Design, synthesis, and evaluation of a novel fluorescent probe for competitive fluorescence polarization assay to screen galectin-8 inhibitors.

IF 2.1 4区医学 Q3 PHARMACOLOGY & PHARMACY

Acta Pharmaceutica Pub Date : 2025-04-30 DOI:10.2478/acph-2025-0010

Edvin Purić, Marina Marinović, Zala Kojek, Barbro Kahl-Knutson, Hakon Leffler, Ulf J Nilsson, Marko Anderluh, Janez Mravljak

引用次数: 0

Abstract

In the present work, we describe the design, synthesis, and evaluation of a galectin-8- binding fluorescent probe designed for a competitive fluorescence polarization (FP) assay for screening new galectin-8N inhibitors. The probe was characterized for its photophysical properties and its binding affinity for galectin-8N was determined by using FP. We evaluated the probe in a competitive FP assay with three known galectin-8N inhibitors and demonstrated its suitability for high-throughput screening.

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一种新型荧光探针的设计、合成和评价，用于竞争性荧光偏振法筛选半乳糖凝集素-8抑制剂。

在目前的工作中，我们描述了半乳糖凝集素-8结合荧光探针的设计、合成和评价，该探针设计用于竞争性荧光偏振（FP）测定，以筛选新的半乳糖凝集素- 8n抑制剂。对探针进行了光物理性质表征，并用FP测定了其对半乳糖凝集素- 8n的结合亲和力。我们在竞争性FP分析中对该探针与三种已知的半乳糖凝集素- 8n抑制剂进行了评估，并证明了其高通量筛选的适用性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Acta Pharmaceutica PHARMACOLOGY & PHARMACY-

CiteScore

5.20

自引率

3.60%

发文量

审稿时长

>12 weeks

期刊介绍： AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.