PIK3CA Antibody, Biotin conjugated

Preservative: 0.03% ProClin 300; Constituents: 50% Glycerol, 0.01M PBS, pH 7.4

Liquid

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PIK3CA

P42336

Phosphoinositide-3-kinase (PI3K) is a kinase that phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at the 3-position of the inositol ring, producing 3-phosphoinositides. Utilizing ATP and phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2), it generates phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a crucial role in recruiting PH domain-containing proteins, such as AKT1 and PDPK1, to the cell membrane. This recruitment activates signaling cascades involved in cell growth, survival, proliferation, motility, and morphology. PI3K participates in cellular signaling in response to various growth factors and is involved in AKT1 activation upon stimulation by receptor tyrosine kinase ligands, including EGF, insulin, IGF1, VEGFA, and PDGF. It is also involved in signaling via insulin-receptor substrate (IRS) proteins. PI3K is essential for endothelial cell migration during vascular development via VEGFA signaling, potentially by regulating RhoA activity. It's required for lymphatic vasculature development, possibly through RAS binding and activation by EGF and FGF2 (but not PDGF). Additionally, PI3K regulates invadopodia formation via the PDPK1-AKT1 pathway, participates in cardiomyogenesis in embryonic stem cells through an AKT1 pathway, and participates in vasculogenesis in embryonic stem cells through the PDK1 and protein kinase C pathways. Beyond its lipid kinase activity, PI3K exhibits serine-protein kinase activity, resulting in autophosphorylation of the p85alpha regulatory subunit and phosphorylation of other proteins such as 4EBP1, H-Ras, the IL-3 beta c receptor, and potentially others. Finally, PI3K plays a role in the positive regulation of phagocytosis and pinocytosis.

