131748-26-0
Chemical Structure
Sialorphin
- CAS No.: 131748-26-0
- Formula:C26H42N12O8
- Molecular Weight:650.69
InChIKey: FVDBNXBFCARYQV-ATIWLJMLSA-N
SMILES: NC(CC[C@H](N)C(N[C@@H](CC1=CN=CN1)C(N[C@@H](CC(N)=O)C(N2[C@@H](CCC2)C(N[C@H](C(O)=O)CCCNC(N)=N)=O)=O)=O)=O)=O
Biological Activity: Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease[1][2][3][4][5].
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Sialorphin | Sialorphin is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin is also a copper (II) ion-binding ligand. Sialorphin has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease. | |||||||||||||||||||||
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- [1]. Rougeot C, et al. Sialorphin, a natural inhibitor of rat membrane-bound neutral endopeptidase that displays analgesic activity. Proc Natl Acad Sci U S A. 2003;100(14):8549-8554. [Content Brief]
- [2]. Salaga M, et al. Systemic Administration of Sialorphin Attenuates Experimental Colitis in Mice via Interaction With Mu and Kappa Opioid Receptors. J Crohns Colitis. 2017;11(8):988-998. [Content Brief]
- [3]. Mizerska-Kowalska M, et al. Neutral endopeptidase (NEP) inhibitors–thiorphan, sialorphin, and its derivatives exert anti-proliferative activity towards colorectal cancer cells in vitro[J]. Chemico-Biological Interactions, 2019, 307: 105-115.
- [4]. Kamysz E, et al. Antitumor activity of opiorphin, sialorphin and their conjugates with a peptide klaklakklaklak. J Pept Sci. 2016;22(11-12):723-730. [Content Brief]
- [5]. Kamysz E, et al. Sialorphin and its analog as ligands for copper (II) ions[J]. Polyhedron, 2013, 55: 216-224.
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