Article
Chemistry, Medicinal
Dipti Kanabar, Mimansa Goyal, Emma Kane, Tejashri Chavan, Abbas Kabir, Xuechun Wang, Snehal Shukla, Joseph Almasri, Sona Goswami, Gizem Osman, Marino Kokolis, Donald E. Spratt, Vivek Gupta, Aaron Muth
Summary: This study reports the structure-based design of small molecules that can bind to Gankyrin and inhibit its overexpression in breast and lung cancers, showing potential therapeutic value.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Isha Bansal, Amit Kumar Pandey, Munindra Ruwali
Summary: Breast cancer is the most common malignancy in women worldwide and despite advancements in cancer detection and treatment, it remains the leading cause of women's malignancy related deaths. Understanding the biology of breast cancer and developing new diagnostic and therapeutic strategies have gained renewed focus in recent studies.
FRONTIERS IN PHARMACOLOGY
(2023)
Review
Medicine, General & Internal
Jianjing Lin, Shicheng Jia, Weifei Zhang, Mengyuan Nian, Peng Liu, Li Yang, Jianwei Zuo, Wei Li, Hui Zeng, Xintao Zhang
Summary: Osteoarthritis is a degenerative disease characterized by joint pain, caused by factors such as fibrosis, chapping, ulcers, and loss of articular cartilage. Traditional treatments only delay its progression, while small molecule inhibitors targeting proteins show promising effects in managing osteoarthritis. This review examines small molecule inhibitors targeting various proteins and discusses disease-modifying osteoarthritis drugs based on them, providing valuable insights for the treatment of osteoarthritis.
JOURNAL OF CLINICAL MEDICINE
(2023)
Review
Biochemistry & Molecular Biology
Chao Zhang, Qian Xie, Chi Cheong Wan, Zhe Jin, Chun Hu
Summary: HIV-1 integrase plays a crucial role in HIV-1 treatment, but issues like drug resistance require further research. This review discussed the structure, function, and recent advances in small-molecule inhibitors of HIV-1 integrase.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Chao Yang, Wansheng Xie, Heqian Zhang, Wenjian Xie, Tiantian Tian, Zhiwei Qin
Summary: Dengue is an acute tropical infectious disease transmitted by mosquitoes, posing a major challenge to global public health. The lack of clinically proven specific drugs for prevention and treatment is mainly due to the incomplete understanding of the pathogenesis of dengue fever.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Anirban Das, Yogesh M. Gangarde, Ranit Pariary, Anirban Bhunia, Ishu Saraogi
Summary: This article introduces a novel amphiphilic molecule called PAD-S, which acts as a chemical chaperone to completely inhibit the fibrillation of insulin and its biosimilars. PAD-S can bind to the key hydrophobic regions of insulin, preventing its self-assembly and protecting cells from insulin amyloid-induced cytotoxicity.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2022)
Review
Pharmacology & Pharmacy
Rong Xiang, Zhengsen Yu, Yang Wang, Lili Wang, Shanshan Huo, Yanbai Li, Ruiying Liang, Qinghong Hao, Tianlei Ying, Yaning Gao, Fei Yu, Shibo Jiang
Summary: The COVID-19 pandemic has caused chaos worldwide, with vaccines in distribution but treatment methods lagging behind. Researchers are working hard to understand the virus and develop effective treatments.
ACTA PHARMACEUTICA SINICA B
(2022)
Review
Chemistry, Medicinal
Douglas W. Thomson, Giovanna Bergamini
Summary: TBK1, a key mediator of innate immunity processes, plays important roles in inflammatory and autoimmune diseases, cancer, and metabolic disorders. The increasing interest in TBK1 as a drug target is evidenced by the growing number of patents reporting on novel TBK1 small molecule inhibitors and new applications of TBK1 inhibitors. The complexity of TBK1 biology presents challenges, but the discovery of selective small molecule inhibitors holds promise for further research on its biological role and validation as a drug target.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2021)
Review
Biochemistry & Molecular Biology
Jiatao Song, Jiawei Wang, Sheng Tian, Huanqiu Li
Summary: STAT3 is a crucial signal transducer and transcription factor protein that plays important roles in cell proliferation, differentiation, apoptosis, and immune/inflammatory responses. Various STAT3 inhibitors have been discovered based on different mechanisms, and their structures, bioactivity, and mechanisms of action have been summarized. These inhibitors can directly target the SH2 domain, DNA binding domain, or coiled-coil domain of STAT3. Small molecule inhibitors, natural product inhibitors, peptides/peptidomimetics, and their analogues have shown promising application potential.
CURRENT MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Pengxia Qin, Yingying Ran, Yujing Liu, Chao Wei, Xiaoyi Luan, Haoqian Niu, Jie Peng, Jie Sun, Jingde Wu
Summary: This review discusses the roles of JNK3 in the pathogenesis and treatment of AD, as well as the latest progress in the development of JNK3 inhibitors.
