Inhibition human cancers cancer aurora kinases. Medical search. Frequent questions

Treating SCCHN cell lines with a pan-Aurora kinase inhibitor resulted in defective cytokinesis, polyploidy and apoptosis, which was effective irrespective of the EGFR status. (oncotarget.com)
A key feature of prostate cancer progression is the induction and activation of survival proteins, including the Inhibitor of Apoptosis (IAP) family member survivin. (oncotarget.com)
Our study demonstrates that survivin and APE1/Ref-1 are significantly higher in human prostate cancer specimens compared to noncancerous controls and that APE1/Ref-1 redox-specific inhibition with small molecule inhibitor, APX3330 and a second-generation inhibitor, APX2009, decreases prostate cancer cell proliferation and induces cell cycle arrest. (oncotarget.com)
MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. (xcessbio.com)
Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. (xcessbio.com)
The drug - called an Aurora kinase inhibitor - improved survival for mice when combined with chemotherapy. (cancerresearchuk.org)
M any kinase inhibitor compounds have been found. (callaix.com)
The first kinase inhibitor introduced for cancer was imatinib, which the FDA approved in 2001. (callaix.com)
Oss, April, 8th, 2016 - At the AACR 2016 conference, to be held in New Orleans next week, Jos de Man, Senior Investigator Chemistry at NTRC, will present on the unique binding mode of NTRC's TTK kinase inhibitor clinical candidate NTRC 0066-0. (oncolines.com)
It is shown that the biochemical target of an inhibitor predicts its clustering, and that empirical cell line responses correspond to well-known cancer hallmarks. (oncolines.com)
For example, alteronol (protein kinase B (PKB, also known as Akt)/the mechanistic target of rapamycin (mTOR) inhibitor) induces autophagy in melanoma cancer cells and inhibits their metastasis and migration via inhibition of EMT. (highwire.org)
7 8 Alisertib (inhibitor of phosphatidylinositol 3-kinase (PI3K)/Akt/mTOR) induces autophagy and inhibits metastasis in ovarian cancers cells via inhibition of EMT. (highwire.org)

Patients characterized by elevated EGFR and elevated Aurora-A protein expression in tumor tissue represent a risk group with poor disease-free and overall survival (EGFR low Aurora-A low versus EGFR high Aurora-A high , p=0.024). (oncotarget.com)
Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
Due to the role of oncogenic transcriptional activators NFĸB and STAT3 in survivin protein expression, and APE1/Ref-1 redox activity regulating their transcriptional activity, we assessed selective inhibition of APE1/Ref-1's redox function as a novel method to halt prostate cancer cell growth and survival. (oncotarget.com)
Inhibition of APE1/Ref-1 redox function significantly reduced NFĸB transcriptional activity, survivin mRNA and survivin protein levels. (oncotarget.com)
Pfizer) plus Everolimus are underway (35 36 Furthermore preclinical data have shown that mTORC1 inhibition results in a hyperactivation of the PI3K pathway and simultaneous increase of the signaling through the mitogen-activated protein kinase kinase (MAPK) pathway (37) thus proving the presence of another opinions loop that connect the PI3K-AKT-mTOR with the MAPK pathway. (biomasswars.com)
The protein encoded by this gene is a putative serine/threonine kinase that localizes to the mitotic apparatus and complexes with cell cycle controller CDC2 kinase in early mitosis. (cancerindex.org)
The N-terminal region of the protein binds CDC2 to form a complex showing reduced H1 histone kinase activity, indicating a role as a negative regulator of CDC2/cyclin A. In addition, the C-terminal kinase domain binds to its own N-terminal region, suggesting potential negative regulation through interference with complex formation via intramolecular binding. (cancerindex.org)
Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (lookformedical.com)
The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)
Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
Receptor Tyrosine Kinases (RTKs) are a family of tyrosine protein kinases. (callaix.com)
The protein kinase TTK is a component of the spindle assembly checkpoint, a protein machinery that regulates correct segregation of chromosomes over daughter cells during cell division. (oncolines.com)
In addition, NTRC develops own novel targeted therapies based on small molecules, such as selective inhibitors of TTK (Mps1) protein kinase for chromosomal unstable tumours and inhibitors of the tryptophan metabolizing enzymes IDO1 and TDO for cancer immunotherapy. (oncolines.com)

Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. (xcessbio.com)
Works in various organisms have revealed that the kinase is involved in centrosome separation, duplication and maturation as well as in bipolar spindle assembly and stability. (lookformedical.com)

The phosphatidylinositol 3' kinase (PI3K)/AKT axis, Hedgehog signaling pathway, nuclear factor-kappaB and Activating Transcription Factor 2 have also been implicated to be involved in EMT. (wikipedia.org)
A story of two complexes The PI3K-AKT-mTOR pathway (Physique 1) is commonly altered in human cancers. (biomasswars.com)
In contrast simultaneous inhibition of PI3K-AKT and MAPK BIBR 953 pathways decreased cell viability and pointed towards as this combination as the most optimal way to effectively inhibit both pathways (38). (biomasswars.com)
15 16 Activation of PI3K/Akt/mTOR pathway induces EMT in several cancer models via activation of EMT transcription factors. (highwire.org)
14 18 19 Inhibition of PI3K/Akt/mTOR pathway can be reversed using specific inhibitors of the pathway and decrease tumor metastasis. (highwire.org)

The phosphatydilinositol-3-kinase (PI3K)/mammalian focus on of rapamycin (mTOR) pathway is a main concentrate of attention for cancers researchers before decade. (biomasswars.com)
Finally the last section will be devoted to a new class of compounds that are able to inhibit both mTOR complexes and the new dual inhibitors that are also adding activity against the phosphatydilinositol-3-kinase (PI3K) a key component of the main opinions loop involved in this pathway. (biomasswars.com)
Moreover Wan et al showed in human rhabdomyosarcoma cell lines and xenografts that blockade of IGF-1R led to an inhibition of the Rapamycin-induced AKT activation (31) providing evidence for any synergistic effect of mTOR and IGF-1R inhibition. (biomasswars.com)
This observation has provided rationale for combining several ongoing phase I clinical trials combining mTOR PI3K or AKT inhibitors with MAP/ERK kinase (MEK) inhibitors. (biomasswars.com)
HNK controls various intracellular signaling pathways involved in cancer, including those related to nuclear factor kappa B (NF- B), signal transducers and activators of transcription 3 (STAT3), epidermal growth factor receptor (EGFR), and mammalian targets of rapamycin (mTOR) [ 12 ]. (hindawi.com)
Different subclasses of PI3K/mTOR, Aurora and EZH2 inhibitors were identified that relate to different mechanisms of activity or different genetic targeting. (oncolines.com)
Several recent investigations have showed that inhibition of EMT in cancer cells induces autophagy, while inhibition of mTOR (autophagy induction) slows down the metastasis of cancer cells. (highwire.org)

A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)
Other kinases work on serine or threonine residues. (callaix.com)

Aurora A overexpression in many malignant tumor types suggests that it may be directly involved in NEOPLASTIC CELL TRANSFORMATION. (lookformedical.com)

An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
kinase in candida, is an important mitosis regulatory proteins encoded on human being chromosome 20q13.2 that induces oncogenic change followed with centrosome amplification and aneuploidy when over indicated SEMA3E in rodent cells and (6-8). (arcillaresearch.com)

Aurora kinases are found in all organisms in which their function has been conserved throughout evolution, namely the control of chromosome segregation. (lookformedical.com)
Inhibition of TTK results in chromosome missegregation and apoptosis of tumour cells. (oncolines.com)

Aurora Kinase-A gene is usually amplified and overexpressed in lots of human malignancies, including colorectal, breasts, ovarian, bladder, gastric and pancreatic malignancies. (arcillaresearch.com)

