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GENE:

PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)

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Other names: PIK3CA, Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha, Phosphoinositide-3-kinase, catalytic, alpha polypeptide, Serine/threonine protein kinase PIK3CA, PtdIns-3-kinase subunit P110-alpha, PI3K-alpha, Phosphatidylinositol-4,5-bisphosphate 3-kinase 110 KDa catalytic subunit alpha, Phosphatidylinositol 3-kinase, Catalytic, 110-KD, alpha, PI3-kinase P110 subunit alpha, PI3-kinase subunit alpha, PtdIns-3-kinase subunit alpha, PI3Kalpha, P110alpha, PI3K
1d
Programmable Argonaute-mediated single-nucleotide variant sequencing of cell-free DNA for multi-cancer early detection. (PubMed, Nat Commun)
Lastly, we evaluate its feasibility for multi-cancer early detection in population-scale screening using pooled plasma samples. The EC-SNV-Seq assay can enable highly sensitive and specific identification of low-frequency mutations, facilitating early cancer diagnosis and personalized treatment strategies.
Journal
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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KRAS mutation • EGFR mutation • PIK3CA mutation
1d
Design and synthesis of kidjoranin neoglycoside derivatives as potent anticancer agents. (PubMed, Fitoterapia)
Furthermore, exploratory molecular docking was also performed to probe possible binding modes of 4a with PI3Kα, STAT3, and Cyclin D1. Collectively, these findings indicate that C-3 glycosylation of kidjoranin may represent a viable approach for developing new anticancer candidates.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CCND1 (Cyclin D1) • STAT3 (Signal Transducer And Activator Of Transcription 3)
1d
Wuwei Ganlu counters exercise-induced fatigue via mitochondrial reinforcement and redox-inflammatory modulation. (PubMed, J Ethnopharmacol)
WGL counters exercise-induced fatigue by reinforcing CoQ-linked mitochondrial function and rebalancing redox-inflammatory signaling, which provides mechanistic support for its traditional external use and a rationale for further development.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • AKT1 (V-akt murine thymoma viral oncogene homolog 1) • TNFA (Tumor Necrosis Factor-Alpha) • TGFB1 (Transforming Growth Factor Beta 1) • IL1B (Interleukin 1, beta)
4d
Addition of ipatasertib to dual anti-HER2 maintenance therapy in HER2-positive metastatic breast tumors with PIK3CA mutations: the phase 1b SOLTI-1507 IPATHER trial. (PubMed, Clin Cancer Res)
These results support ipatasertib plus HP as a safe and promising maintenance strategy for HER2-positive breast tumors harboring PIK3CAmut.
P1 data • Journal
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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HER-2 positive • PIK3CA mutation
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Herceptin (trastuzumab) • Perjeta (pertuzumab) • ipatasertib (RG7440)
4d
A Case of Uterine Serous Carcinoma in a Patient with a Germline BRCA1 Mutation: Genomic Profiling Reveals an Ovarian Cancer-Like Molecular Signature. (PubMed, Case Rep Oncol)
This finding suggests that BRCA1-associated USC may be sensitive to poly ADP-ribose polymerase inhibitors, and also raises the question of whether risk-reducing hysterectomy should be considered for patients with BRCA1 mutation. USC with a BRCA1 mutation may have molecular characteristics distinct from those of sporadic USC, and further accumulation and analysis of such cases are needed to evaluate the clinical implications.
