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Gene | BRAF |
Variant | N581S |
Impact List | missense |
Protein Effect | unknown |
Gene Variant Descriptions | BRAF N581S lies within the protein kinase domain of the Braf protein (UniProt.org). N581S has been identified as a secondary resistance mutation (PMID: 32553555), and results in intermediate Braf kinase activity (PMID: 15035987) as well as low Braf kinase activity (PMID: 28783719), and results in Ras-dependent activation of Erk signaling in cell culture (PMID: 28783719), however in another study, demonstrates increased transformation ability in one of two different cell lines compared to wild-type Braf (PMID: 29533785), and therefore, its effect on Braf protein function is unknown. |
Associated Drug Resistance | Y |
Category Variants Paths |
BRAF mutant BRAF N581X BRAF N581S |
Transcript | NM_004333.6 |
gDNA | chr7:g.140753393T>C |
cDNA | c.1742A>G |
Protein | p.N581S |
Source Database | RefSeq |
Genome Build | GRCh38/hg38 |
Transcript | gDNA | cDNA | Protein | Source Database | Genome Build |
---|---|---|---|---|---|
NM_004333 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_001378468.1 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_004333.5 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_001354609.2 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_004333.6 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_001354609.1 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
NM_001378474.1 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
XM_005250045 | chr7:g.140753393T>C | c.1742A>G | p.N581S | RefSeq | GRCh38/hg38 |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
BRAF N581S | lung adenocarcinoma | predicted - sensitive | PF-00477736 + PF3644022 | Preclinical - Patient cell culture | Actionable | In a preclinical study, Chk1 inhibitor PF-477736 and MK2 inhibitor PF3644022 combination treatment resulted in significant apoptosis in primary tumor cells isolated from a lung adenocarcinoma patient harboring BRAF N581S in culture (PMID: 26140595). | 26140595 |
BRAF N581S | Advanced Solid Tumor | no benefit | Vemurafenib | Clinical Study - Cohort | Actionable | In a Phase II trial (MyPathway), Zelboraf (vemurafenib) treatment resulted in an objective response in only 4% (1/23) of patient with advanced solid tumors harboring non-V600 BRAF mutations, 2 of the non-responding patients harbored BRAF N581S (PMID: 29320312; NCT02091141). | 29320312 |
BRAF N581S | lung non-small cell carcinoma | no benefit | Vemurafenib | Case Reports/Case Series | Actionable | In a Phase II trial, Zelboraf (vemurafenib) treatment did not result in response in the cohort of 15 non-small cell lung cancer patients with non-V600 BRAF mutations, which included 3 patients harboring BRAF N581S, and enrollment in this cohort was discontinued (PMID: 31959346; NCT02304809). | 31959346 |
BRAF N581S | female reproductive organ cancer | no benefit | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment did not demonstrate clinical activity in patients with advanced solid tumors or lymphoma harboring BRAF fusion or non-V600 mutations, resulted in stable disease in a patient with gynecologic cancer harboring BRAF N581S (PMID: 31924734; NCT02465060). | 31924734 |
BRAF N581S | lung adenocarcinoma | no benefit | Trametinib | Case Reports/Case Series | Actionable | In a Phase II trial (NCI-MATCH), Mekinist (trametinib) treatment did not demonstrate clinical activity in patients with advanced solid tumors or lymphoma harboring BRAF fusion or non-V600 mutations, resulted in progressive disease in a patient with lung adenocarcinoma harboring BRAF N581S (PMID: 31924734; NCT02465060). | 31924734 |
BRAF N581S | colorectal cancer | not predictive | Cetuximab + Fluorouracil + Irinotecan + Leucovorin | Case Reports/Case Series | Actionable | In a clinical study, the combination of Erbitux (cetuximab) with FOLFIRI as a first-line therapy resulted in a partial response with progression-free survival lasting 16 months in a patient with metastatic colorectal cancer harboring BRAF N581S (PMID: 31515458). | 31515458 |