Therefore, the altered capacity of cancer cells to repair and/or replicate DNA is the basis of many classical therapies, such as platinum-based agents, and also recently introduced or upcoming therapies, such as PARP inhibitors or ATR inhibitors (reviewed in refs. (nature.com)
Kinase inhibitors are now one of the major categories of chemotherapy medicine. (callaix.com)
Over 50 kinase inhibitors are approved in the US for cancer treatment with more under development. (callaix.com)
Of the 69 new drugs approved by the FDA for cancer from 2015 to 2020, 26 were kinase inhibitors. (callaix.com)
Most kinase inhibitors work on tyrosine kinases . (callaix.com)
As oncology drugs, kinase inhibitors were created out of modern genetics- the understanding of DNA, the cell cycle, and molecular signaling pathways- and thus represent a change from general to molecular methods of cancer treatment. (callaix.com)
An article published in the journal Molecular Cancer in 2018 claimed that over 10,000 patents had been filed in the US for kinase inhibitors since 2001. (callaix.com)
Tyrosine kinase inhibitors (TKIs) are a class of chemotherapy medications that inhibit, or block, one or more of the enzyme tyrosine kinases. (callaix.com)
Tyrosine kinase inhibitors treat cancer by correcting this deregulation. (callaix.com)
NTRC has developed a series of highly selective inhibitors of TTK enzyme activity that potently inhibit proliferation of human cancer cells and tumour growth in mouse models. (oncolines.com)
Increased target residence time correlated with increased activity of TTK inhibitors in cancer cell line proliferation assays. (oncolines.com)
Although immune checkpoint inhibitors (ICIs), in particular blockade of PD-1/PD-L1, show promising therapy response in some cancers, they are less effective in PCa which may be poor infiltration of cytotoxic T-cells [ 7 - 9 ]. (thno.org)

EMT has also been shown to occur in wound healing, in organ fibrosis and in the initiation of metastasis in cancer progression. (wikipedia.org)
The breast cancer bone metastasis has activated TGF-β signaling, which contributes to the formation of these lesions. (wikipedia.org)
Breast cancer stem cells (BCSCs) play a critical role in chemoresistance, metastasis, and poor prognosis of breast cancer. (hindawi.com)
is known to exert anticancer effects, such as inducing cell cycle arrest, inhibiting metastasis, and overcoming immunotherapy resistance in breast cancer cells. (hindawi.com)
Metastasis is one of the most important challenges in cancer therapy strategies. (highwire.org)
1 Therefore, understanding the mechanisms of metastasis is a powerful weapon to increase the survival of patients with cancer and improve their quality of life. (highwire.org)
For the first time, Jean Claude used the term 'metastasis' as one of the most important hallmarks of cancer in 1829. (highwire.org)
Epithelial to mesenchymal transition (EMT) is one of the several processes, which is involved in metastasis, and development of drug resistance in cancer. (highwire.org)
Advances in Cancer Biology - Metastasis. (elsevierpure.com)

Also, active Wnt/beta-catenin pathway correlates with poor prognosis in breast cancer patients in the clinic. (wikipedia.org)
Breast cancer stem cells (BCSCs) are one of the main factors driving chemoresistance, thereby contributing to poor prognosis and clinical outcomes [ 3 - 5 ]. (hindawi.com)
Advanced prostate cancer (PCa) has limited treatment regimens and shows low response to chemotherapy and immunotherapy, leading to poor prognosis. (thno.org)

Dr. Multani has extensive expertise in the field of Human and Mammalian Cytogenetics, and specializes in the evaluation of genetic instability and complex chromosomal rearrangements in cancer cells, telomere dysfunction, characterization of embryonic stem cells, and authentication of cell lines. (mdanderson.org)

The tumor microenvironment (TME) promotes BCSC survival and cancer progression, and targeting the TME can aid in successful immunotherapy. (hindawi.com)
Survival for small cell lung cancer is low and how we treat the disease hasn't really changed over the last 20 years. (cancerresearchuk.org)

But these latest results, published in the journal Cancer Cell , suggest there may be further differences among the small cell tumours. (cancerresearchuk.org)
In human, aurora-A has focused a lot of attention, since its overexpression has been found to be correlated with the grade of various solid tumours. (lookformedical.com)
Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene. (lookformedical.com)

Tumors or cancers of the ADRENAL CORTEX. (ucdenver.edu)

The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)

We herein demonstrated that CADM1 interacts with Hippo pathway core kinases and enhances the phosphorylation of YAP1, and also that the membranous co-expression of CADM1 and LATS2 predicts a favorable prognosis in lung adenocarcinoma. (cancerindex.org)

Kinases are a class of enzyme that promote phosphorylation. (callaix.com)
Imatinib, for example, blocks a kinase receptor from binding to ATP, preventing the phosphorylation that would benefit the cancerous cell and promote cell division. (callaix.com)

Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)
Both inhibition of WDR5 by siRNA and OICR-9429 could reduce proliferation, and increase apoptosis and chemosensitivity to cisplatin in vitro and in vivo . (thno.org)

