Highly Sensitive Naphthalene-Based Twisted Intramolecular Charge Transfer Molecules for the Detection of In Vitro and In Cellulo Protein Aggregates.

IF 4 3区医学 Q2 CHEMISTRY, MEDICINAL ACS Medicinal Chemistry Letters Pub Date : 2024-11-29 eCollection Date: 2024-12-12 DOI:10.1021/acsmedchemlett.4c00363

Joy Debnath, Yuvasree Sekar, Anwesha Bera

引用次数: 0

Abstract

Newly synthesized naphthalene-based twisted intramolecular charge transfer (TICT) molecules show 8.5- and 2.6-fold increases in fluorescence intensity upon binding with protein aggregates in comparison with the fluorescence enhancement for thioflavin T (ThT). The dissociation constant (K _d ) values of these compounds with bovine serum albumin (BSA) aggregates are in the 145-176 nM range, which is 10³ times lower than that of ThT. Along with the strong binding propensity, these molecules are also capable of measuring protein aggregate (BSA) concentration in the 500 to 5 pM level. Interestingly, one of the synthesized molecules was also able to bind with the intracellular protein aggregates.

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用于检测体外和纤维素蛋白聚集体的高灵敏度萘基扭曲分子内电荷转移分子。

新合成的萘基扭曲分子内电荷转移（TICT）分子与蛋白质聚集体结合后，荧光强度比硫黄素T （ThT）增强8.5倍和2.6倍。这些化合物与牛血清白蛋白（BSA）聚集体的解离常数（kd）值在145 ~ 176 nM范围内，比ThT低103倍。除了具有很强的结合倾向外，这些分子还能够测量500至5pm水平的蛋白质聚集体（BSA）浓度。有趣的是，其中一个合成的分子也能够与细胞内蛋白质聚集体结合。

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

ACS Medicinal Chemistry Letters CHEMISTRY, MEDICINAL-

CiteScore

7.30

自引率

2.40%

发文量

328

审稿时长

1 months

期刊介绍： ACS Medicinal Chemistry Letters is interested in receiving manuscripts that discuss various aspects of medicinal chemistry. The journal will publish studies that pertain to a broad range of subject matter, including compound design and optimization, biological evaluation, drug delivery, imaging agents, and pharmacology of both small and large bioactive molecules. Specific areas include but are not limited to: Identification, synthesis, and optimization of lead biologically active molecules and drugs (small molecules and biologics) Biological characterization of new molecular entities in the context of drug discovery Computational, cheminformatics, and structural studies for the identification or SAR analysis of bioactive molecules, ligands and their targets, etc. Novel and improved methodologies, including radiation biochemistry, with broad application to medicinal chemistry Discovery technologies for biologically active molecules from both synthetic and natural (plant and other) sources Pharmacokinetic/pharmacodynamic studies that address mechanisms underlying drug disposition and response Pharmacogenetic and pharmacogenomic studies used to enhance drug design and the translation of medicinal chemistry into the clinic Mechanistic drug metabolism and regulation of metabolic enzyme gene expression Chemistry patents relevant to the medicinal chemistry field.