Recent progress in natural product-based inhibitor screening with enzymatic fluorescent probes

Chen, Yi

doi:10.1039/d1ay00245g

Cited by 5 publications

(1 citation statement)

References 106 publications

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“…However, because of the low affinity of 6-carboxyfluorescein, the IC 50 values of benzbromarone and lesinurad against URAT1 measured by this method could be 100 times greater than the radioactive methods, meaning that a high concentration of compounds is required to produce the fluorescence signal. The fluorescence method has the advantages of high throughput and easy quantitative analysis and is widely used to detect in vitro activity in recent years [ 78 – 80 ]. The primary disadvantage of this approach is its low sensitivity, making the identification of strong fluorescence substrates a priority.…”

Section: Resultsmentioning

confidence: 99%

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Chen

You

Wang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Human urate anion transporter 1 (hURAT1) is responsible for the reabsorption of uric acid in the proximal renal tubules and is a promising therapeutic target for treating hyperuricemia. To mitigate the side effects of URAT1-targeted clinical agents such as benzbromarone, there is significant interest in discovering new URAT1 inhibitors and developing technology that can evaluate URAT1 inhibition. This review summarizes the methods for assay of URAT1 inhibition and the progress on the discovery of natural and synthetic URAT1 inhibitors in the past five years.

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Section: Resultsmentioning

confidence: 99%

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Chen

You

Wang

et al. 2021

Evidence-Based Complementary and Alternative Medicine

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Discovery of Fluorescent Naturally‐Occurring Inhibitor of SARS‐CoV‐2 Main Protease by AIE Fluorescent Probe

Lin,

Zhang

2024

ChemMedChem

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Target‐based high‐throughput screening (HTS) is an efficient way to identify potent drugs. However, the accuracy of HTS could be affected by Pan‐Assay Interference Compounds (PAINS). One reason for the generation of PAINS is that the inherent photophysical property of screened compounds could interfere with typically used assay signals including absorption and fluorescence. Our previous studies indicate that the fluorescent probe based on the fluorophore with characteristics of aggregation‐induced emission (AIE) could provide high accuracy of HTS, especially for the fluorescent natural products. Herein, we report an AIE‐based fluorescent probe for the main protease (Mpro) of SARS‐CoV‐2. We designed and synthesized an AIE fluorescent probe ZLHG5, which has a site that can be specifically cleaved by Mpro to produce a light‐up fluorescence. Thanks to the large Stokes shift of AIE fluorophore (~300 nm), the probe could be effectively used for HTS of Mpro inhibitors. After screening a library of fluorescent natural products with ZLHG5, we obtained two coumarin‐originated natural compounds with potent inhibitory activity towards Mpro protease. This study provides both useful fluorescent HTS probe and potent inhibitors for Mpro protease.

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Sensing and Imaging Agents for Cyclooxygenase Enzyme

Rao Cheekatla,

Murale,

Gopala

et al. 2024

ChemMedChem

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In this concept, we present a comprehensive study on the development and application of COX‐2‐specific fluorescent probes for cancer imaging and diagnosis. Targetting cancer cells and measuring cancer‐related activities in specific organelles quickly and accurately are crucial factors for early diagnosis and research on cancer pathology and treatment. This concept explores a variety of probes which include BDIMC1‐2, TPI‐IMC, YZP1, IQ‐1, ANQ‐IMC‐6, Niblue‐C6‐IMC, AZB‐IMC2, CMP, CF3‐Fluorocoxib, IBPC1, CoxFluor, etc. and each one demonstrates unique mechanisms and high selectivity towards COX‐2 enzymes. These probes were designed to enhance fluorescence upon binding to COX‐2 which enable precise visualization of tumor and inflamed tissues. The research emphasizes the importance of COX‐2 as a biomarker in cancer diagnostics, particularly in identifying cancer stem cells and inflamed tissues. This concept highlights the potentiality of these probes in non‐invasive imaging techniques which offering significant advancements in cancer diagnosis and monitoring. The in vivo and in vitro experiments, including applications in mouse models and human tissue samples, confirm the efficacy of these probes in providing detailed imaging for clinical and research applications.

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Recent progress in natural product-based inhibitor screening with enzymatic fluorescent probes

Abstract: In this mini review, small-molecule based enzymatic fluorescent probes for natural inhibitor screening has been discussed, which includes the construction and sensing mechanisms of developed probes and their applications in inhibitor screening.

Cited by 5 publications

References 106 publications

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Recent Updates of Natural and Synthetic URAT1 Inhibitors and Novel Screening Methods

Discovery of Fluorescent Naturally‐Occurring Inhibitor of SARS‐CoV‐2 Main Protease by AIE Fluorescent Probe

Sensing and Imaging Agents for Cyclooxygenase Enzyme

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