探索四氢异喹啉（THIQ）支架作为Sigma受体的治疗调节剂。

IF 3.3 3区医学 Q2 CHEMISTRY, MEDICINAL

Mini reviews in medicinal chemistry Pub Date : 2025-07-22 DOI:10.2174/0113895575379843250711134106

Dikshita Lama, A Michael Crider, Marcelo J Nieto

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引用次数: 0

摘要

σ受体（σ r）包括σ1和σ2亚型，是多种药理靶点，在癌症、神经退行性疾病和精神疾病中起重要作用。四氢异喹啉（THIQ）支架是许多生物活性化合物的核心结构，作为设计σ r配体的通用平台而受到关注。thiq基化合物表现出强大的σ r结合亲和力，具有从神经保护到抗肿瘤的治疗作用。这篇综述探讨了THIQ配体的结构特征，它们与σ r的相互作用，以及它们的治疗意义。讨论了THIQ衍生物在σ r研究中的挑战和前景。

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Exploring Tetrahydroisoquinoline (THIQ) Scaffold as Therapeutic Modulators of Sigma Receptors.

Sigma receptors (σRs), comprising σ1 and σ2 subtypes, are versatile pharmacological targets with significant roles in cancer, neurodegeneration, and psychiatric disorders. The tetrahydroisoquinoline (THIQ) scaffold, a core structure in many biologically active compounds, has garnered attention as a versatile platform for designing σRs ligands. THIQ-based compounds exhibit potent σRs binding affinity, leading to therapeutic effects ranging from neuroprotection to antitumor activity. This mini-review explores the structural features of THIQ ligands, their interaction with σRs, and their therapeutic implications. Challenges and future prospects for THIQ derivatives in σRs research are also discussed.

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来源期刊

Mini reviews in medicinal chemistry 医学-医药化学

CiteScore

7.80

自引率

0.00%

发文量

231

审稿时长

6 months

期刊介绍： The aim of Mini-Reviews in Medicinal Chemistry is to publish short reviews on the important recent developments in medicinal chemistry and allied disciplines. Mini-Reviews in Medicinal Chemistry covers all areas of medicinal chemistry including developments in rational drug design, synthetic chemistry, bioorganic chemistry, high-throughput screening, combinatorial chemistry, drug targets, and natural product research and structure-activity relationship studies. Mini-Reviews in Medicinal Chemistry is an essential journal for every medicinal and pharmaceutical chemist who wishes to be kept informed and up-to-date with the latest and most important developments.