Medicinal Chemistry Research ( IF 2.6 ) Pub Date : 2021-07-28 , DOI: 10.1007/s00044-021-02771-0 Benjamin E. Blass 1 , Rong Gao 1 , John C. Gordon 1 , Daniel J. Canney 1 , Kevin M. Blattner 2 , Douglas A. Pippin 2
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Nearly 40 years after the first disclosure of sigma receptors, the sigma-2 (σ2) receptor was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein). This macromolecule has been associated with a number of disease states such as schizophrenia, Alzheimer’s disease, neuropathic pain, traumatic brain injury, and cancer. We have recently identified a series of novel, functionalized γ-butyrolactones that are potent σ2 receptor ligands that are drug-like and identified a potential candidate (9z) for future in vivo study.
中文翻译：
新型选择性 γ-丁内酯 sigma-2 配体的设计、合成和评估
在 sigma 受体首次公开近 40 年后，sigma-2 (σ2) 受体最近被鉴定为跨膜蛋白 97（TMEM97，也称为 MAC30（脑膜瘤相关蛋白）。这种大分子与许多疾病状态，如精神分裂症、阿尔茨海默病、神经性疼痛、创伤性脑损伤和癌症。我们最近确定了一系列新型的、功能化的 γ-丁内酯，它们是有效的 σ2 受体配体，类似于药物，并确定了一个潜在的候选者 (9z ) 用于未来的体内研究。
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