We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
New modalities that have immune cell therapy should be developed using chimeric antigen receptor (CAR)-T cells which is one of the most promising next-generation cancer therapies for hematological cancers, and with awaited practical application in AML. (bvsalud.org)

Activation of Wnt pathway in breast cancer cells induces the EMT regulator SNAIL and upregulates the mesenchymal marker, vimentin. (wikipedia.org)

When these kinases go wrong, normal cellular function can go awry. (callaix.com)

Data table showing topics related to specific cancers and associated disorders. (cancerindex.org)
This allows for targeted treatment of specific cancers , which lessens the risk of damage to healthy cells and increases treatment success. (callaix.com)

Wnt signaling pathway regulates EMT in gastrulation, cardiac valve formation and cancer. (wikipedia.org)

Background Aurora kinase A (AURKA) is amplified with varying occurrence in multiple human being cancers including mind and throat squamous cell carcinoma (HNSCC). (arcillaresearch.com)

In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. (xcessbio.com)
Drugs given to stop kinases can slow the proliferation of malignant cells and angiogenesis (growth of blood vessels). (callaix.com)
NTRC will also present a poster on OncolinesProfiler™, the comparative analysis of drug candidates in cancer cell line proliferation assays. (oncolines.com)

14 On the other hand, our recent investigation showed that ATG7 knock down and chemical inhibition of autophagy inhibit EMT and invasiveness of non-small cell lung cancer cells. (highwire.org)

3. State Key Laboratory of Oncology in South China & Collaborative Innovation Center of Cancer Medicine, Sun Yat-sen University Cancer Center, Guangzhou, 510060, China. (thno.org)

Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (oncotarget.com)

RAC1 Alterations Induce Acquired Dabrafenib Resistance in Association with Anaplastic Transformation in a Papillary Thyroid Cancer Patient. (mdanderson.org)

C, Berthon A, Drougat L, Kiseljak-Vassiliades K, Wierman ME, Faucz FR, Fa?a VM, Tone LG, Stratakis CA. Inhibition of Aurora kinase A activity enhances the antitumor response of beta-catenin blockade in human adrenocortical cancer cells. (ucdenver.edu)

These data indicate that APE1/Ref-1 is a key regulator of survivin and a potentially viable target in prostate cancer. (oncotarget.com)

Chemoresistance, or the insensitivity of cancer cells to drug therapy, is a major factor in the failure of chemotherapy against breast cancer. (hindawi.com)
its derivatives topotecan and irinotecan have already been used in pet models and medically to treat specific human TAK 165 malignancies [13], and various human cancers differ within their sensitivities to camptothecin-based chemotherapy [14, 15]. (arcillaresearch.com)

Breast cancer was the most prevalent cancer in 2020 (in terms of new cases) and the leading cause of cancer-related deaths among females [ 1 ]. (hindawi.com)

15 On the other hand, TGF-β can induce simultaneous autophagy and EMT in several cancer models, while TGF-β-induced autophagy is necessary for its EMT induction. (highwire.org)
20 On the other hand, NF-κB has a dual role in autophagy (inhibition and induction) by different mechanisms 14 which can negatively or positively regulate EMT and tumor invasion. (highwire.org)

Kinase deregulation can contribute to the growth of cancer. (callaix.com)

The altered expression of p63 isoforms reduced cell-cell adhesion and increased the migratory properties of cancer cells. (wikipedia.org)
Because APE1/Ref-1 is expressed and elevated in prostate cancer, we sought to characterize APE1/Ref-1 expression and activity in human prostate cancer cell lines and determine the effect of selective reduction-oxidation (redox) function inhibition on prostate cancer cells in vitro and in vivo . (oncotarget.com)
Feodoroff M, Mikkonen P, Turunen L, Hassinen A, Paasonen L, Paavolainen L, Potdar S, Murumägi A, Kallioniemi O, Pietiäinen V. Comparison of two supporting matrices for patient-derived cancer cells in 3D drug sensitivity and resistance testing assay (3D-DSRT). (helsinki.fi)
Feodoroff M, Mikkonen P, Arjama M, Murumägi A, Kallioniemi O, Potdar S, Turunen L, Pietiäinen V. Protocol for 3D Drug Sensitivity and Resistance Testing of Patient-Derived Cancer Cells in 384-Well Plates. (helsinki.fi)
A new study in mice suggests that a type of lung cancer could be split into two different diseases based on cells' molecular fingerprints. (cancerresearchuk.org)
It is paramount to identify predictive markers that are associated with failures of DNA maintenance in cancer cells. (nature.com)
This enables cancer cells to be more motile, have less extracellular matrix adhesion and be prone to detachment and moving toward distant organs. (highwire.org)
It has been suggested that radiation sensitivity and chemosensitivity of cancer cells may play an important role in the local control of the tumor following these therapies. (researchsquare.com)

