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Raf

Clonorchis sinensis ESPs enhance the activation of hepatic stellate cells by a cross-talk of TLR4 and TGF-β/Smads Signaling pathway

3 views | Jan 17 2020

Li B et al. demonstrated that activation of HSCs caused by CsESPs is mediated by a cross-talk between TLR4 and TGF-β/Smads signaling pathway, and may be provide a potential treatment strategy to interrupt the process of liver fibrosis caused by C. sinensis. [Read the Full Post]

VCAM-1 Upregulation Contributes to Insensitivity of Vemurafenib in BRAF-Mutant Thyroid Cancer

7 views | Jan 09 2020

Chen S et al. demonstrated that VCAM-1 is upregulated in thyroid cancer cells treated with vemurafenib and contributes to vemurafenib resistance in BRAF-mutant thyroid cancer cells. [Read the Full Post]

Glucocorticoid receptor antagonism overcomes resistance to BRAF inhibition in BRAFV600E-mutated metastatic melanoma

6 views | Jan 09 2020

Estrela JM et al. found that melanoma resistance is decreased if AKT and NF-κB signaling pathways are blocked. [Read the Full Post]

Effects of pharmacogenetic variants on vemurafenib-related toxicities in patients with melanoma

11 views | Dec 31 2019

Goey AK found that genetic variants in CYP3A4 and ABCB1 are associated with vemurafenib-associated toxicities. [Read the Full Post]

Adjuvant Dabrafenib plus Trametinib in Stage III BRAF-Mutated Melanoma

62 views | Sep 25 2019

Long GV et al. indicated that adjuvant use of combination therapy with dabrafenib plus trametinib resulted in a significantly lower risk of recurrence in patients with stage III melanoma with BRAF V600E or V600K mutations than the adjuvant use of placebo and was not associated with new toxic effects. [Read the Full Post]

Genome-scale transcriptional activation by an engineered CRISPR-Cas9 complex

60 views | Sep 24 2019

Konermann S et al. demonstrated the potential of Cas9-based activators as a powerful genetic perturbation technology. [Read the Full Post]

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models

75 views | Aug 29 2019

Yang H et al. indicated their findings offer evidence of the potent antitumor activity of RG7204 against melanomas harboring the mutant BRAF(V600E) gene. [Read the Full Post]

Reversal of sorafenib resistance in hepatocellular carcinoma: epigenetically regulated disruption of 14-3-3η/hypoxia-inducible factor-1α

69 views | Jul 26 2019

Qiu Y et al. indicated that miR-16/14-3-3η is involved in sorafenib resistance in HCC and that these two factors could be potential therapeutic targets and biomarkers for predicting the response to sorafenib treatment. [Read the Full Post]

A high-performance liquid chromatography-tandem mass spectrometry method for the determination of lifrafenib, a novel RAF kinase and EGFR inhibitor, in human plasma and urine and its application in clinical pharmacokinetic study

159 views | Jul 01 2019

Yao X et al. showed robust and sensitive, it successfully fulfilled the requirement of clinical pharmacokinetic study of lifirafenib in Chinese patients with locally advanced or metastatic solid tumors. [Read the Full Post]

Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic

60 views | Jun 28 2019

Ramurthy S et al. indicated that a structure-based approach led to a pyridine series with an alcohol side chain that could interact with the DFG loop and significantly improved cell potency. Further mitigation of human intrinsic clearance and time-dependent inhibition led to the discovery of 15. Due to its excellent properties, it was progressed through toxicology studies and is being tested in phase 1 clinical trials. [Read the Full Post]