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Raf

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

11 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

22 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

127 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

67 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]

A TLR7 agonist strengthens T and NK cell function during BRAF-targeted therapy in a preclinical melanoma model

72 views | Jul 16 2020

Lydia Bellmann found that combined BRAFi with an immune stimulating agent such as a TLR ligand could be a promising alternative approach for the treatment of melanoma. [Read the Full Post]

HO-1 Downregulation Favors BRAF V600 Melanoma Cell Death Induced by Vemurafenib/PLX4032 and Increases NK Recognition

116 views | Jun 13 2020

Anna L Furfaro et al. indicated that HO-1 downregulation can both improve the efficacy of Vemurafenib on melanoma cells and favor melanoma susceptibility to NK cell-mediated recognition and killing. [Read the Full Post]

Ocular Side Effects of Target Therapy and Immunotherapy in Patients With Cutaneous Malignant Melanoma

92 views | Jun 07 2020

Jennifer Eikenberry et al. highlighted the frequency of ocular side effects in patients treated with target therapy and immunotherapy for CMM and showed that symptom resolution could be effectively achieved with proper ophthalmic care. [Read the Full Post]

Severe pyrexia from nivolumab-resistant advanced melanoma after successful combined therapy with encorafenib plus binimetinib.

0 views | May 04 2020

Amagai R et al. suggested that pyrexia caused by BRAF/MEK inhibitors may possess a similar pathophysiology as that of AOSD. [Read the Full Post]

Skin toxicity and efficacy of sunitinib and sorafenib in metastatic renal cell carcinoma: a national registry-based study

139 views | Feb 09 2020

Poprach A et al. found that the presence of skin toxicity is associated with improved OS and PFS in patients with mRCC treated with sunitinib. [Read the Full Post]