Antiestrogen/histone deacetylase inhibitor (HDACi) hybrids were designed by merging structures of raloxifene with suberoylanilide hydroxamic acid, incorporating the HDACi unit into the phenolic ring of the antiestrogen. These hybrids were synthesized with a range of HDACi chain lengths and assessed for bifunctionality. Four hybrids, 21 (YW471), 22 (YW490), 27(YW486), and 28 (YW487) showed good potency both as antiestrogens in a BRET assay and in a fluorometric HDACi assay. The antiproliferative activity of the hybrids was demonstrated in both ER+ MCF7 and ER- MDA-MB-231 breast cancer cell lines.

13 Jun 2023·Nutrients

Bioinformatics Analysis of the Molecular Networks Associated with the Amelioration of Aberrant Gene Expression by a Tyr-Trp Dipeptide in Brains Treated with the Amyloid-β Peptide.

Article

Author: Tashiro, Kosuke ; Yasuda, Tokio ; Furuya, Shigeki ; Ishijima, Tomoko ; Okada, Shinji ; Hamano, Momoko ; Abe, Keiko ; Ichinose, Takashi

Short-chain peptides derived from various protein sources have been shown to exhibit diverse bio-modulatory and health-promoting effects in animal experiments and human trials. We recently reported that the oral administration of the Tyr-Trp (YW) dipeptide to mice markedly enhances noradrenaline metabolism in the brain and ameliorates the working-memory deficits induced by the β-amyloid 25-35 peptide (Aβ_25-35). In the current study, we performed multiple bioinformatics analyses of microarray data from Aβ_25-35/YW-treated brains to determine the mechanism underlying the action of YW in the brain and to infer the molecular mechanisms and networks involved in the protective effect of YW in the brain. We found that YW not only reversed inflammation-related responses but also activated various molecular networks involving a transcriptional regulatory system, which is mediated by the CREB binding protein (CBP), EGR-family proteins, ELK1, and PPAR, and the calcium-signaling pathway, oxidative stress tolerance, and an enzyme involved in de novo l-serine synthesis in brains treated with Aβ_25-35. This study revealed that YW has a neuroprotective effect against Aβ_25-35 neuropathy, suggesting that YW is a new functional-food-material peptide.

01 Jul 2019·Food Chemistry

The interaction mechanism of oligopeptides containing aromatic rings with β-cyclodextrin and its derivatives

Article

Author: Wang, Huabin ; Wang, Yu ; Liu, Benguo ; Liang, Guizhao ; Lv, Yonghui ; Geng, Sheng ; Li, Jiaqi

We investigate the formation mechanism of supramolecular complexes of four antioxidant oligopeptides (YW, WY, WYS, and WYSL) with β-cyclodextrin (β-CD), hydroxypropyl-β-cyclodextrin (HP-β-CD) and 6-O-α-maltosyl-β-cyclodextrin (M-β-CD) by combined computational and experimental methods. The formation of complexes is determined by UV, IR and DSC, and the rank-ordered acquired stability of the complexes is as follows: WYSL/HP-β-CD > WYS/HP-β-CD > WY/HP-β-CD > YW/M-β-CD > YW/HP-β-CD > YW/β-CD. The ¹H NMR analysis and molecular docking results reveal that the aromatic rings of these oligopeptides are embedded into the cavities of the studied β-CD and its derivatives, indicating that hydrophobic interaction is a major driving force for the formation of the complexes. We also demonstrate that H-bonds play a key role in maintaining the supramolecular complexes. In addition, the results of the antioxidant assay indicate that the radical scavenging capacity of the oligopeptides is enhanced by the CD-based inclusion.

100 Deals associated with YW program(Shangpharma Corp.)

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Preclinical	CN	Shangpharma Corp.	16 Sep 2022
Fatty Liver	Preclinical	CN	Shangpharma Corp.	16 Sep 2022
Inflammation	Preclinical	CN	Shangpharma Corp.	16 Sep 2022
Neoplasms	Preclinical	CN	Shangpharma Corp.	16 Sep 2022

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