Discovery of Clinically Used Octenidine as NRAS Repressor That Effectively Inhibits NRAS-Mutant Melanoma.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c00094
Abstract: Mutations in NRAS promote tumorigenesis and drug resistance. As this protein is often considered an undruggable target, it is urgent to develop novel strategies to suppress NRAS for anticancer therapy. Recent reports indicated that a… read more here.
Keywords: discovery clinically; mutant melanoma; nras mutant; nras repressor ... See more keywords
The lincRNA MIRAT binds to IQGAP1 and modulates the MAPK pathway in NRAS mutant melanoma
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-27643-3
Abstract: Despite major advances in targeted melanoma therapies, drug resistance limits their efficacy. Long noncoding RNAs (lncRNAs) are transcriptome elements that do not encode proteins but are important regulatory molecules. LncRNAs have been implicated in cancer… read more here.
Keywords: nras mutant; mutant melanoma; mapk pathway; modulates mapk ... See more keywords
BRAF Inhibitors Amplify the Proapoptotic Activity of MEK Inhibitors by Inducing ER Stress in NRAS-Mutant Melanoma
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DOI: 10.1158/1078-0432.ccr-17-0098
Abstract: Purpose: NRAS mutations in malignant melanoma are associated with aggressive disease requiring rapid antitumor intervention, but there is no approved targeted therapy for this subset of patients. In clinical trials, the MEK inhibitor (MEKi) binimetinib… read more here.
Keywords: melanoma; nras mutant; mutant melanoma; braf ... See more keywords
Phase Ib/II Trial of Ribociclib in Combination with Binimetinib in Patients with NRAS-mutant Melanoma
Sign Up to like & getrecommendations! Published in 2022 at "Clinical Cancer Research"
DOI: 10.1158/1078-0432.ccr-21-3872
Abstract: Abstract Purpose: Enhanced MAPK pathway signaling and cell-cycle checkpoint dysregulation are frequent in NRAS-mutant melanoma and, as such, the regimen of the MEK inhibitor binimetinib and the selective CDK4/6 inhibitor ribociclib is a rational combination.… read more here.
Keywords: patients nras; phase; combination; mutant melanoma ... See more keywords
Abstract 4108: Longitudinal diffusion-weighted MRI assessment of NRAS mutant melanoma response to dual RAF-MEK inhibition reveals differences associated with collagen deposition
Sign Up to like & getrecommendations! Published in 2018 at "Cancer Research"
DOI: 10.1158/1538-7445.am2018-4108
Abstract: Background and Purpose: Oncogenic NRAS, which drives the constitutive activation of the RAS-RAF-MEK-ERK pathway, is expressed in 15–20% of melanomas and is the second most common driver mutation in this disease. Inhibition of oncogenic RAS… read more here.
Keywords: nras mutant; diffusion; diffusion weighted; dual raf ... 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
Initial Evidence for the Efficacy of Naporafenib in Combination With Trametinib in NRAS-Mutant Melanoma: Results From the Expansion Arm of a Phase Ib, Open-Label Study
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Clinical Oncology"
DOI: 10.1200/jco.22.02018
Abstract: PURPOSE No approved targeted therapy for the treatment of patients with neuroblastoma RAS viral (v-ras) oncogene homolog (NRAS)–mutant melanoma is currently available. PATIENTS AND METHODS In this phase Ib escalation/expansion study (ClinicalTrials.gov identifier: NCT02974725), the… read more here.
Keywords: plus trametinib; expansion; mutant melanoma; nras mutant ... See more keywords
MEK inhibitors for the treatment of NRAS mutant melanoma
Sign Up to like & getrecommendations! Published in 2018 at "Drug Design, Development and Therapy"
DOI: 10.2147/dddt.s131721
Abstract: Melanoma is increasing rapidly in incidence and prevalence, especially in younger females and older males. Treatment options have expanded beyond high-dose interleukin 2 and adoptive T-cell therapy to include inhibitors of immune checkpoints programmed death… read more here.
Keywords: melanoma; nras mutant; mutant melanoma; treatment ... See more keywords
Current Perspectives and Novel Strategies of NRAS-Mutant Melanoma
Sign Up to like & getrecommendations! Published in 2021 at "OncoTargets and therapy"
DOI: 10.2147/ott.s278095
Abstract: Abstract Melanoma is the deadliest cutaneous cancer. Activating mutations in NRAS are found in 20% of melanomas. NRAS-mutant melanoma is more aggressive and, therefore, has poorer outcomes, compared to non-NRAS-mutant melanoma. Despite promising preclinical data,… read more here.
Keywords: mek inhibitors; nras mutant; melanoma; mutant melanoma ... See more keywords
Efficacy of Targeted Radionuclide Therapy Using [131I]ICF01012 in 3D Pigmented BRAF- and NRAS-Mutant Melanoma Models and In Vivo NRAS-Mutant Melanoma
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DOI: 10.3390/cancers13061421
Abstract: Simple Summary Targeted radionuclide therapy (TRT) aims to selectively deliver radioactive molecules to tumor cells. For this purpose, we deliver iodine-131 ([131I]) to melanoma cells by using our laboratory-developed melanin specific radiotracer, the ICF01012. Approximately… read more here.
Keywords: melanoma; nras mutant; 131i icf01012; mutant melanoma ... See more keywords