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B-Raf is a 766-amino acid, regulated signal transduction serine/threonine-specific protein kinase.Broadly speaking, it is composed of three conserved domains characteristic of the Raf kinase family: conserved region 1 (CR1), a Ras-GTP-binding [11] self-regulatory domain, conserved region 2 (CR2), a serine-rich hinge region, and conserved region 3 (CR3), a catalytic protein kinase domain that ...
Treatment of adults with locally advanced, unresectable (stage III) non-small cell lung cancer (NSCLC) whose disease has not progressed during or following concurrent or sequential platinum-based chemoradiation therapy and whose tumors have EGFR exon 19 deletions or exon 21 L858R mutations, as detected by an FDA-approved test [2]
BRAF kinase inhibitor. BRAF kinase mutation V600E-positive Metastatic melanoma. Skin reactions, secondary malignancies (mostly squamous cell carcinoma), anaphylaxis (rare) and hypotension (rare). Abbreviations/Acronyms: IM – Intramuscular. IV – Intravenous. IA – Intra-arterial. SC – Subcutaneous. PO – Per os, oral. IP – Intrapleural.
Vemurafenib only works in melanoma patients whose cancer has a V600E BRAF mutation (that is, at amino acid position number 600 on the B-Raf protein, the normal valine is replaced by glutamic acid). [4] About 60% of melanomas have this mutation. It also has efficacy against the rarer V600K BRAF (the normal valine is replaced by lysine) mutation ...
V600E is a mutation of the BRAF gene in which valine (V) is substituted by glutamic acid (E) at amino acid 600. [1] [2] It is a driver mutation in a proportion of certain diagnoses, including melanoma, [3] [4] hairy cell leukemia, [5] [6] papillary thyroid carcinoma, [7] [8] colorectal cancer, [9] non-small-cell lung cancer, [10] [11] Langerhans cell histiocytosis, [12] Erdheim–Chester ...
10673 24099 Ensembl ENSG00000102524 ENSMUSG00000031497 UniProt Q9Y275 Q9WU72 RefSeq (mRNA) NM_001145645 NM_006573 NM_033622 NM_001347309 RefSeq (protein) NP_001139117 NP_006564 NP_001334238 NP_296371 Location (UCSC) Chr 13: 108.25 – 108.31 Mb Chr 8: 10.06 – 10.09 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse B-cell activating factor (BAFF) also known as tumor necrosis factor ...
Germline mutations in drug targets can also influence response to medications, though this is an emerging subfield within pharmacogenomics. One well-established gene-drug interaction involving a germline mutation to a drug target is warfarin (Coumadin) and VKORC1, which codes for vitamin K epoxide reductase (VKOR).
For example, Erbitux increases the survival rate of colorectal cancer patients if they carry a particular mutation in the EGFR gene. [19] Some drugs are specifically approved for certain genotypes. Vemurafenib is such a case which is used for melanoma patients who carry a mutation in the BRAF gene. [19]