Metabolic targeting synergizes with MAPK inhibition and delays drug resistance in melanoma.
Sign Up to like & getrecommendations! Published in 2019 at "Cancer letters"
DOI: 10.1016/j.canlet.2018.11.018
Abstract: Tumors, including melanomas, frequently show an accelerated glucose metabolism. Mutations in the v-Raf murine sarcoma viral oncogene homolog B (BRAF), detected in about 50% of all melanomas, result in further enhancement of glycolysis. Therefore anti-metabolic… read more here.
Keywords: melanoma; targeting synergizes; metabolic targeting; resistance ... See more keywords
The stability of R-spine defines RAF inhibitor resistance: A comprehensive analysis of oncogenic BRAF mutants with in-frame insertion of αC-β4 loop
Sign Up to like & getrecommendations! Published in 2021 at "Science Advances"
DOI: 10.1126/sciadv.abg0390
Abstract: The stabilized R-spine of oncogenic BRAF mutants impairs RAF inhibitor association and confers drug resistance. Although targeting BRAF mutants with RAF inhibitors has achieved promising outcomes in cancer therapy, drug resistance remains a remarkable challenge,… read more here.
Keywords: braf mutants; braf; oncogenic braf; resistance ... See more keywords
Abstract 5160: Development of REDX05358, a novel highly selective and potent pan RAF inhibitor and a potential therapeutic for BRAF and RAS mutant tumors
Sign Up to like & getrecommendations! Published in 2017 at "Cancer Research"
DOI: 10.1158/1538-7445.am2017-5160
Abstract: REDX05358 has been identified as a novel, highly selective and potent next generation pan RAF inhibitor with improved therapeutic potential and predicted safety profile. Aberrant signalling via the MAPK pathway is commonly seen in cancer.… read more here.
Keywords: braf; ras mutant; braf ras; raf inhibitor ... See more keywords
Abstract CT032: Trials in progress: a global phase 1/1b clinical trial evaluating exarafenib (KIN-2787), a highly selective pan-RAF inhibitor, in adult patients with BRAF-altered solid tumors and NRAS mutant melanoma
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-ct032
Abstract: Background: Patients with cancers driven by BRAF Class II (C II) or C III alterations and/or NRAS mutations are unlikely to benefit from approved BRAF-targeted therapies and have few other treatment options. Exarafenib is a… read more here.
Keywords: raf inhibitor; solid tumors; evaluating exarafenib; pan raf ... See more keywords