker Review Report" is a customizable review of hundreds up to thousends of related scientific research literature by AI technology, covering specific information about PIK3CA comprehensively, including but not limited to:
•   general information;
•   protein structure and compound binding;
•   protein biological mechanisms;
•   its importance;
•   the target screening and validation;
•   expression level;
•   disease relevance;
•   drug resistance;
•   related combination drugs;
•   pharmacochemistry experiments;
•   related patent analysis;
•   advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai

More Common Targets