Results 91 to 100 of about 626,720 (343)

Combinatorial and fragment-based in silico design of PI3K-alpha natural hybrid antagonists for breast cancer therapeutics [PDF]

open access: yesExploration of Drug Science
Aim: The PI3K (phosphoinositide 3-kinase)-alpha isoform is found upregulated in 30–40% of breast cancer. Currently, there are limited selective and specific drugs that target PI3K-alpha, and no natural therapeutic option is available.
Navya Aggarwal   +2 more
doaj   +1 more source

Integrated genomic and proteomic profiling reveals insights into chemoradiation resistance in cervical cancer

open access: yesMolecular Oncology, EarlyView.
A comprehensive genomic and proteomic analysis of cervical cancer revealed STK11 and STX3 as a potential biomarkers of chemoradiation resistance. Our study demonstrated EGFR as a therapeutic target, paving the way for precision strategies to overcome treatment failure and the DNA repair pathway as a critical mechanism of resistance.
Janani Sambath   +13 more
wiley   +1 more source

Corilagin inhibits angiotensin II-induced atrial fibrosis and fibrillation in mice through the PI3K-Akt pathway [PDF]

open access: yesIranian Journal of Basic Medical Sciences
Objective(s): Corilagin (Cor) is reported as beiing hepatoprotective, anti-inflammatory, antibacterial, and anti-oxidant, while the effect on atrial fibrosis remains unknown.
Xiaogang Zhang   +3 more
doaj   +1 more source

Oncogenic pathway driven by p85β: upstream signals to activate p110

open access: yesMolecular & Cellular Oncology, 2020
The phosphatidylinositol 3-kinase (PI3K), which is composed of the p85 regulatory and p110 catalytic subunits, is known to be downstream of the receptor tyrosine kinase (RTK).
Ling Rao, Lydia W. T. Cheung
doaj   +1 more source

Tumor-stroma interactions influence the response to PI3K targeted agents in preclinical models of colorectal cancer (CRC) [PDF]

open access: yes, 2019
Introduction: One of the main obstacle to the successful development of therapeutic strategies remains the identification of biomarker underlying drug resistance. Recently, investigators have become more aware the role of the tumor microenvironment (TME)
Bazzichetto, Chiara
core  

First-in-Human Phase I Study to Evaluate the Brain-Penetrant PI3K/mTOR Inhibitor GDC-0084 in Patients with Progressive or Recurrent High-Grade Glioma. [PDF]

open access: yes, 2020
PurposeGDC-0084 is an oral, brain-penetrant small-molecule inhibitor of PI3K and mTOR. A first-in-human, phase I study was conducted in patients with recurrent high-grade glioma.Patients and methodsGDC-0084 was administered orally, once daily, to ...
Cloughesy, Timothy F   +11 more
core  

PYCR1 inhibition in bone marrow stromal cells enhances bortezomib sensitivity in multiple myeloma cells by altering their metabolism

open access: yesMolecular Oncology, EarlyView.
This study investigated how PYCR1 inhibition in bone marrow stromal cells (BMSCs) indirectly affects multiple myeloma (MM) cell metabolism and viability. Culturing MM cells in conditioned medium from PYCR1‐silenced BMSCs impaired oxidative phosphorylation and increased sensitivity to bortezomib.
Inge Oudaert   +13 more
wiley   +1 more source

The link between inhibition of PI3K signaling, induction of autophagy, and elimination of organelles to form the lens organelle-free zone

open access: yesAutophagy Reports, 2022
The elimination of organelles to create the lens organelle-free zone (OFZ) is a macroautophagy/autophagy-dependent mechanism that occurs without causing cell death.
A. Sue Menko
doaj   +1 more source

Early and late effects of pharmacological ALK inhibition on the neuroblastoma transcriptome [PDF]

open access: yes, 2017
Background: Neuroblastoma is an aggressive childhood malignancy of the sympathetic nervous system. Despite multi-modal therapy, survival of high-risk patients remains disappointingly low, underscoring the need for novel treatment strategies.
Cannoodt, Robrecht   +6 more
core   +3 more sources

The neural crest‐associated gene ERRFI1 is involved in melanoma progression and resistance toward targeted therapy

open access: yesMolecular Oncology, EarlyView.
ERRFI1, a neural crest (NC)‐associated gene, was upregulated in melanoma and negatively correlated with the expression of melanocytic differentiation markers and the susceptibility of melanoma cells toward BRAF inhibitors (BRAFi). Knocking down ERRFI1 significantly increased the sensitivity of melanoma cells to BRAFi.
Nina Wang   +8 more
wiley   +1 more source

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