|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
These studies yielded (1) 2-aminoquinazolin-4(3 H)-ones as potential lead structures for new antimalarial drugs, (2) a novel lipodepsipeptide specifically inducing apoptosis in cells deficient for the pVHL tumor suppressor, (3) small-molecule-based ROCK inhibitors that induce definitive endoderm formation and can potentially be used for regenerative medicine, (4) potential pharmacological chaperones for inborn errors of metabolism and a familiar form of acute myeloid leukemia (AML), and (5) novel tankyrase inhibitors that entered a lead-to-candidate program.
|
30616481 |
2019 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
Here, using new animal models, human cell lines, and <i>ex vivo</i> organoid cultures, we show that tankyrase (TNKS) inhibition can control WNT hyperactivation and provide long-term tumor control <i>in vivo</i>, but that effective responses are critically dependent on how APC is disrupted.
|
31337618 |
2019 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
With the goal of investigating the effects of tankyrase and Wnt pathway inhibition on tumor growth, we set out to find small-molecule inhibitors of TNKS/TNKS2 with suitable drug-like properties.
|
30883102 |
2019 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
In addition to their roles in telomere maintenance and regulation of mitosis, tankyrase proteins regulate tumor suppressors, including AXIN, phosphatase and tensin homolog and angiomotin.
|
30546421 |
2018 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
We also describe the use of 41 to investigate the biology of tankyrase, revealing the compound induced growth inhibition of a number of tumor derived cell lines, demonstrating the potential of tankyrase inhibitors in oncology.
|
28591512 |
2017 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
Three molecular inhibitors of the Wnt/β-catenin pathway demonstrated antitumor efficacy in various GIST models, both <i>in vitro</i> and <i>in vivo</i> Notably, the tankyrase inhibitor G007-LK alone had substantial activity against tumors of genetically engineered <i>Kit<sup>V558Δ/+</sup></i> mice, and the effect was increased by the addition of the Kit inhibitor imatinib mesylate.
|
28611108 |
2017 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
Finally, coadministration of an EGFR inhibitor and AZ1366 provided better tumor control and improved survival for Wnt-responsive lung cancers in an orthotopic mouse model.<b>Conclusions:</b> Tankyrase inhibition is a potent route of tumor control in EGFR-dependent NSCLC with confirmed dependence on canonical Wnt signaling.
|
27663586 |
2017 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
In addition, ARTD-5, or Tankyrase (TNKS), is a positive regulator of the WNT signaling implicated in the development and biological behavior of many neoplasms, such as Medulloblastoma (MB), in which radiotherapy is an essential part of the treatment.
|
25835728 |
2015 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
Forced resolution of sister telomere cohesion induces excessive recombination between non-homologs, genomic instability, and impaired cell growth, indicating the ATRX-macroH2A1.1-tankyrase axis as a potential therapeutic target in ALT tumors.
|
26373281 |
2015 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
Repressing TNKS activity through either genetic or pharmacological approaches antagonized canonical Wnt signaling, reduced murine and human lung cancer cell line growth, and decreased tumor formation in mouse models.
|
23621985 |
2013 |
|
Neoplasms
|
0.100 |
Biomarker
|
group |
BEFREE |
It was previously unknown whether the level of AXIN protein stabilization by tankyrase inhibition is sufficient to impact tumor growth in the absence of normal APC activity.
|
23539443 |
2013 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
Tankyrase 1 over-expression by gastric cancerous tissue was significantly associated with tumor histology differentiation and tumor stage.
|
21455637 |
2011 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
Tankyrase 1 mRNA expression showed a grade-dependent increase in tumor tissues and its expression was also high in estrogen and progesterone negative tumors.
|
18720522 |
2008 |
|
Neoplasms
|
0.100 |
AlteredExpression
|
group |
BEFREE |
We evaluated for the first time TNKS-1 mRNA expression by real time RT-PCR in tumor tissue, paired normal mucosa and urine sediment in patients with transitional cell carcinoma (TCC) of the bladder.
|
17617028 |
2007 |