Journal • BRCA Biomarker • PARP Biomarker
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • BRCA1 (Breast cancer 1, early onset) • RB1 (RB Transcriptional Corepressor 1) • MAP3K1 (Mitogen-Activated Protein Kinase Kinase Kinase 1)
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TP53 mutation • PIK3CA mutation
6d
Morpheus-TNBC: A Study Evaluating the Efficacy and Safety of Multiple Treatment Combinations in Patients With Metastatic or Locally Advanced Breast Cancer (clinicaltrials.gov)
P1/2, N=792, Recruiting, Hoffmann-La Roche | N=580 --> 792 | Trial completion date: May 2028 --> Sep 2030 | Trial primary completion date: May 2028 --> Sep 2030
Enrollment change • Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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PD-L1 expression • PIK3CA mutation
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VENTANA PD-L1 (SP142) Assay
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • Ibrance (palbociclib) • carboplatin • gemcitabine • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Verzenio (abemaciclib) • albumin-bound paclitaxel • Kisqali (ribociclib) • fulvestrant • Halaven (eribulin mesylate) • letrozole • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Itovebi (inavolisib) • Actemra IV (tocilizumab) • atirmociclib (PF-07220060) • ladiratuzumab vedotin (SGN-LIV1A) • selicrelumab (RG7876)
6d
PIK75 effectively reverses PI3K‒AKT activation caused by palbociclib resistance and synergistically inhibits the progression of esophageal squamous cell carcinoma. (PubMed, Sci Rep)
The combined use of palbociclib and PIK75 synergistically inhibited the expression of the cell cycle proteins CCNE1, CDC6, and CDC25A, as well as the abnormal activation of PIK3CA and AKT phosphorylation. The combination of these two drugs synergistically inhibited tumor cell cycle progression and promoted apoptosis in vitro and in vivo, which provides a promising idea for the treatment of ESCC in the future.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • CCNE1 (Cyclin E1) • CDC25A (Cell Division Cycle 25A) • GNRP (Ras-Specific Guanine Nucleotide-Releasing Factor 1)
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Ibrance (palbociclib) • PIK-75
7d
Preclinical • Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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Mekinist (trametinib) • carboplatin • paclitaxel • omipalisib (GSK2126458)
7d
Tumor necrosis associates with aggressive breast cancer features, increased hypoxia signaling and reduced patient survival. (PubMed, Sci Rep)
Mutational profiling pointed to enrichment of TP53 and PIK3CA mutations in tumors with and without necrosis, respectively. This study confirms the association of breast cancer necrosis with aggressive tumor features and reduced survival, and points to the BCNS score as a potential biomarker that should be further explored and validated to improve breast cancer diagnosis and management.
Journal
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TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
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TP53 mutation • PIK3CA mutation
7d
Clinicopathological features and mutational landscape of colorectal cancer subgroups defined by MSI and EMAST status. (PubMed, Pathol Res Pract)
MSS/EMAST-L tumors aligned with chromosomally stable, KRAS/Wnt-driven CRC. In conclusion, MSS/EMAST-H tumors represent an underrecognized CRC subtype with intermediate genomic instability and a distinctive molecular profile, with potential implications for prognostic assessment and personalized therapeutic strategies.
Journal • MSi-H Biomarker
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KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • MSI (Microsatellite instability) • MLH1 (MutL homolog 1) • CTNNB1 (Catenin (cadherin-associated protein), beta 1)
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TP53 mutation • KRAS mutation • MSI-H/dMMR • BRAF mutation • PIK3CA mutation
8d
Laser Desorption-Rapid Evaporative Ionization Mass Spectrometry (LD-REIMS): A New Tool for the High-Throughput Metabolomic and Lipidomic Profiling of Live Cells. (PubMed, Anal Chem)
We also applied the method to establish lipidomic differences across the isogenic MCF10A cells harboring either WT or MUT PIK3CA. Finally, we conducted time-series experiments on hypoxic cells, which revealed significant dynamic changes in metabolism, including lactate accumulation due to anaerobic glycolysis.
Journal • Metabolomic study
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha)
8d
Gene discovery in extensive dermal melanocytosis reveals multiple mosaic causes. (PubMed, Br J Dermatol)
Clinically, our findings highlight the importance of differentiating EDM from common blue spots, and we recommend ophthalmological investigation even in the absence of periocular cutaneous involvement. The association with CNS infarct is unclear, but we suggest clinical neurological features be sought and MRI undertaken if there are concerns. Genetically, these results not only expand the causative genotype of EDM, but also challenge our concept of the Mosaic Disorders currently described with HRAS, ACTB, PIK3CA, and GNA11. Stratification by genotype may help determine patient melanoma risk more accurately in the future. Patient- and variant-specific genetic counselling should be given where there is a potential risk of germline transmission to offspring.
Journal
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PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • HRAS (Harvey rat sarcoma viral oncogene homolog) • GNAQ (G Protein Subunit Alpha Q) • GNA11 (G Protein Subunit Alpha 11)