Braftide
Description
Application Data
Description
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Braftide is an allosteric inhibitor of BRAF kinase activity, leading to BRAF degradation and downregulation of MAPK signalling.
Application Data
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Material Safety Data Sheet (MSDS)Catalogue number crb1001646 Molecular Weight 1241.7 Sequence (three letter code) Thr-Arg-His-Val-Asn-Ile-Leu-Leu-Phe-Met-amide
Storage -20°C Citations Beneker, (2021). Design and Synthesis of Macrocyclic Peptide BRAF-WT Dimerization Inhibitors for the Treatment of Metastatic Melanoma. University of South Carolina, USA.
Gunderwala et al., (2019). Development of Allosteric BRAF Peptide Inhibitors Targeting the Dimer Interface of BRAF. ACS Chem. Biol., 14(7): 1471. PMID: 31243962.
References Beneker, (2021). Design and Synthesis of Macrocyclic Peptide BRAF-WT Dimerization Inhibitors for the Treatment of Metastatic Melanoma. University of South Carolina, USA.
Gunderwala et al., (2019). Development of Allosteric BRAF Peptide Inhibitors Targeting the Dimer Interface of BRAF. ACS Chem. Biol., 14(7): 1471. PMID: 31243962.
BRAF dimers are a core component of the MAPK cascade to pass extracellular stimulus signalling to the nucleus. However, BRAF is also the most often mutated kinase in human cancers resulting in hyperactivation of signalling. BRAF inhibitors are thus a target for cancer therapy treatments.
Braftide is a decamer of BRAF sequence found in the dimer interface. It binds allosterically to BRAF preventing kinase activity of mono/dimeric forms. It also leads to the degradation of BRAF and downregulation of MAPK signalling. This creates an ideal dual function inhibitor of a key kinase in cancers such as metastatic melanoma.