FAK inhibitors induce cell multinucleation and dramatically increase pro‐tumoral cytokine expression in RAW 264.7 macrophages
Sign Up to like & getrecommendations! Published in 2017 at "FEBS Letters"
DOI: 10.1002/1873-3468.12895
Abstract: Macrophages are abundant in the tumor microenvironment. They are highly plastic and able to acquire pro‐tumoral phenotypes in response to microenvironmental stimuli. When we treated RAW 264.7 macrophages with inhibitors of various oncogenic pathways, we… read more here.
Keywords: raw 264; fak inhibitors; cell multinucleation; pro tumoral ... See more keywords
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
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2.
Sign Up to like & getrecommendations! Published in 2021 at "Cell chemical biology"
DOI: 10.1016/j.chembiol.2021.01.003
Abstract: There is increasing evidence of a significant correlation between prolonged drug-target residence time and increased drug efficacy. Here, we report a structural rationale for kinetic selectivity between two closely related kinases: focal adhesion kinase (FAK)… read more here.
Keywords: kinetic selectivity; fak inhibitors; structure kinetic; selectivity ... See more keywords
Design, synthesis, biological evaluation and molecular docking study of novel thieno[3,2-d]pyrimidine derivatives as potent FAK inhibitors.
Sign Up to like & getrecommendations! Published in 2019 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2019.112024
Abstract: A series of 2,7-disubstituted-thieno[3,2-d]pyrimidine derivatives were designed, synthesized and evaluated as novel focal adhesion kinase (FAK) inhibitors. The novel 2,7-disubstituted-thieno[3,2-d]pyrimidine scaffold has been designed as a new kinase inhibitor platform that mimics the bioactive conformation… read more here.
Keywords: mda 231; compound 26f; pyrimidine derivatives; thieno pyrimidine ... See more keywords
Design, Synthesis, and Biological Evaluation of 4-Arylamino Pyrimidine Derivatives as FAK Inhibitors and Tumor Radiotracers.
Sign Up to like & getrecommendations! Published in 2022 at "Molecular pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.2c00180
Abstract: Focal adhesion kinase (FAK) is considered a promising target for the diagnosis and treatment of cancer. In this work, a series of N,N'-(4-((5-bromo-2-(phenylamino)pyrimidin-4-yl)amino)-1,3-phenylene)diacetamide derivatives were synthesized and evaluated as FAK inhibitors and radiotracers. The studied… read more here.
Keywords: design synthesis; synthesis biological; fak inhibitors; biological evaluation ... See more keywords
Phase I study of defactinib combined with pembrolizumab and gemcitabine in advanced cancer.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.2017.35.4_suppl.tps505
Abstract: TPS505Background: Focal adhesion kinase (FAK) is consistently hyperactivated in pancreatic ductal adenocarcinoma (PDAC), and FAK signaling is a key driver in forming its fibrotic and proinflammatory tumor microenvironment. Inhibition of FAK signaling leads to significant… read more here.
Keywords: fak; defactinib; phase study; fak inhibitors ... See more keywords
New insights on Fak and Fak inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Current medicinal chemistry"
DOI: 10.2174/0929867327666201103162239
Abstract: BACKGROUND Focal adhesion kinase (Fak) is a cytoplasmic protein tyrosine kinase overexpressed and activated in different solid cancer; it showed important role in metastasis formation, cell migration, invasion and angiogenesis and consequently it has been… read more here.
Keywords: chemical scaffolds; chemistry; insights fak; new insights ... See more keywords
The Development of FAK Inhibitors: A Five-Year Update
Sign Up to like & getrecommendations! Published in 2022 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms23126381
Abstract: Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase over-expressed in different solid cancers. In recent years, FAK has been recognized as a new target for the development of antitumor agents, useful to contrast tumor… read more here.
Keywords: fak inhibitors; development; development fak; inhibitors five ... See more keywords
Drug Discovery Targeting Focal Adhesion Kinase (FAK) as a Promising Cancer Therapy
Sign Up to like & getrecommendations! Published in 2021 at "Molecules"
DOI: 10.3390/molecules26144250
Abstract: FAK is a nonreceptor intracellular tyrosine kinase which plays an important biological function. Many studies have found that FAK is overexpressed in many human cancer cell lines, which promotes tumor cell growth by controlling cell… read more here.
Keywords: phase; promising cancer; fak; fak inhibitors ... See more keywords