A combinatorial strategy using YAP and pan-RAF inhibitors for treating KRAS-mutant pancreatic cancer.
Sign Up to like & getrecommendations! Published in 2017 at "Cancer letters"
DOI: 10.1016/j.canlet.2017.05.015
Abstract: KRAS mutation is the most common genetic event in pancreatic cancer. Whereas KRAS itself has proven difficult to inhibit, agents that target key downstream signals of KRAS, such as RAF, are possibly effective for pancreatic… read more here.
Keywords: using yap; pancreatic cancer; kras mutant; strategy using ... See more keywords
Discovery of New Imidazo[2,1-b]thiazole Derivatives as Potent Pan-RAF Inhibitors with Promising In Vitro and In Vivo Anti-melanoma Activity.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00230
Abstract: BRAF is an important component of MAPK cascade. Mutation of BRAF, in particular V600E, leads to hyperactivation of the MAPK pathway and uncontrolled cellular growth. Resistance to selective inhibitors of mutated BRAF is a major… read more here.
Keywords: melanoma; vivo; new imidazo; activity ... See more keywords
Pan-RAF inhibition induces apoptosis in acute myeloid leukemia cells and synergizes with BCL2 inhibition
Sign Up to like & getrecommendations! Published in 2020 at "Leukemia"
DOI: 10.1038/s41375-020-0972-0
Abstract: Pan-RAF inhibitors have shown promise as antitumor agents in RAS and RAF mutated solid cancers. However, the efficacy of pan-RAF inhibitors in acute myeloid leukemia (AML) has not previously been explored. In AML, the RAS–RAF–MEK–ERK… read more here.
Keywords: myeloid leukemia; inhibition; acute myeloid; raf inhibition ... See more keywords
Simultaneous blocking of the pan‐RAF and S100B pathways as a synergistic therapeutic strategy against malignant melanoma
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Cellular and Molecular Medicine"
DOI: 10.1111/jcmm.15994
Abstract: Melanoma is a very aggressive form of skin cancer. Although BRAF inhibitors have been utilized for melanoma therapy, advanced melanoma patients still face a low five‐year survival rate. Recent studies have shown that CRAF can… read more here.
Keywords: melanoma; raf; blocking pan; raf s100b ... 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 1742: Dual inhibitor of immunokinase and pan-RAF for the treatment of KRAS-mutated cancers
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-1742
Abstract: Tumor-associated macrophages (TAMs) represent most of the white blood cell population in solid tumors. TAMs usually display an M2-like phenotype due to signals from the tumor microenvironment, such as IL-10, VEGFA and CSF-1/M-CSF. These anti-inflammatory… read more here.
Keywords: inhibitor; sjp 1601; treatment; cancer ... See more keywords
Abstract 1627: PHI-501, a novel and potent pan-RAF inhibitor in metastatic melanoma
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-1627
Abstract: Background: PHI-501 has been developed as a novel inhibitor of NRAS mutated acute myeloid leukemia. Big data and artificial intelligence (AI)-based drug discovery platform and cell-based investigation identified PHI-501 repurposable against melanoma as a novel… read more here.
Keywords: cell; melanoma; inhibitor; pan raf ... See more keywords
Abstract 411: PHI-501, a novel pan-RAF/DDRs dual kinase inhibitor, overcomes BRAF or MEK inhibitor resistance in melanoma
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-411
Abstract: Background: PHI-501 is a newly developed, highly effective, and orally accessible dual inhibitor for pan-RAF and discoidin domain receptor (DDR) that is a collagen-activated receptor tyrosine kinase. Mutations of the BRAF and NRAS are the… read more here.
Keywords: pan raf; phi 501; inhibitor; melanoma ... See more keywords
Abstract 4927: Exarafenib (KIN-2787) is a potent, selective pan-RAF inhibitor with activity in preclinical models of BRAF class II/III mutant and NRAS mutant melanoma
Sign Up to like & getrecommendations! Published in 2023 at "Cancer Research"
DOI: 10.1158/1538-7445.am2023-4927
Abstract: Background: MAPK activating mutations are common in melanoma, with 40% of cases attributed to oncogenic BRAF mutations and 20-25% NRAS mutations. Secondary MAPK activation is a known resistance mechanism to approved BRAF inhibitors in BRAFV600… read more here.
Keywords: melanoma; kin 2787; pan raf; activity ... 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
Pan-RAF Inhibition Shows Anti-Leukemic Activity in RAS-Mutant Acute Myeloid Leukemia Cells and Potentiates the Effect of Sorafenib in Cells with FLT3 Mutation
Sign Up to like & getrecommendations! Published in 2020 at "Cancers"
DOI: 10.3390/cancers12123511
Abstract: Simple Summary We demonstrate that the pan-RAF inhibitor LY3009120 induces apoptosis and inhibits proliferation in AML cells harboring RAS or FLT3 mutations through action on the RAS/RAF/MEK/ERK and the AKT/mTOR pathways. Notably, pan-RAF inhibition combined… read more here.
Keywords: inhibition; sorafenib; aml cells; raf inhibition ... See more keywords