POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative
Por um escritor misterioso
Last updated 17 julho 2024
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.por-journal.com/files/Articles/1611038/pore-29-1611038-HTML-r2/image_m/pore-29-1611038-g005.jpg)
CVM-1118 (foslinanib) is a phosphoric ester compound selected from 2-phenyl-4-quinolone derivatives. The NCI 60 cancer panel screening showed CVM-1125, the major active metabolite of CVM-1118, to exhibit growth inhibitory and cytotoxic effects at nanomolar range. CVM-1118 possesses multiple bioactivities, including inducing cellular apoptosis, cell cycle arrest at G2/M, as well as inhibiting vasculogenic mimicry (VM) formation. The TNF receptor associated protein 1 (TRAP1) was identified as the binding target of CVM-1125 using nematic protein organization technique (NPOT) interactome analysis. Further studies demonstrated CVM-1125 reduced the protein level of TRAP1 and impeded its downstream signaling by reduction of cellular succinate levels and destabilization of HIF-1α. The pharmacogenomic biomarkers associated with CVM-1118 were also examined by Whole Genome CRISPR Knock-Out Screening. Two hits (STK11 and NF2) were confirmed with higher sensitivity to the drug in cell knock-down experiments. Biological assays indicate that the mechanism of action of CVM-1118 is via targeting TRAP1 to induce mitochondrial apoptosis, suppress tumor cell growth, and inhibit vasculogenic mimicry formation. Most importantly, the loss-of-function mutations of STK11 and NF2 are potential biomarkers of CVM-1118 which can be applied in the selection of cancer patients for CVM-1118 treatment. CVM-1118 is currently in its Phase 2a clinical development.
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.tandfonline.com/cms/asset/55aee63e-5b10-4e59-b8c7-ba0d662719e6/iedc_a_2246366_f0004a_oc.jpg)
Full article: Developing our knowledge of the quinolone scaffold and its value to anticancer drug design
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.researchgate.net/profile/Dawn-Kirschmann-2/publication/223986776/figure/fig1/AS:305177090379778@1449771296753/figure-fig1_Q320.jpg)
Richard E. B. Seftor's research works Shepherd University, Shepherdstown and other places
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.researchgate.net/publication/326558657/figure/fig2/AS:651602608275457@1532365576756/Nematic-protein-organisation-technique-NPOT-for-interactome-analysis-of-evodiamine-a.png)
Nematic protein organisation technique (NPOT) for interactome analysis
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://pub-med-central-images-cdn.bioz.com/pub_med_central_ids_ending_with_4716/pmc10354716/pmc10354716__dmm-16-049930-g2.jpg)
Lkb1 (Qiagen), Bioz
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.researchgate.net/publication/348885218/figure/tbl1/AS:996408245121024@1614573646472/Most-frequently-comutated-genes-with-STK11-in-non-small-cell-lung-cancer-according-to.png)
Most frequently comutated genes with STK11 in non-small cell lung
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.frontiersin.org/files/MyHome%20Article%20Library/1296456/1296456_Thumb_400.jpg)
Frontiers The development of cancers research based on mitochondrial heat shock protein 90
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://media.springernature.com/lw685/springer-static/image/art%3A10.1007%2Fs11030-019-09952-5/MediaObjects/11030_2019_9952_Sch10_HTML.png)
4-Hydroxy-2-quinolones: syntheses, reactions and fused heterocycles
![POR CVM-1118 (foslinanib), a 2-phenyl-4-quinolone derivative](https://www.researchgate.net/profile/Yi-Fong-Chen-3/publication/267696543/figure/fig21/AS:1184687749898240@1659462978646/Alkylation-of-4-hydroxyquinolin-21H-ones-A-Tautomerism-of_Q320.jpg)
Li-Chen Chou's research works China Medical University (ROC), Taichung and other places
2-Phenylquinolin-4-ol, C15H11NO
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