40-fold more selective inhibitory activity for Aurora A compared with Aurora B. In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. (xcessbio.com)

2017). MYC Drives Progression of Small Cell Lung Cancer to a Variant Neuroendocrine Subtype with Vulnerability to Aurora Kinase Inhibition. (cancerresearchuk.org)

Prostate cancer (PCa) is the most commonly diagnosed malignancy and the second leading cause of male cancer-related death in the Western world [ 1 ]. (thno.org)

As part of our mission to eliminate cancer, MD Anderson researchers conduct hundreds of clinical trials to test new treatments for both common and rare cancers. (mdanderson.org)

In addition, bitter melon extract or its isolated ingredients have demonstrated noteworthy anticancer activity against skin, prostate, breast, colon, bladder, and pancreatic cancers in several preclinical investigations (Raina et al. (excli.de)

The p63 factor is involved in inhibiting EMT and reduction of certain p63 isoforms may be important in the development of epithelial cancers. (wikipedia.org)

Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)

According to the World Health Organization, breast cancer has the highest incidence rate in Indonesia, with a mortality rate of 22,692 cases per year [ 1 ]. (hindawi.com)

The inhibition profiles of 120 anti-cancer agents were compared, revealing 43 therapeutic clusters, many of them taken by novel therapies that were never part of any comparative profiling. (oncolines.com)

The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
Scientists are looking the possibility of kinase inhibition for other diseases including hypertension and Parkinson's disease but here we focus on cancer medicines. (callaix.com)

In vitro, awareness to camptothecin provides been shown to alter significantly within a -panel of breasts and cancer of the colon cell lines [17, 18]. (arcillaresearch.com)

Prostate cancer (PCa) is one of the most common male malignancies and the third leading cause of cancer-related death of men in the United States [ 1 - 2 ]. (oncotarget.com)
Prostate cancer (PCa) is a multifactorial disease with an unclear etiology. (mdpi.com)
A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. (xcessbio.com)
However, when the disease progresses to castration-resistant prostate cancer (CRPC), there are limited treatments for those patients and lead to dissatisfied outcomes [ 2 , 3 ]. (thno.org)

The findings suggest that the two types of small cell lung cancer could each be treated differently, according to the researchers from the Huntsman Cancer Institute (HCI) at the University of Utah in the US. (cancerresearchuk.org)
Lung cancers are usually defined as either small cell or non-small cell. (cancerresearchuk.org)
So these latest findings will help us work out how best to target them in small cell lung cancer. (cancerresearchuk.org)
There are no genetic tests available for small cell lung cancer patients to select different treatments, so they are all treated in much the same way, says Professor Trudy Oliver, an investigator at HCI who led the study. (cancerresearchuk.org)
This group, which is based on genetic differences, makes up around 1 in 5 patients with small cell lung cancer. (cancerresearchuk.org)

Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers. (xcessbio.com)

Since EMT in cancer progression recaptures EMT in developmental programs, many of the EMT-TFs are involved in promoting metastatic events. (wikipedia.org)

Cancers (Basel) 13(19), 2021. (mdanderson.org)

BACKGROUND: Solid organ transplant recipients are at increased risk for skin cancers due to immune-suppressive therapies. (bvsalud.org)
Cancer precision medicine draws on the presence of somatically acquired changes in the tumor, which serve as predictive markers of response to drugs and other therapies. (nature.com)

However, overexpression of aurora-A in particular cell lines such as NIH3T3 is sufficient to induce growth on soft agar. (lookformedical.com)

The Lyda Hill Cancer Prevention Center provides cancer risk assessment, screening and diagnostic services. (mdanderson.org)

In the HCT-116 tumor-bearing mice, MLN8054, administered orally at 3 mg/kg, 10 mg/kg, and 30 mg/kg once a day, leads to dose-dependent tumor growth inhibition (TGI: 76% and 84% for 10 mg/kg and 30 mg/kg). (xcessbio.com)

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