BIOORGANIC CHEMISTRY
(2022)
Article
Multidisciplinary Sciences
Zhiquan Liu, Siyu Chen, Liangxue Lai, Zhanjun Li
Summary: Researchers repurposed virus-derived anti-deaminase proteins to inhibit cytosine base editors (CBEs) and efficiently regulate their activity in gene modification and therapeutic applications. Through inhibition of the APOBEC3 catalytic domain, relocation of deaminases, or degradation of the CBE complex, these anti-deaminases can moderately inhibit various commonly used base editors. They outperform traditional anti-CRISPRs in reducing Cas9-dependent and Cas9-independent off-target effects of CBEs. Additionally, a cell type-specific CBE-ON switch based on miRNA-responsive adenovectors was created, demonstrating its practicality.
NATURE COMMUNICATIONS
(2022)
Article
Cell Biology
Zhe Liu, Liang Ma, Yiming Sun, Wenying Yu, Xue Wang
Summary: The study demonstrated that the STAT3/ZEB1 axis is critical in gefitinib resistance in lung cancer, and a new potential therapeutic strategy targeting STAT3 has been identified with the inhibitor LL1. LL1 was shown to sensitize resistant cells to gefitinib by depleting STAT3 activity and blocking its signaling pathways, with little observed toxicity in animal models, indicating it could be a chemotherapeutic adjuvant for gefitinib resistance in NSCLC.
CELL DEATH & DISEASE
(2021)
Review
Biochemistry & Molecular Biology
Soonsil Hyun, Dongyun Shin
Summary: The study explores methods for treating cancers caused by KRAS mutations, including controlling the activity of RAS pathway proteins, small-molecule inhibitors, and targeted protein degradation strategies. These novel approaches are expected to provide promising therapeutic options for tumor patients with KRAS mutations.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biochemistry & Molecular Biology
Xia-Wen Dang, Ji-Long Duan, Emily Ye, Nian-Dong Mao, Renren Bai, Xinglu Zhou, Xiang-Yang Ye
Summary: This review summarizes the important role of c-Src kinase in cell division, motility, adhesion, and survival, as well as its implications in disease. It provides valuable insights and new ideas for researchers in areas such as inhibitor development, combination therapy, and clinical research.
BIOORGANIC CHEMISTRY
(2024)
Article
Oncology
Kristina Witt, Susan Evans-Axelsson, Andreas Lundqvist, Martin Johansson, Anders Bjartell, Rebecka Hellsten
Summary: The combination of STAT3 inhibition with anti-CTLA-4 therapy enhances antitumoral activity in prostate cancer, reducing intratumoral Treg frequency.
CANCER IMMUNOLOGY IMMUNOTHERAPY
(2021)
Editorial Material
Pharmacology & Pharmacy
Songtao Li, Zhenyuan Song, Ping Yao, Jiangjiang Qin
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Biotechnology & Applied Microbiology
Xuan Hong, Xiaoqing Guan, Qiliang Lai, Dehua Yu, Zhongwei Chen, Xiaoteng Fu, Beibei Zhang, Changkun Chen, Zongze Shao, Jinmei Xia, Jiang-Jiang Qin, Weiyi Wang
Summary: A new meroterpenoid, taladrimanin A (1), was isolated from a marine-derived fungus, and its structure and activity were studied. Compound 1 showed inhibitory activity against gastric cancer cells and certain bacteria.
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Simin Qi, Xiaoqing Guan, Jia Zhang, Dehua Yu, Xuefei Yu, Qinglin Li, Wenjuan Yin, Xiang-Dong Cheng, Weidong Zhang, Jiang-Jiang Qin
Summary: Inhibiting UbcH5c has been identified as a novel and effective strategy for treating pancreatic cancer, and DHPO represents a new class of UbcH5c inhibitor with potential as an anti-pancreatic cancer therapeutic agent.
Article
Pharmacology & Pharmacy
Jing-Li Xu, Li Yuan, Can Hu, Chun-Yan Weng, Han-Dong Xu, Yun-Fu Shi, Ling Huang, Jie-Er Ying, Zhi-Yuan Xu, Jiang-Jiang Qin, Xiang-Dong Cheng
Summary: The combination of TRM extract (TRMBE) and 5-FU can enhance the anticancer activity of 5-FU, prolong the survival time of mice bearing MFC xenograft tumors, and reduce the risk of liver metastasis in gastric cancer. This combination therapy also modulates immune cytokines, reshapes the tumor microenvironment, and improves the therapeutic effects of 5-FU.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Dehua Yu, Simin Qi, Xiaoqing Guan, Wenkai Yu, Xuefei Yu, Maohua Cai, Qinglin Li, Weiyi Wang, Weidong Zhang, Jiang-Jiang Qin
Summary: In this study, the marine-derived natural product terphenyllin was identified to directly interact with STAT3 and exhibit potent anticancer efficacy against gastric cancer through inhibiting the STAT3 signaling pathway.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Xuefei Yu, Xuhang Zhu, Lizhuo Zhang, Jiang-Jiang Qin, Chunlai Feng, Qinglin Li
Summary: This study confirmed the association between PDGFRA and radioiodine resistance in thyroid cancer and developed a prediction model of PDGFRA inhibitors using bioinformatics analysis, machine learning, and molecular docking. A potential PDGFRA inhibitor was identified from a traditional Chinese medicine compound library, which showed significant inhibitory effects on PDGFRA-MAPK pathway activation and improved radioiodine uptake capacity in radioiodine-refractory thyroid cancer.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Oncology
Li Yuan, Jingli Xu, Yunfu Shi, Zhiyuan Jin, Zhehan Bao, Pengcheng Yu, Yi Wang, Yuhang Xia, Jiangjiang Qin, Bo Zhang, Qinghua Yao
Summary: The study found that CD3D protein is highly expressed in gastric cancer tissues and is associated with prognosis and factors such as tumor infiltrating lymphocytes. CD3D may play an important regulatory role in the tumor immune microenvironment of gastric cancer and could potentially serve as a marker for prognosis and immunotherapy response.
