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

IF 3.5 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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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.