G蛋白偶联受体抑制在淋巴瘤治疗中的应用
GPCR Inhibition in Treating Lymphoma.
作者信息
Barreca Marilia, Spanò Virginia, Raimondi Maria V, Bivacqua Roberta, Giuffrida Stefano, Montalbano Alessandra, Cavalli Andrea, Bertoni Francesco, Barraja Paola
机构信息
Department of Biological, Chemical and Pharmaceutical Sciences and Technologies (STEBICEF), University of Palermo, Via Archirafi 32, 90123 Palermo, Italy.
Institute for Research in Biomedicine, Faculty of Biomedical Sciences, USI, Via Francesco Chiesa 5, 6500 Bellinzona, Switzerland.
出版信息
ACS Med Chem Lett. 2022 Feb 15;13(3):358-364. doi: 10.1021/acsmedchemlett.1c00600. eCollection 2022 Mar 10.
G protein-coupled receptors (GPCRs) are important classes of cell surface receptors involved in multiple physiological functions. Aberrant expression, upregulation, and mutation of GPCR signaling pathways are frequent in many types of cancers, promoting hyperproliferation, angiogenesis, and metastasis. Recent studies showed that alterations of GPCRs are involved in different lymphoma types. Herein, we review the synthetic strategies to obtain GPCR inhibitors, focusing on CXCR4 inhibitors which represent most of the GPCR inhibitors available in the market or under preclinical investigations for these diseases.
G蛋白偶联受体（GPCRs）是参与多种生理功能的重要细胞表面受体类别。GPCR信号通路的异常表达、上调和突变在多种癌症中很常见，会促进细胞过度增殖、血管生成和转移。最近的研究表明，GPCRs的改变与不同类型的淋巴瘤有关。在此，我们综述了获得GPCR抑制剂的合成策略，重点关注CXCR4抑制剂，这类抑制剂占市场上或处于针对这些疾病的临床前研究阶段的GPCR抑制剂的大多数。
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