Article
Medicine, Research & Experimental
Kai Fang, Yueping Zhan, Ruiqiu Zhu, Yuqian Wang, Chengqi Wu, Min Sun, Yanyan Qiu, Zeting Yuan, Xin Liang, Peihao Yin, Ke Xu
Summary: This study found that bufalin inhibits tumor microenvironment-mediated angiogenesis by targeting the STAT3 signaling pathway in vascular endothelial cells. This suggests that bufalin may be used as a new antiangiogenic adjuvant therapy for treating colorectal cancer.
JOURNAL OF TRANSLATIONAL MEDICINE
(2021)
Review
Cell Biology
Yongchang Lai, Fucai Tang, Yapeng Huang, Chengwu He, Chiheng Chen, Jiquan Zhao, Wenqi Wu, Zhaohui He
Summary: Renal cell carcinoma (RCC) is a common urinary system tumor, with clear cell renal cell carcinoma being the most prevalent subtype. Advanced RCC is treated with molecular-targeted drugs and immune checkpoint inhibitors, but resistance may occur due to the dynamic tumor microenvironment and metabolic characteristics. Novel findings on the TME and tumor metabolism in RCC may offer insights for future treatment strategies to overcome resistance.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Review
Immunology
Ricardo M. Sainz, Jorge Humberto Rodriguez-Quintero, Maria Constanza Maldifassi, Brendon M. Stiles, Erik Wennerberg
Summary: While the expression of P2X7 receptor on tumor cells promotes cancer growth and metastasis, its expression by the host immune system is essential for coordinating immune responses against cancer. However, there are conflicting roles of P2X7 receptor in regulating immune responses to tumors, making it challenging to develop P2X7 receptor modulators for cancer treatment. This review discusses the prognostic value of P2X7 receptor in cancer, current approaches targeting P2X7 receptor in tumor models, and how tumors manipulate immune responses through P2X7 receptor to promote immune escape. Alternative strategies to overcome tumor immune escape via P2X7 receptor for enhancing immunotherapeutic strategies in cancer patients are also discussed.
FRONTIERS IN IMMUNOLOGY
(2023)
Review
Chemistry, Medicinal
Jingyu Zhang, Yu Zhang, Bingxue Qu, Haiyan Yang, Shengquan Hu, Xiaowu Dong
Summary: Anti-cancer immunotherapy, including cellular immunotherapy, immune checkpoint inhibitors, and cancer vaccines, has revolutionized the treatment of various malignancies in recent decades. The focus has shifted towards developing small molecule inhibitors to overcome the limitations of monoclonal antibodies. Clinical trials are currently testing the combination of immune checkpoint inhibitors with various small molecule agonists/inhibitors to improve treatment outcomes and prevent tumor recurrence.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Munawaer Muaibati, Abasi Abuduyilimu, Tao Zhang, Yun Dai, Ruyuan Li, Fanwei Huang, Kexin Li, Qing Tong, Xiaoyuan Huang, Liang Zhuang
Summary: Ovarian cancer is a deadly female reproductive system tumor with a complex immunosuppressive microenvironment. Immune checkpoint inhibitors (ICIs) have revolutionized the treatment of many solid tumors but have shown limited benefits in ovarian cancer. Therefore, a comprehensive understanding of immune checkpoint mechanisms is needed to improve the efficacy of ICIs in ovarian cancer.
EXPERT REVIEWS IN MOLECULAR MEDICINE
(2023)
Review
Biochemistry & Molecular Biology
Madelaine Magali Audero, Natalia Prevarskaya, Alessandra Fiorio Pla
Summary: This review presents the impact of hypoxia and acidosis in the tumor microenvironment (TME) on cancer progression, and focuses on the role of Ca2+ channels in this process.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Oncology
Zhimin Du, Hui Zhang, Yueyuan Feng, Dewen Zhan, Shuya Li, Chenggong Tu, Jinbao Liu, Jinheng Wang
Summary: This study comprehensively investigated the impact of tumour-derived small extracellular vesicles (sEVs) on the systemic immune system using mass cytometry. The results revealed that tumour-derived sEVs significantly altered the composition and function of the global immune macroenvironment, leading to an immunosuppressive peripheral and tumour immune microenvironment. Knockdown of Rab27a reduced sEV secretion and delayed tumour growth and metastasis.
