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Published in 2017 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2017.08.147
Abstract: Oncogenic KRas activity is central to several cancer types including pancreatic ductal adenocarcinoma (PDAC) but has been determined to be "undruggable". Recent studies have indicated that oncogenic KRas is not constitutively active but relies on…
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Keywords:
pdac;
oncogenic kras;
rage;
cancer ... See more keywords
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1
Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b01113
Abstract: RAS mutations are found in 30% of all human cancers, with KRAS the most frequently mutated among the three RAS isoforms (KRAS, NRAS, and HRAS). However, directly targeting oncogenic KRAS with small molecules in the…
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Keywords:
nucleotide binding;
oncogenic kras;
binding site;
small molecules ... See more keywords
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Published in 2025 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.5c00628
Abstract: This highlight outlines the development of novel imidazo-pyrimidine compounds as potent inhibitors targeting oncogenic KRAS mutations, including G12D, G12V, and G12C. The disclosure includes details on synthetic methods, biological evaluation, metabolic stability, and pharmaceutical compositions.
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Keywords:
oncogenic kras;
inhibition oncogenic;
pyrimidine compounds;
imidazo pyrimidine ... See more keywords
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1
Published in 2017 at "Journal of the American Chemical Society"
DOI: 10.1021/jacs.7b02988
Abstract: The Ras proteins are essential GTPases involved in the regulation of cell proliferation and survival. Mutated oncogenic forms of Ras alter effector binding and innate GTPase activity, leading to deregulation of downstream signal transduction. Mutated…
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Keywords:
total chemical;
variants oncogenic;
oncogenic kras;
chemical synthesis ... See more keywords
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Published in 2018 at "Nature Communications"
DOI: 10.1038/s41467-018-07472-8
Abstract: Oncogenic KRAS is the key driver of pancreatic ductal adenocarcinoma (PDAC). We previously described a role for KRAS in PDAC tumor maintenance through rewiring of cellular metabolism to support proliferation. Understanding the details of this…
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Keywords:
pdac;
oncogenic kras;
kras supports;
kras resistant ... See more keywords
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Published in 2024 at "Scientific Reports"
DOI: 10.1038/s41598-024-78333-2
Abstract: KRAS is one of the most frequently mutated oncogenes across various cancers. Oncogenic KRAS mutations rewire cellular signaling, leading to significant alterations in gene expression. RNA-binding proteins (RBPs) play a pivotal role in gene expression…
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Keywords:
oncogenic kras;
interaction dynamics;
rna interaction;
kras mutant ... See more keywords
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1
Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2113180119
Abstract: Significance We report a molecular brush-based oligonucleotide therapeutics platform which uniquely provides conjugated antisense oligonucleotides with binding selectivity, improved pharmacological properties, and an unusual biodistribution profile. These improvements lead to superior in vivo performance compared…
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Keywords:
conjugated antisense;
targeting oncogenic;
antisense oligonucleotides;
oncogenic kras ... See more keywords
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Published in 2018 at "Autophagy"
DOI: 10.1080/15548627.2018.1450708
Abstract: ABSTRACT Defects in basal autophagy limit the nutrient supply from recycling of intracellular constituents. Despite our understanding of the prosurvival role of macroautophagy/autophagy, how nutrient deprivation, caused by compromised autophagy, affects oncogenic KRAS-driven tumor progression…
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Keywords:
tumorigenesis;
oncogenic kras;
driven tumor;
autophagic reliance ... See more keywords
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1
Published in 2022 at "BMC Cancer"
DOI: 10.1101/2022.05.20.492866
Abstract: Background Alternative RNA splicing is widely dysregulated in cancers including lung adenocarcinoma, where aberrant splicing events are frequently caused by somatic splice site mutations or somatic mutations of splicing factor genes. However, the majority of…
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Keywords:
lung;
alternative splicing;
oncogenic kras;
cancer ... See more keywords
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Published in 2019 at "Cancer research"
DOI: 10.1158/0008-5472.can-18-3511
Abstract: Genetic and epigenetic changes (e.g., histone methylation) contribute to cancer development and progression, but our understanding of whether and how specific mutations affect a cancer's sensitivity to histone demethylase (KDM) inhibitors is limited. Here, we…
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Keywords:
gsk;
metabolic oxidative;
oncogenic kras;
cancer ... See more keywords
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1
Published in 2020 at "Immunology"
DOI: 10.1158/1538-7445.am2020-2575
Abstract: Changes in the mechanical microenvironment and mechanical signals are observed during tumor progression, malignant transformation, and metastasis. In this context, understanding the molecular details of mechanotransduction signaling may provide unique therapeutic targets. Here we report…
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Keywords:
nox2 generated;
oncogenic kras;
mechanoactivation nox2;
cancer ... See more keywords