|
Malignant neoplasm of colon and/or rectum
|
|
0.020 |
GeneticVariation
|
BEFREE |
Collectively, our data suggest that PF-04691502 exhibits potent anticancer activity in colorectal cancer by targeting both PIK3CA (H1047R) mutant CSCs and their derivatives.
|
23826249 |
2013 |
|
Carcinoma
|
|
0.020 |
GeneticVariation
|
BEFREE |
Somatic mutations of the PIK3CA gene were detected in 10/23 (43%) carcinomas and in all cases the type of mutation was H1047R in the kinase domain.
|
21735444 |
2011 |
|
Neoplasm Metastasis
|
|
0.030 |
GeneticVariation
|
BEFREE |
One hundred twenty-three patients were evaluated and the PIK3CA-H1047R mutation was assayed in sentinel LNs (SLNs), non-SLNs without metastasis, and serum by digital PCR.
|
30805870 |
2019 |
|
Neoplasm Metastasis
|
|
0.030 |
GeneticVariation
|
BEFREE |
This is best illustrated by an activating PIK3CA mutation (H1047R) which was clonal in the primary tumor, but completely absent from either the metastasis or cfDNA.
|
26317216 |
2015 |
|
Neoplasm Metastasis
|
|
0.030 |
GeneticVariation
|
BEFREE |
In addition, the oncogenic PIK3CA(H1047R) mutation was detected in a subpopulation of PV1, but this mutation did not seem to play a major role in vemurafenib resistance in this metastasis.
|
23948972 |
2013 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
Structural Perturbations due to Mutation (H1047R) in Phosphoinositide-3-kinase (PI3Kα) and Its Involvement in Oncogenesis: An in Silico Insight.
|
31592171 |
2019 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
The results suggest PIK3CA H1047R mutant cells have a selective advantage in breast, contribute to breast cancer susceptibility, and drive tumor progression during breast carcinogenesis, even when present as only a subpopulation of tumor cells.
|
27108388 |
2016 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
PIK3CA(H1047R) expression alone failed to promote tumor formation, but dramatically enhanced tumorigenesis initiated by KRAS(G12D).
|
26567140 |
2015 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
Using in situ genetic lineage tracing and limiting dilution transplantation, we have unravelled the potential of PIK3CA(H1047R), one of the most frequent mutations occurring in human breast cancer, to induce multipotency during tumorigenesis in the mammary gland.
|
26266975 |
2015 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
Recent studies by Meyer and colleagues, and Liu and colleagues demonstrate that expression of the H1047R exon 20 mutant of PIK3CA in luminal mammary epithelial cells induces tumorigenesis, implying that PIK3CA mutation is an early event in breast cancer.
|
22315990 |
2012 |
|
Carcinogenesis
|
|
0.060 |
GeneticVariation
|
BEFREE |
To better understand the role of mutant PIK3CA in the initiation or progression of tumorigenesis, we generated mice in which a PIK3CA mutation commonly detected in human cancers (the H1047R mutation) could be conditionally knocked into the endogenous Pik3ca locus.
|
22214849 |
2012 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
Since the PI3Kα isoform is implicated mostly in cancer, we conducted a high-throughput screening (HTS) campaign using a 3-step PI3K homogenous time-resolved fluorescence assay against this isoform bearing the H1047R mutation.
|
29991713 |
2018 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
The sequencing identified two hotspot mutations in exon 20 of one cancer samples at p. H1047L (c. 3140A > T) and eight cancer sample at p. H1047R (c. 3140A > G).
|
28269754 |
2017 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
The cell proliferation and migration of cancer cells bearing H1047R mutation were also reduced by P6-55.
|
28743532 |
2017 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
We developed a sensitive, simple and rapid approach to detect the low-abundance PIK3CA (H1047R) mutation in real CRC specimens, providing an effective tool for guiding cancer targeted therapy.
|
27405731 |
2016 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
Our results define a key effect of PIK3CA(H1047R) on mammary cell fate in the pre-neoplastic mammary gland and show that the cell of origin of PIK3CA(H1047R) tumours dictates their malignancy, thus revealing a mechanism underlying tumour heterogeneity and aggressiveness.
|
26266975 |
2015 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
Understanding how the H1047R mutation causes the enhanced activity of the protein in atomic detail is central to developing mutant-specific therapeutics for cancer.
|
25340423 |
2014 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
One EBV-positive cancer with PIK3CA mutation (H1047R) was MSI-positive.
|
23236232 |
2012 |
|
Primary malignant neoplasm
|
|
0.080 |
GeneticVariation
|
BEFREE |
We performed exome sequencing of DNA from unaffected and affected cells from an individual with an unclassified syndrome of congenital progressive segmental overgrowth of fibrous and adipose tissue and bone and identified the cancer-associated mutation encoding p.His1047Leu in PIK3CA, the gene that encodes the p110α catalytic subunit of PI3K, only in affected cells.
|
22729222 |
2012 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
Since the PI3Kα isoform is implicated mostly in cancer, we conducted a high-throughput screening (HTS) campaign using a 3-step PI3K homogenous time-resolved fluorescence assay against this isoform bearing the H1047R mutation.
|
29991713 |
2018 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
The sequencing identified two hotspot mutations in exon 20 of one cancer samples at p. H1047L (c. 3140A > T) and eight cancer sample at p. H1047R (c. 3140A > G).
|
28269754 |
2017 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
Furthermore, P6-55 was capable of inhibiting the elevated basal PI3K activity of H1047R, a hotspot mutation found in many types of human cancers.
|
28743532 |
2017 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
We developed a sensitive, simple and rapid approach to detect the low-abundance PIK3CA (H1047R) mutation in real CRC specimens, providing an effective tool for guiding cancer targeted therapy.
|
27405731 |
2016 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
The hotspot mutations c.1624G>A, c.1633G>A, and c.3140A>G (p.Glu542Lys, p.Glu545Lys, and p.His1047Arg), frequent in PIK3CA-associated cancers, overgrowth syndromes, and lymphatic malformation (LM), account for >92% of individuals who carry mutations.
|
26637981 |
2015 |
|
Malignant Neoplasms
|
|
0.090 |
GeneticVariation
|
BEFREE |
Our results define a key effect of PIK3CA(H1047R) on mammary cell fate in the pre-neoplastic mammary gland and show that the cell of origin of PIK3CA(H1047R) tumours dictates their malignancy, thus revealing a mechanism underlying tumour heterogeneity and aggressiveness.
|
26266975 |
2015 |