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Products
Pharmacology
Type
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- Technical support
- Resources
BRC4wt
Cat. No. PP-390
Structure:
Ac-Leu-Leu-Gly-Phe-His-Thr-Ala-Ser-Gly-Lys-Lys-Val-Lys-Ile-Ala-Lys-NH2
Other Names:
BRC4 peptide
Activity:
Blocks BRCA2–RAD51 interaction
BRC4wt is a peptide derived from the BRC4 repeat motif of the BReast CAncer gene 2 (BRCA2) protein, which is able to prevent the DNA repair protein RAD51 binding to BRCA2. Cancer cells rely on efficient DNA repair to survive and proliferate and the BRCA2 tumour suppressor protein is indispensable for repair of DNA double-strand breaks through promotion of RAD51 loading onto single-stranded DNA. Through blockade of this interaction BRC4wt inhibits camptothecin and ionising radiation induced RAD51 foci formation and homologous recombination in cancer cells. BRC4wt can impair the replication fork-protective function of BRCA2 and trigger double-strand break repair protein MRE11 dependent degradation of nascent DNA in response to replication stress. A BRC4wt cell penetrating peptide derivative confers selective hypersensitivity to PARP inhibition in cancer cells but spares noncancerous cells, giving it potential as a radio and chemosensitiser.
Trenner et al (2018) A Short BRCA2-Derived Cell-Penetrating Peptide Targets RAD51 Function and Confers Hypersensitivity toward PARP Inhibition. Mol Cancer Ther. 17(7) 1392 PMID: 29654063
Related areas
All peptides >
All protein-protein interaction modulators >
All cancer research categories >
Technical Data
| Structure | Ac-Leu-Leu-Gly-Phe-His-Thr-Ala-Ser-Gly-Lys-Lys-Val-Lys-Ile-Ala-Lys-NH2 |
| Molecular Weight | 1738.06 |
| Formula | C81H139N23O19 |
| Sequence | Ac-LLGFHTASGKKVKIAK-NH2 |
| Modifications | N terminal acetyl, C terminal amide |
Solubility and Storage
| Solubility | Soluble in water |
| Appearance | Freeze dried sold |
| Storage | Store dry, frozen and in the dark |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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