PAD4抑制剂的构效关系及其在肿瘤免疫治疗中的作用
Structure-Activity Relationship of PAD4 Inhibitors and Their Role in Tumor Immunotherapy.
作者信息
Jia Yijiang, Jia Renbo, Taledaohan Ayijiang, Wang Yanming, Wang Yuji
机构信息
Department of Medicinal Chemistry, School of Pharmaceutical Sciences of Capital Medical University, 10 Xi Tou Tiao, You An Men, Beijing 100069, China.
Department of Medicinal Chemistry, Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Beijing Laboratory of Biomedical Materials, Engineering Research Center of Endogenous Prophylactic of Ministry of Education of China, 10 Xi Tou Tiao, You An Men, Beijing 100069, China.
出版信息
Pharmaceutics. 2024 Feb 28;16(3):335. doi: 10.3390/pharmaceutics16030335.
Protein arginine deiminase 4 (PAD4) plays an important role in cancer progression by participating in gene regulation, protein modification, and neutrophil extracellular trap (NET) formation. Many reversible and irreversible PAD4 inhibitors have been reported recently. In this review, we summarize the structure-activity relationships of newly investigated PAD4 inhibitors to bring researchers up to speed by guiding and describing new scaffolds as optimization and development leads for new effective, safe, and selective cancer treatments. In addition, some recent reports have shown evidence that PAD4 inhibitors are expected to trigger antitumor immune responses, regulate immune cells and related immune factors, enhance the effects of immune checkpoint inhibitors, and enhance their antitumor efficacy. Therefore, PAD4 inhibitors may potentially change tumor immunotherapy and provide an excellent direction for the development and clinical application of immunotherapy strategies for related diseases.
蛋白质精氨酸脱亚氨酶4（PAD4）通过参与基因调控、蛋白质修饰和中性粒细胞胞外诱捕网（NET）形成，在癌症进展中发挥重要作用。最近报道了许多可逆和不可逆的PAD4抑制剂。在本综述中，我们总结了新研究的PAD4抑制剂的构效关系，通过指导和描述新的骨架作为新的有效、安全和选择性癌症治疗的优化和开发线索，使研究人员跟上最新进展。此外，最近的一些报告显示，有证据表明PAD4抑制剂有望触发抗肿瘤免疫反应，调节免疫细胞和相关免疫因子，增强免疫检查点抑制剂的效果，并提高其抗肿瘤疗效。因此，PAD4抑制剂可能会改变肿瘤免疫治疗，并为相关疾病免疫治疗策略的开发和临床应用提供一个极好的方向。
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