3D-QSAR (CoMFA, CoMSIA, HQSAR and topomer CoMFA), MD simulations and molecular docking studies on purinylpyridine derivatives as B-Raf inhibitors for the treatment of melanoma cancer
Sign Up to like & getrecommendations! Published in 2019 at "Structural Chemistry"
DOI: 10.1007/s11224-019-01334-9
Abstract: As per the World Health Organization (WHO), cancer is the second most leading cause of death after cardiovascular diseases in worldwide with around 9.88 million total new cases and 1.08 million were observed due to… read more here.
Keywords: topomer comfa; cancer; raf inhibitors; comfa ... See more keywords
Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Cell"
DOI: 10.1016/j.ccell.2017.02.007
Abstract: Citation for published version: Girotti, MR, Lopes, F, Preece, N, Niculescu-Duvaz, D, Zambon, A, Davies, L, Whittaker, S, Saturno, G, Viros, A, Pedersen, M, Suijkerbuijk, BMJM, Menard, D, McLeary, R, Johnson, L, Fish, L, Ejiama,… read more here.
Keywords: also target; paradox breaking; raf inhibitors; breaking raf ... See more keywords
Classical RAS proteins are not essential for paradoxical ERK activation induced by RAF inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2113491119
Abstract: Significance RAF inhibitors unexpectedly induce ERK activation in normal and oncogenic RAS tumor cells, making them unsuitable for treating RAS-driven cancers. The precise mechanism of this paradox is not fully understood but is believed to… read more here.
Keywords: paradoxical erk; erk activation; raf; raf inhibitors ... See more keywords
On the development of B-Raf inhibitors acting through innovative mechanisms
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DOI: 10.12688/f1000research.108761.2
Abstract: B-Raf is a protein kinase participating to the regulation of many biological processes in cells. Several studies have demonstrated that this protein is frequently upregulated in human cancers, especially when it bears activating mutations. In… read more here.
Keywords: innovative mechanisms; competitive inhibitors; raf; raf inhibitors ... See more keywords