2232233-39-3
Chemical Structure
Peptide R54
Synonym(s): Pep R54; CXCR4 antagonist peptide 19
- CAS No.: 2232233-39-3
- Formula:C44H63N15O9S2
- Molecular Weight:1010.20
InChIKey: GJEUUOMBZBMZAQ-HVTDVQKZSA-N
SMILES: O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](C)C(N[C@H](CSSC(C)([C@H](NC([C@@H](NC([C@@H](N1)CC(C=C2)=CC3=C2C=CC=C3)=O)CC4=CNC=N4)=O)C(O)=O)C)C(N[C@@H](CCCNC(N)=N)C1=O)=O)=O)=O)C
Biological Activity: Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma[1][2].
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Peptide R54 | Peptide R54 (Pep R54; CXCR4 antagonist peptide 19) is an antagonistic peptide targeting CXCR4 with significant anticancer activity. Peptide R54 inhibits CXCR4-dependent cell migration, epithelial-mesenchymal transition, and lung metastasis development, with better serum stability and higher CXCR4 affinity than the lead compound (IC50=20 nM). Peptide R54 synergizes with anti-PD-1 therapy to exert anti-tumor activity in vivo, enhances granzyme activity, and reduces infiltration of Foxp3 cells. Peptide R54 can be used in the study of colon cancer, ovarian cancer, and melanoma. | |||||||||||||||||||||
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- [1]. D'Alterio C, et al. Targeting CXCR4 potentiates anti-PD-1 efficacy modifying the tumor microenvironment and inhibiting neoplastic PD-1. J Exp Clin Cancer Res. 2019 Oct 28;38(1):432. [Content Brief]
- [2]. Russo D, et al. The CXCR4 antagonist R54 targets epithelial-mesenchymal transition (EMT) in human ovarian cancer cells. PLoS One. 2024 Dec 19;19(12):e0314735. [Content Brief]
Keywords
