PDE7作为精确靶点：连接疾病调节和潜在的转化医学PET成像。

IF 3.5 3区医学 Q2 CHEMISTRY, MEDICINAL

ACS Medicinal Chemistry Letters Pub Date : 2025-04-15 eCollection Date: 2025-05-08 DOI:10.1021/acsmedchemlett.5c00160

Taoqian Zhao, Steven H Liang

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引用次数: 0

摘要

磷酸二酯酶7 （PDE7）调节cAMP-PKA信号，在免疫功能、神经保护和炎症中发挥重要作用。PDE7活性失调与神经退行性、自身免疫和代谢紊乱有关，使其成为一个有希望的治疗靶点。近年来PDE7抑制剂的研究进展，特别是以嘧啶为基础的化合物，显示出高选择性和强大的生物效应。除了治疗之外，放射标记的PDE7抑制剂提供了PET成像的潜力，使非侵入性疾病监测和治疗评估成为可能。

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PDE7 as a Precision Target: Bridging Disease Modulation and Potential PET Imaging for Translational Medicine.

Phosphodiesterase 7 (PDE7) regulates cAMP-PKA signaling and plays a crucial role in immune function, neuroprotection, and inflammation. Dysregulated PDE7 activity is linked to neurodegenerative, autoimmune, and metabolic disorders, making it a promising therapeutic target. Recent advancements in PDE7 inhibitors, particularly pyrimidinone-based compounds, have shown high selectivity and potent biological effects. Beyond therapeutics, radiolabeled PDE7 inhibitors offer potential for PET imaging, enabling noninvasive disease monitoring and treatment assessment.

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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.