BI 853520, a FAK-Simile of Prior FAK Inhibitors?
Sign Up to like & getrecommendations! Published in 2019 at "Targeted Oncology"
DOI: 10.1007/s11523-019-00621-z
Abstract: In this issue of Targeted Oncology, the BI 853520 investigators present three complementary studies of BI 853520 that investigate this drug in both Western and Eastern patient populations, as well as investigating the effects of… read more here.
Keywords: fak; kinase; defactinib; cancer ... See more keywords
High glucose/ox-LDL induced hepatic sinusoidal capillarization via αvβ5/FAK/ERK signaling pathway.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2019.04.082
Abstract: OBJECTIVE The main purpose of this study is to explore the role of integrin αvβ5 in hepatic sinusoidal capillarization under high glucose/ox-LDL conditions. METHODS Establish rat model of diabetic fatty liver disease. LSECs were extracted… read more here.
Keywords: hepatic sinusoidal; fak; sinusoidal capillarization; high glucose ... See more keywords
Inhibition of SRC/FAK cue: A novel pathway for the synergistic effect of rosuvastatin on the anti‐cancer effect of dasatinib in hepatocellular carcinoma
Sign Up to like & getrecommendations! Published in 2018 at "Life Sciences"
DOI: 10.1016/j.lfs.2018.10.002
Abstract: Purpose: Statins extended their hypocholestremic effect to show a promising anticancer activity. Hepatocellular carcinoma (HCC), the third common cause of cancer‐related death, responded positively to statins. Some in‐vitro studies reveal the rosuvastatin antitumor effect, but… read more here.
Keywords: hepatocellular carcinoma; rosuvastatin; fak; effect ... See more keywords
ADP ribosylation factor guanylate kinase 1 promotes the malignant phenotype of gastric cancer by regulating focal adhesion kinase activation.
Sign Up to like & getrecommendations! Published in 2021 at "Life sciences"
DOI: 10.1016/j.lfs.2021.119264
Abstract: AIMS ADP ribosylation factor guanylate kinase 1 (ASAP1), a phospholipid-dependent guanosine triphosphate (GTP)ase activating protein, has been reported to be involved in the development of various malignant tumors. However, the biological function of ASAP1 in… read more here.
Keywords: fak; kinase; malignant biological; biological behavior ... See more keywords
Cucurbitacin B suppresses metastasis mediated by reactive oxygen species (ROS) via focal adhesion kinase (FAK) in breast cancer MDA-MB-231 cells.
Sign Up to like & getrecommendations! Published in 2018 at "Chinese journal of natural medicines"
DOI: 10.1016/s1875-5364(18)30025-6
Abstract: Metastasis is responsible for the majority of cancer-related deaths and prevention of metastasis remains a big challenge for cancer therapy. Cucurbitacin B (Cuc B) is a natural triterpenoid with potent anticancer activities while its effect… read more here.
Keywords: mda 231; fak; adhesion; breast cancer ... See more keywords
Design, Synthesis, and Evaluation of Highly Potent FAK-Targeting PROTACs.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.9b00372
Abstract: Focal adhesion kinase (FAK), a cytoplasmic protein tyrosine kinase, exerts kinase-dependent enzymatic functions and kinase-independent scaffolding functions, both of which are crucial in cancer development, early embryonic development, and reproduction. However, previous efforts for FAK… read more here.
Keywords: highly potent; design synthesis; fak; evaluation highly ... See more keywords
Molecular Docking, Molecular Dynamics Simulations, and Free Energy Calculation Insights into the Binding Mechanism between VS-4718 and Focal Adhesion Kinase
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.2c03951
Abstract: Focal adhesion kinase (FAK) is a 125 kDa nonreceptor tyrosine kinase that plays an important role in many carcinomas. Thus, the targeting of FAK by small molecules is considered to be promising for cancer therapy.… read more here.
Keywords: molecular docking; fak; kinase; adhesion kinase ... See more keywords
Inhibition of the integrin/FAK signaling axis and c-Myc synergistically disrupts ovarian cancer malignancy
Sign Up to like & getrecommendations! Published in 2017 at "Oncogenesis"
DOI: 10.1038/oncsis.2016.86
Abstract: Integrins, a family of heterodimeric receptors for extracellular matrix, are promising therapeutic targets for ovarian cancer, particularly high-grade serous-type (HGSOC), as they drive tumor cell attachment, migration, proliferation and survival by activating focal adhesion kinase… read more here.
Keywords: signaling axis; integrin fak; fak; ovarian cancer ... See more keywords
The binding of DCC-P3 motif and FAK-FAT domain mediates the initial step of netrin-1/DCC signaling for axon attraction
Sign Up to like & getrecommendations! Published in 2017 at "Cell Discovery"
DOI: 10.1038/s41421-017-0008-8
Abstract: Netrin-1 plays a key role in axon guidance through binding to its receptor, Deleted in Colorectal Cancer (DCC). The initial step of signaling inside the cell after netrin-1/DCC ligation is the binding of DCC cytoplasmic… read more here.
Keywords: fat domain; fak; fat; netrin dcc ... See more keywords
Pericyte FAK negatively regulates Gas6/Axl signalling to suppress tumour angiogenesis and tumour growth
Sign Up to like & getrecommendations! Published in 2020 at "Nature Communications"
DOI: 10.1038/s41467-020-16618-6
Abstract: The overexpression of the protein tyrosine kinase, Focal adhesion kinase (FAK), in endothelial cells has implicated its requirement in angiogenesis and tumour growth, but how pericyte FAK regulates tumour angiogenesis is unknown. We show that… read more here.
Keywords: pericyte fak; fak; tumour growth; angiogenesis ... See more keywords
Design, synthesis, and biological evaluation of potent FAK-degrading PROTACs
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2022.2100886
Abstract: Abstract FAK mediated tumour cell migration, invasion, survival, proliferation and regulation of tumour stem cells through its kinase-dependent enzymatic functions and kinase-independent scaffolding functions. At present, the development of FAK PROTACs has become one of… read more here.
Keywords: design synthesis; synthesis biological; fak; biological evaluation ... See more keywords