1. Five distinct PIK3CA (NM_006218.2) mutations were identified, including one hotspot mutation (c.1624G>A;p.Glu542Lys); two recurrent, strong gain-of-function mutations (c.3140A>T;p.His1047Leu, c.1258T>C;p.Cys420Arg); one previously reported mutation associated with macrodactyly (c.344G>C;p.Arg115Pro); and one novel somatic mutation (c.248T>C; p.Phe83Ser). PMID: 29446767
2. PIK3CA mutations in gastric cancer are rare, strongly associated with microsatellite instability (MSI), and correlate with a worse prognosis compared to other MSI patients. Exon 9 and exon 20 mutations exhibit distinct prognostic implications, with exon 20 mutations showing a more favorable outcome. PMID: 29905413
3. In early-stage breast cancer, PIK3CA mutations appear to identify HER2+ patients less likely to achieve a pathologic complete response (pCR). Exon 9 and exon 20 mutations show varying clinical implications requiring further investigation. PMID: 29575819
4. miR152 plays a significant role in pancreatic beta-cell function and is associated with the PI3Kalpha axis. PMID: 30106118
5. Most PIK3CA H1047R mutations in breast cancer precede genome doubling. PMID: 29170395
6. In Stage I colorectal cancer, KRAS mutations, simultaneous PIK3CA mutations, or multiple KRAS mutations were significantly associated with reduced cancer-specific survival. PIK3CA or multiple KRAS mutations were also associated with nodal micrometastases and poorly differentiated clusters (G3). PMID: 30018674
7. CTNNB1 mutations were prevalent (60%) in basal cell adenomas but absent in basal cell adenocarcinomas. No PIK3CA mutations were detected. CTNNB1 mutations were more common in tumors with tubular or tubulotrabecular patterns. PMID: 29224720
8. The critical roles of p110beta and p110alpha in PIP3 production following platelet stimulation have been demonstrated. PMID: 29902570
9. High PI3K expression is associated with metastasis in ovarian cancer. PMID: 29739299
10. Phenotypic metabolic changes following a single-copy knock-in of mutant PIK3CA (H1047R) in the MCF10A cell line (a model for studying oncogenic transformation in breast tissue) were examined. PMID: 28393905
11. Impactful PIK3CA and PIK3R1 mutations show mutual exclusivity, resulting in PI3K pathway hyperactivity and oncogenesis in breast cancer. PMID: 29636477
12. PIK3CA mutation is associated with a decreased risk of peritoneal metastases in chemoresistant metastatic colorectal cancer. PMID: 29380640
13. High PIK3CA expression is associated with metastasis via epithelial-mesenchymal transition in colorectal cancer. PMID: 30066935
14. High PI3KCA expression is associated with drug resistance and proliferation in breast cancer. PMID: 28165066
15. High PI3K expression is associated with periodontitis. PMID: 30218719
16. IDH2 R172 hotspot mutations and PIK3CA hotspot mutations were validated in 100% and 67% of solid papillary breast carcinomas with reverse polarity, respectively. PMID: 29603332
17. High PIK3CA expression is associated with metastasis in colon cancer. PMID: 29305742
18. Hotspot regions from PIK3CA, AKT, and PTEN genes were sequenced using the Ion Personal Genome Machine (PGM) and Ion Torrent Ampliseq Cancer panel in 39 samples of triple-negative breast cancer (TNBC) from Moroccan patients; results were correlated with clinical-pathologic data. PMID: 30227836
19. Low-grade adenosquamous carcinoma of the breast is a low-grade triple-negative breast cancer with a basal-like phenotype, lacking androgen receptor expression, and exhibiting a high rate of PIK3CA mutations. PMID: 29537649
20. Multivariate analyses revealed that PIK3CA mutation and clinical T stage were independent favorable prognostic factors. PIK3CA mutations were significantly associated with APC alterations and BRAF mutations. PMID: 30115035
21. Plasma samples showed a higher frequency of ESR1 and PIK3CA mutations than serum samples in metastatic breast cancer (MBC) patients, suggesting plasma as the preferred source of cell-free DNA (cfDNA). PMID: 29689710
22. Cases with a PIK3CA mutation and/or low PTEN expression had a lower pathologic complete response (pCR) rate (4%) compared to cases with wild-type PIK3CA and high PTEN expression (39%). PMID: 29110152
23. PI3K acts as a signal linker between L-selectin and PSGL-1 in IL-18 transcriptional activation at the promoter level. PMID: 29218606
24. The role of PI3K in cancer, including PIK3CA mutations (present in approximately 30% of human cancers), is well-established. This review discusses PI3K structures, activation modes, and implications in angiogenesis, extracellular matrix remodeling, and tumor immunity. PMID: 29219001
25. Double mutations of PIK3CA and TP53 are an independent predictive factor for overall survival in stage II/III colorectal cancer patients receiving 5-FU-based chemotherapy. PMID: 29434452
26. High PI3K expression is associated with cervical cancer. PMID: 29328485
27. High PIK3CA expression is associated with head and neck carcinoma. PMID: 29506489
28. pK15-dependent signaling may originate from intracellular vesicles and utilize the endocytic machinery. Specifically, PI3K-C2alpha, a class II PI3K, is recruited by pK15 and involved in pK15-dependent intracellular signaling and viral reactivation from latency. PMID: 29950425
29. Oncogenic PIK3CA mutations cause glutamine dependency in colorectal cancer, suggesting that targeting glutamine metabolism may be an effective treatment strategy for patients with PIK3CA mutations. PMID: 27321283
30. High-resolution melting analysis is a rapid and sensitive method for PIK3CA mutation screening. PIK3CA dysregulation in bladder cancer suggests its role in cancer development and potential for targeted therapy. PMID: 29353467
31. In patients without PIK3CA alterations, nonfunctional TP53 mutations are associated with a poor prognosis. PMID: 29714670
32. Knowing the mutation status of KRAS, BRAF, or PIK3CA in stage II colorectal cancer improves prognostic accuracy. PMID: 28685592
33. PIK3CA mutation was a significant prognostic factor for poor overall and cancer-specific survival in stage IIB to IVA cervical cancers treated with concurrent chemoradiotherapy. PMID: 30075505
34. Oncogenic PIK3CA alters methionine and cysteine utilization, partly by inhibiting xCT, contributing to methionine dependency in human breast cancer cells. PMID: 29259101
35. The bladder cancer cell line TCCSUP (harboring a PIK3CA E545K mutation) showed sensitivity to pictilisib compared to cell lines with wild-type PIK3CA. Pictilisib demonstrated stronger antitumor activity in patient-derived xenograft models with PI3KCA H1047R mutation or amplification. PMID: 28808038
36. PI3K/Akt regulation of glycolysis is a multifaceted modulator of single-cell metabolic dynamics, maintaining metabolic stability in proliferating cells. PMID: 29239720
37. c-Jun, p38 MAPK, PIK3CA/Akt, and GSK3 signaling are involved in the effect of miR-203 on hepatocellular carcinoma cell proliferation. PMID: 28887744
38. Aspirin inhibits human uterine leiomyoma cell growth by regulating K-Ras/p110alpha interaction, suggesting its potential as a new therapeutic drug. PMID: 28849118
39. PIK3CA mutation is a distinctive genetic feature of non-small cell lung cancer (NSCLC) with chronic obstructive pulmonary disease (COPD), regardless of age, smoking history, pathological stage, or histology. PMID: 29191607
40. In a study of 71 patients with advanced solid tumors (86% with PIK3CA mutations), three different dose schedules of TAK-117 were evaluated, establishing the maximum tolerated dose. PMID: 28490463
41. Head and neck squamous cell carcinoma tumors with low P120CTN and PI3K pathway mutations exhibit higher MMP1 levels than tumors with high P120CTN and no PI3K pathway mutations, indicating that P120CTN downregulation and PIK3CA mutations promote MMP1-driven invasion. PMID: 28637905
42. Case reports show PIK3CA mutations in multiple tissues affected by facial infiltrating lipomatosis. PMID: 28665924
43. p85alpha plays a tumor-suppressive role; p110alpha-selective therapeutics may be effective in breast cancer patients with PIK3R1 loss. PMID: 28630349
44. High PI3K expression is associated with metastasis in esophageal squamous cell carcinoma. PMID: 28418888
45. The E545K missense mutation of PIK3CA is associated with loss of protein stability and breast cancer development. PMID: 27581627
46. Telomere length did not correlate with BRAF, PIK3CA, or MSI status but was significantly associated with KRAS mutations. PMID: 28850092
47. The combination of SAR256212 and SAR245408 resulted in stable disease as the best response, with side effects similar to those of individual drugs; outcome was independent of PI3KCA mutation status. PMID: 28031425
48. High PI3K expression is associated with nasopharyngeal carcinoma. PMID: 28586035
49. Co-occurring oncogenic HER2 and mutant PIK3CA induce replication stress in mammary epithelial cells and drive breast cancer progression. PMID: 28902361
50. Mosaic gain-of-function PIK3CA mutations cause abnormal AKT-mTOR pathway activation and associated clinical manifestations. PMID: 28577738

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HGNC: 8975

OMIM: 114480

KEGG: hsa:5290

STRING: 9606.ENSP00000263967

UniGene: Hs.553498

Colorectal cancer (CRC); Breast cancer (BC); Ovarian cancer (OC); Hepatocellular carcinoma (HCC); Keratosis, seborrheic (KERSEB); Megalencephaly-capillary malformation-polymicrogyria syndrome (MCAP); Congenital lipomatous overgrowth, vascular malformations, and epidermal nevi (CLOVE); Cowden syndrome 5 (CWS5)

PI3/PI4-kinase family