FRONTIERS IN ONCOLOGY
(2022)
Review
Oncology
Fei Cao, Can Hu, Zhi-Yuan Xu, Yan-Qiang Zhang, Ling Huang, Jia-Hui Chen, Jiang-Jiang Qin, Xiang-Dong Cheng
Summary: This article introduces the existing treatments for adenocarcinoma of the esophagogastric junction (AEG), including surgical therapy, neoadjuvant therapy, and targeted therapy, and forecasts future research directions.
ANNALS OF TRANSLATIONAL MEDICINE
(2022)
Editorial Material
Biochemistry & Molecular Biology
Jian-ye Zhang, Jiang-Jiang Qin, Dongmei Zhang, Dong-Hua Yang
FRONTIERS IN MOLECULAR BIOSCIENCES
(2022)
Editorial Material
Cell Biology
Yancheng Tang, Liming Wang, Jiangjiang Qin, Yingying Lu, Han-Ming Shen, Hu-Biao Chen
Summary: Inhibition of PINK1-PRKN-mediated mitophagy enhances the anticancer efficacy of magnolol and could be a promising therapeutic strategy for overcoming cancer drug resistance and improving the therapeutic efficacy of anticancer agents.
Article
Biochemistry & Molecular Biology
Jinyun Dong, Jing Yang, Wenkai Yu, Haobin Li, Maohua Cai, Jing-Li Xu, Han-Dong Xu, Yun-Fu Shi, Xiaoqing Guan, Xiang-Dong Cheng, Jiang-Jiang Qin
Summary: The study found that the quinolin-6-yl substituted derivative KL-6 effectively inhibited the growth and invasion of gastric cancer cells, and induced apoptosis. The compound also showed anticancer activity in a mouse model of gastric cancer without significant toxicity. Therefore, KL-6 may be a promising candidate for further research and development of gastric cancer treatment drugs.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Chunxiao Zhu, Xiaoqing Guan, Xinuo Zhang, Xin Luan, Zhengbo Song, Xiangdong Cheng, Weidong Zhang, Jiang-Jiang Qin
Summary: KRAS is the most frequently mutated oncogene in various tumor types and has been considered undruggable due to the lack of classic drug binding sites. However, the development of KRAS inhibitors has made KRAS mutations druggable. Despite remarkable clinical responses, resistance to monotherapy of KRAS inhibitors has been observed. Significant progress has been made in understanding the mechanisms of drug resistance to KRAS-mutant inhibitors.
Article
Pharmacology & Pharmacy
Jing Yang, Lingling Wang, Xiaoqing Guan, Jiang-Jiang Qin
Summary: STAT3 is a critical player in cell signal transmission, making it a promising target for anticancer drug development. Many natural products have been shown to inhibit the STAT3 signaling pathway, demonstrating significant anticancer activities, but there is currently no FDA-approved STAT3 inhibitor.
PHARMACOLOGICAL RESEARCH
(2022)
Article
Microbiology
Dongli Lv, Jinmei Xia, Xiaoqing Guan, Qiliang Lai, Beibei Zhang, Jianhui Lin, Zongze Shao, Sulan Luo, Dongting Zhangsun, Jiang-Jiang Qin, Weiyi Wang
Summary: Two new bioactive compounds were isolated from a deep-sea-derived fungus and their structures were determined. Compounds 1, 5-7 exhibited significant inhibition against Staphylococcus aureus, while compound 8 showed potent reduction in cell viability of gastric cancer cells.
FRONTIERS IN MICROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Handong Xu, Can Hu, Yi Wang, Yunfu Shi, Li Yuan, Jingli Xu, Yanqiang Zhang, Jiahui Chen, Qin Wei, Jiangjiang Qin, Zhiyuan Xu, Xiangdong Cheng
Summary: Gastric cancer (GC) is a deadly malignancy that requires new therapeutic targets for effective treatment. Glutathione peroxidase-2 (GPx2) was found to be overexpressed in clinical GC samples and negatively correlated with prognosis. Knockdown of GPx2 inhibited GC progression and metastasis by suppressing the KYNU-kyn-AhR signaling pathway, which was activated by reactive oxygen species (ROS) accumulation.