AZ304, a novel dual BRAF inhibitor, exerts anti-tumour effects in colorectal cancer independently of BRAF genetic status

2 views | Apr 29 2021

Rui Ma et al. found that the BRAF inhibitor AZ304 had broad spectrum antitumour activity, which was significantly enhanced by combination with Cetuximab in colorectal cancers in vitro and in vivo. [Read the Full Post]

Mini review: The FDA-approved prescription drugs that target the MAPK signaling pathway in women with breast cancer

2 views | Apr 28 2021

Fatemeh Khojasteh Poor et al. summarized the FDA-approved prescription drugs that targeted the MAPK signaling pathway in women with BC. [Read the Full Post]

Combined blockade of polo-like kinase and pan-RAF is effective against NRAS-mutant non-small cell lung cancer cells

2 views | Apr 28 2021

Siyeon Park et al. found that human NRAS-mutant NSCLC cells were moderately sensitive to pan-RAF inhibitors. [Read the Full Post]

LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors

7 views | Apr 01 2021

Kelli-Ann Monaco et al. found that LXH254 was a novel RAF inhibitor, which was able to inhibit dimerized BRAF and CRAF, as well as monomeric BRAF, while largely sparing ARAF. [Read the Full Post]

Reversal of Cancer Multidrug Resistance (MDR) Mediated by ATP-Binding Cassette Transporter G2 (ABCG2) by AZ-628, a RAF Kinase Inhibitor

8 views | Mar 16 2021

Jing-Quan Wang et al. indicated that AZ-628 could be used in combination chemotherapy against ABCG2-mediated MDR in cancers. [Read the Full Post]

BRAF paradox breakers PLX8394, PLX7904 are more effective against BRAFV600Ε CRC cells compared with the BRAF inhibitor PLX4720 and shown by detailed pathway analysis

20 views | Jan 06 2021

Kassandra Koumaki et al. showed that the BRAF paradox breakers PLX7904 and PLX8394 caused a more prolonged MAPK pathway inhibition and achieved a stronger blockage of proliferation and reduced viability than PLX4720, the sister compound of Vemurafenib. [Read the Full Post]

Targeting of BCR-ABL1 and IRE1α induces synthetic lethality in Philadelphia-positive acute lymphoblastic leukemia

0 views | Nov 01 2020

Margherita Vieri et al. found that the identified combined action of nilotinib and MKC-8866 might represent a successful therapeutic strategy in high-risk Ph + ALL. [Read the Full Post]

Selective targeting of the αC and DFG-out pocket in p38 MAPK

29 views | Nov 01 2020

Sandra Röhm et al. provided valuable insights into back-pocket interactions that were not addressed in SR-318 and it provided an alternative chemical tool with good cellular activity targeting also the p38 back pocket. [Read the Full Post]

Regorafenib for Metastatic Colorectal Cancer: An Analysis of a Registry-Based Cohort of 555 Patients

134 views | Aug 06 2020

Alena Novakova-Jiresova ETAL. found that regorafenib was a safe and active treatment option for a subgroup of patients with mCRC who were progressing after other systemic therapies and maintain good performance status. [Read the Full Post]

The Anti-Cancer Drug Dabrafenib Is a Potent Activator of the Human Pregnane X Receptor

74 views | Jul 19 2020

Nicolas Creusot et al. revealed that by using a panel of different cellular techniques it was possible to improve the assessment of hPXR agonist activity for new developed drugs. [Read the Full Post]