BRITISH JOURNAL OF CANCER
(2023)
Review
Chemistry, Medicinal
Xinjian Tian, Feng Xu, Qiangsheng Zhu, Ziwen Feng, Wei Dai, Yeling Zhou, Qi-Dong You, Xiaoli Xu
Summary: This review focuses on the connection between the cGAS-STING signaling pathway and autoimmune and inflammatory disorders. It summarizes the development and optimization of cGAS-STING inhibitors and discusses their therapeutic effects on inflammatory diseases. The review also proposes suggestions and insights for future exploration in this area.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Di Zhu, Yu Lu, Bo Hu, Yuheng Pang, Bingru Liu, Miao Zhang, Wenjing Wang, Yuji Wang
Summary: This study aims to obtain highly targeted PAD4 inhibitors by modifying PAD4 protein inhibitors with different phenylboronic acid groups. The activity and mechanism of PBA-PAD4 inhibitors were examined in vitro and in vivo, showing significant antitumor effects and inhibition of tumor cell metastasis. The results suggest that PBA-PAD4 inhibitors have great potential in tumor therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Leishemba K. Thoidingjam, Cedric M. Blouin, Christine Gaillet, Aurelien Brion, Stephanie Solier, Supaporn Niyomchon, Ahmed El Marjou, Sara Mouasni, Fernando E. Sepulveda, Genevieve de Saint Basile, Christophe Lamaze, Raphael Rodriguez
Summary: Interferons (IFNs), important cytokines, play roles in triggering downstream biochemical events upon binding to cell surface receptors. Dysregulated IFN signaling has been linked to cancer progression and autoimmune diseases. Researchers have identified a small molecule that can block the activation of IFN signaling and further developing a more potent analogue that shows potential therapeutic effects in reducing bleeding in a model of hemorrhagic colitis. This first-in-class small molecule also inhibits other types of IFN-induced signaling. This research provides a foundation for the development of pan-IFN inhibitory drugs.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2022)
Review
Chemistry, Multidisciplinary
Jia Zheng, Wei Zhang, Linfeng Li, Yi He, Yue Wei, Yongjun Dang, Shenyou Nie, Zufeng Guo
Summary: Targeted therapy is a groundbreaking innovation in cancer treatment, with FGFRs being recognized as promising therapeutic targets. Several generations of FGFR kinase inhibitors have been developed over the past two decades.
FRONTIERS IN CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Yudong Yang, Chi Zhang, Yixuan Song, Yawen Li, Pingping Li, Min Huang, Feilong Meng, Mingliang Zhang
Summary: Through chemical screening, we have identified and validated SB505124 as an ABE activator. Treating cells with SB505124 enhances on-target editing at multiple genome loci, with little effect on off-target conversions. Furthermore, SB505124 facilitates the editing of disease-associated genes.
NUCLEIC ACIDS RESEARCH
(2022)
Review
Chemistry, Multidisciplinary
Qian Wu, Li Jiang, Si-cheng Li, Qiao-jun He, Bo Yang, Ji Cao
Summary: PD-1/PD-L1 signaling pathway is a target for anticancer drugs, and the development of small molecule inhibitors provides a new avenue for tumor immunotherapy.
ACTA PHARMACOLOGICA SINICA
(2021)
Review
Chemistry, Inorganic & Nuclear
Caiyun Liu, Hanchuang Zhu, Yan Zhang, Meijun Su, Mengyuan Liu, Xiaohui Zhang, Xin Wang, Xiaodi Rong, Kun Wang, Xiwei Li, Baocun Zhu
Summary: Golgi, as an essential organelle in cells, plays a crucial role in cellular functions and disease diagnosis and treatment. The fluorescent probe method is advantageous for studying Golgi and its microenvironment, and new Golgi-targeted probes have potential applications in disease treatment. However, the development of small molecule fluorescent probes for Golgi is still challenging.
COORDINATION CHEMISTRY REVIEWS
(2022)
Review
Biochemistry & Molecular Biology
Zefan Liu, Yajun Zhang, Yucheng Xiang, Xin Kang
Summary: Small-molecule compounds can effectively solve the problems of poor physicochemical properties in macromolecular drugs, improving their application in tumor immunotherapy. The proteolysis targeting chimera (PROTAC) technology provides a novel mode of action for small molecules to interact with therapeutic targets, particularly proteins. This review comprehensively summarizes the immunological targets that have been studied and those that are yet to be explored for PROTAC technology, aiming to provide more options and opportunities for small-molecule-based tumor immunotherapy. In addition, it discusses novel directions to enhance and broaden the efficiency of protein degradation in PROTAC design.
