Tyrosinase is the key rate-limiting enzyme for melanin synthesis. The accumulation and excessive production of melanin lead to skin pigmentation. Therefore, tyrosinase is the target of tyrosinase inhibitors to control melanin synthesis. Only a few TYR inhibitors have been proven to be effective and safe to treat skin pigmentation. This highlights the importance of developing new tyrosinase inhibitors. Based on the reported tyrosinase inhibitors with phenylalanine structure, a series of novel phenylalanine derivatives were synthesized and investigated as mTYR inhibitors. The results demonstrated that most of these derivatives had more potent mTYR inhibitory activities than positive controls. Compound 3e was found to be the strongest inhibitor with an IC₅₀ value of 4.86 ± 0.026 μM. The Lineweaver-Burk plots of mTYR inhibition kinetics revealed that the selected compounds 2d and 3e were reversible and competitive inhibitors. In addition, molecular docking results of compounds 2d and 3e show they could compete with the substrate for the active center, including mTYR and hTYR. And the ADME prediction of selected derivatives assess the potential druglikeness. These results indicated that this class of compounds could be used as leads for developing new TYR inhibitors.

01 Jul 2025·Food Chemistry

Innovative dopamine-modified carbon quantum dot fluorescence sensor meets affinity chromatography: A breakthrough in Tyrosinase inhibitor screening in food

Article

Author: Ma, Fen ; Wilson, Gidion ; Zhang, Yue ; Gao, Tao ; Zhang, Shuxian ; Wang, Weibiao ; Yang, Zhigang ; He, Xinmin ; Chen, Guoning ; Zhang, Weiman ; Sa, Yuping ; Wang, Mei ; Ma, Xueqin

Tyrosinase (TYR), a polyphenol oxidase crucial for melanin synthesis, plays various biological functions, and its inhibitors are widely used in the cosmetics and food industries for skin-lightening and anti-browning applications. Here, an innovative method that integrates biosensing with affinity chromatography was developed, enabling the rapid and precise identification of TYR inhibitors in food. The biosensing segment used a dopamine-modified carbon quantum dot fluorescence sensor for quick detection of TYR inhibitors in complex food samples. In affinity chromatography, bioactive compounds were accurately captured, separated, and identified. The method was validated using both positive and negative controls and applied to screen for TYR inhibitors in 21 foods. The results revealed Wolfberry significantly inhibits TYR, with 2-O-β-D-Glucopyranosyl-L-ascorbic acid (AA-2βG) identified as the active compound. Molecular docking demonstrated strong binding between AA-2βG and TYR, and anti-browning tests confirmed its effectiveness. The findings highlight the potential for quickly identifying enzyme inhibitors in food.

01 Jan 2025·Talanta

MnO4−-triggered wavelength-changeable and rapid-response fluorescence sensor for paper-based on-site sensing of tyrosinase activity in potato

Article

Author: Pang, Lihua ; Ma, Yifei ; Liu, Jinhua ; Li, Yinhui ; Liu, Xiaoxue ; Yang, Hong ; Xing, Guichuan ; Zhu, Shanshan

Rapid-response in situ fluorogenic reactions in aqueous solution are important for designing sensitive and stable sensing platforms. Herein, a wavelength-changeable and rapid-response (within 5 s) fluorescence sensing platform for monitoring tyrosinase (TYR) activity is constructed. The developed assay is based on TYR catalyzing the hydroxylation of mono-phenol to o-diphenol and MnO₄^--triggered fluorogenic between dopamine (DA) and phenol derivatives in aqueous solution. The fluorescence wavelength can be changeable from 470 to 550 nm with strong fluorescence according to different phenol derivatives. Our proposed sensor not only exhibits a good recovery for TYR in high serum concentration (20 %), but also has been successfully applied to the screening of TYR inhibitors modeled on kojic acid. Furthermore, a paper-based wavelength-changeable fluorescence sensor was developed for on-site detection of TYR activity in potatoes with high recovery, which is consistent with our previously reported method. Consequently, the proposed sensing system has broad prospects in the practical application of TYR-associated food monitoring and clinical diagnosis.

100 Deals associated with TYR inhibitors(Hangzhou Normal University)

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Hyperpigmentation	Preclinical	China	Hangzhou Normal University	23 Apr 2024

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

TYR inhibitors(Hangzhou Normal University)

Overview

Basic Info

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation