Article
Cell Biology
Fumimasa Tomooka, Kosuke Kaji, Norihisa Nishimura, Takahiro Kubo, Satoshi Iwai, Akihiko Shibamoto, Junya Suzuki, Koh Kitagawa, Tadashi Namisaki, Takemi Akahane, Akira Mitoro, Hitoshi Yoshiji
Summary: In this study, the effects of the combination of SFN and GEM on human iCCA cell growth were assessed. The results showed that SFN inhibited cell proliferation and invasion, induced cell cycle arrest and apoptosis, and suppressed angiogenesis and EMT in iCCA cells. Combination therapy with SFN and GEM had better therapeutic effects than single agent treatment.
Article
Biochemistry & Molecular Biology
Jeonghyeon Seo, Da Eun Lee, Seong Mi Kim, Eunjung Kim, Jin-Kyung Kim
Summary: The study found that LicA, a major active component of licorice, has anticancer activity against ovarian cancer cells. LicA inhibited cell viability and induced G2/M phase arrest in SKOV3 cells. LicA also induced apoptosis by increasing reactive oxygen species levels, reducing mitochondrial membrane potential, and promoting caspase activation and cytochrome c release. Furthermore, LicA reduced STAT3 protein levels and downstream signaling, suggesting its potential as an anti-cancer agent.
Article
Oncology
Haini Wang, Junli Zuo
Summary: Overexpressed survivin is associated with worse survival of several types of human tumors. In this study, the antitumor activity of shikonin in non-small-cell lung cancer (NSCLC) by regulating survivin pathway was investigated. Result showed that shikonin inhibited the NSCLC H1299 cell proliferation in a dose-dependent manner. Moreover, shikonin fits well with survivin by molecular docking. Shikonin also inhibited the mRNA expression and protein level of survivin in H1299 cells. Shikonin arrested H1299 cell cycle at the G0/G1 phase by regulating CDK/cyclin family members. In addition, shikonin regulated the expression of X-linked inhibitor of apoptosis- (XIAP-) mediated caspases 3 and 9, thus leading to the damage of mitochondrial membrane potential and induction of H1299 cell apoptosis. Overall, shikonin inhibited H1299 cell growth by inducing apoptosis and blocking the cell cycle. The underlying mechanism involves targeting survivin, which subsequently regulates the protein expression of XIAP/caspase 3/9, CDK2/4, and cyclin E/D1. Thus, shikonin, a survivin inhibitor, is a promising therapeutic strategy in NSCLC treatment.
ANALYTICAL CELLULAR PATHOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Li-wen Ren, Wan Li, Xiang-jin Zheng, Jin-yi Liu, Yi-hui Yang, Sha Li, Sen Zhang, Wei-qi Fu, Bin Xiao, Jin-hua Wang, Guan-hua Du
Summary: Analysis of hub genes in GBM revealed benzimidazoles as potential anti-GBM agents, with in vivo studies showing their efficacy in suppressing tumor growth.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Medicine, Research & Experimental
Nuria Mut-Salud, Juan J. Guardia, Antonio Fernandez, Isabel Blancas, Houda Zentar, Jose M. Garrido, Enrique Alvarez-Manzaneda, Rachid Chahboun, Fernando Rodriguez-Serrano
Summary: In this study, the antitumor activity of taiwaniaquinoids, specifically compound C36, was investigated in vitro and in vivo. Results showed that C36 exhibited significant antitumor effects on MCF-7 cells by inducing apoptosis through caspase 9 activation and an increase in the Bax/Bcl-2 ratio. In vivo experiments also demonstrated the efficacy of C36 in reducing tumor growth and improving survival rates in immune-competent C57BL/6 mice implanted with E0771 mouse mammary tumor cells.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Biochemistry & Molecular Biology
Reihaneh Fatehi, Marzieh Rashedinia, Amin Reza Akbarizadeh, Mozhdeh Zamani, Negar Firouzabadi
Summary: This study investigated the effect of metformin in combination with resveratrol and cisplatin on MCF-7 cells. The results showed that metformin inhibited cell proliferation, while resveratrol suppressed proliferation through induction of apoptosis and cell cycle arrest. The triple combination of metformin, resveratrol, and cisplatin exhibited a significant inhibitory effect through the induction of autophagy-mediated cell death, apoptosis, and cell cycle arrest. These findings support the anti-cancer properties of metformin and resveratrol, and suggest their potential synergistic effects in combination therapy.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2023)
Article
Pharmacology & Pharmacy
Catarina Teixeira-Guedes, Ana Rita Bras, Ricardo G. Teixeira, Andreia Valente, Ana Preto
Summary: This study evaluated the anti-cancer properties and mechanisms of action of ruthenium complexes in the treatment of colorectal cancer (CRC). The complexes displayed high bioactivity by reducing cell proliferation, inducing cell cycle arrest, increasing apoptosis, and inhibiting MEK/ERK and PI3K/AKT signaling pathways. The complexes also decreased cellular clonogenic ability and cell migration by disrupting F-actin cytoskeleton integrity, making them promising as a new therapeutic strategy for CRC treatment.
Article
Multidisciplinary Sciences
Zhijie Cao, Ning Kon, Yajing Liu, Wenbin Xu, Jia Wen, Han Yao, Mi Zhang, Zhen Wu, Xiaojun Yan, Wei-Guo Zhu, Wei Gu, Donglai Wang
Summary: The study revealed that PD-1 in cancer cells is a direct target of the tumor suppressor p53, with its transcription being influenced by acetylation of p53. Acetylated p53 enhances PD-1 transcription, facilitating activation of cancer cell-intrinsic PD-1 and inhibiting tumor growth.
Article
Chemistry, Multidisciplinary
Jin-yi Liu, Wei-qi Fu, Xiang-jin Zheng, Wan Li, Li-wen Ren, Jin-hua Wang, Cui Yang, Guan-hua Du
Summary: Avasimibe demonstrated potent anticancer effects on human glioblastoma cells by inhibiting proliferation, inducing apoptosis, and regulating multiple signaling pathways. The drug showed promising potential as a chemotherapy treatment for glioblastoma.
ACTA PHARMACOLOGICA SINICA
(2021)
Article
Biochemistry & Molecular Biology
Daoyu Zhang, Xinglan An, Hao Yu, Ziyi Li
Summary: Breast cancer, especially triple-negative breast cancer, is challenging to treat due to the lack of therapeutic targets. The drug thioguanine has shown antitumor effects and may potentially affect tumor pathways by down-regulating key genes. Competitive endogenous ribonucleic acids may play a role in the regulation of these pathways and could serve as potential targets for alternative breast cancer treatments.
BIOSCIENCE REPORTS
(2021)
Article
Engineering, Biomedical
Simzar Hosseinzadeh, Hojjatollah Nazari, Elaheh Esmaeili, Shadie Hatamie
Summary: Curcumin nanoparticles modified by PEG were successfully developed and showed promising anticancer effects, especially for the treatment of thyroid cancer. The nanoparticles exhibited high efficiency and stability, as confirmed by various evaluation parameters and experimental data.
JOURNAL OF MATERIALS SCIENCE-MATERIALS IN MEDICINE
(2021)
Article
Biochemistry & Molecular Biology
Waleed A. Badawi, Mohamed Samir, Hazem M. Fathy, Tarek M. Okda, Mohamed H. Noureldin, Gamal M. K. Atwa, Omaima M. AboulWafa
Summary: This study focused on the signaling pathway of adenosine diphosphate receptor α1 in lingual osteoblasts and found that hydrazine methyl isoindole has selectivity towards adenosine diphosphate receptor α1. Compared to other pathway inhibitors, hydrazine methyl isoindole shows better selectivity. Furthermore, hydrazine methyl isoindole exhibits significant inhibitory effects on the activity and function of adenosine diphosphate receptor α1 in lingual osteoblasts.
BIOORGANIC CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Magdalena Markowicz-Piasecka, Karol Sadowski, Johanna Huttunen, Joanna Sikora, Kristiina M. Huttunen
Summary: Transporter-mediated cellular uptake of sulfonamide-based derivatives of metformin exhibited strong cytotoxic effects, inducing apoptosis and cell cycle arrest in breast cancer cells. These results suggest the potential of biguanides as anti-cancer agents through effective intracellular transport.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Mohammad Mahdi Vahedi, Ali Shahini, Mehran Mottahedi, Setareh Garousi, Seyed Ali Shariat Razavi, Ghazaleh Pouyamanesh, Amir R. Afshari, Gordon A. Ferns, Afsane Bahrami
Summary: This study investigates the anti-tumor activity of harmaline on glioblastoma cells. The results demonstrate that harmaline inhibits cell proliferation, induces cell cycle arrest and apoptosis. Additionally, harmaline suppresses metastasis and migration of the cells.
MOLECULAR BIOLOGY REPORTS
(2023)
Article
Biochemistry & Molecular Biology
Qinqin Xu, Ryan P. Mackay, Adam Y. Xiao, John A. Copland, Paul M. Weinberger
Summary: ATC is a highly lethal malignancy with no effective treatment currently available. YM155, identified as a promising candidate in a high-throughput screen, shows potential as a targeted therapy for ATC by inhibiting proliferation of cancer cells while sparing normal cells, inducing DNA damage, cell cycle arrest, and apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Ning-Yu Wang, Ying Xu, Kun-Jie Xiao, Wei-Qiong Zuo, Yong-Xia Zhu, Rong Hu, Wan-Li Wang, Yao-Jie Shi, Luo-Ting Yu, Zhi-Hao Liu
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2020)
Article
Oncology
Ying Xu, Qianqian Wang, Kunjie Xiao, Zhihao Liu, Lifeng Zhao, Xuejiao Song, Xi Hu, Zhanzhan Feng, Tiantao Gao, Weiqiong Zuo, Jun Zeng, Ningyu Wang, Luoting Yu
MOLECULAR CANCER THERAPEUTICS
(2020)
Article
Pharmacology & Pharmacy
Qingqing Dai, Yuhang Yan, Xiangli Ning, Gen Li, Junlin Yu, Ji Deng, Lingling Yang, Guo-Bo Li
Summary: AncPhore is a versatile tool for drug discovery that improves prediction ability on different types of target proteins by analyzing pharmacophore features and using anchor pharmacophores. It has the potential to efficiently identify new inhibitors for various protein targets.
ACTA PHARMACEUTICA SINICA B
(2021)
Article
Chemistry, Medicinal
Zhihao Liu, Xi Hu, Qiwei Wang, Xiuli Wu, Qiangsheng Zhang, Wei Wei, Xingping Su, Hualong He, Shuyan Zhou, Rong Hu, Tinghong Ye, Yongxia Zhu, Ningyu Wang, Luoting Yu
Summary: This study presents a novel strategy for treating cancer by targeting proteasomal degradation to block the oncogenic activity of EZH2, offering a new approach compared to current EZH2 inhibitors.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Rong Hu, Wan-Li Wang, Kun-Jie Xiao, Ning-Yu Wang
Summary: Cell-based screening led to the discovery of 9-sulfonyl-9(H)-purine as a new scaffold for HCV inhibitors. However, these inhibitors were found to be unstable in certain mediums, with the sulfonamide bond at the 9-position being the primary degradation site. Further analysis of degradation species is needed to determine the main active components and direct target for these molecules.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2021)
Article
Chemistry, Medicinal
Kai Ran, Jun Zeng, Guoquan Wan, Xiaojie He, Zhanzhan Feng, Wang Xiang, Wei Wei, Xiang Hu, Ningyu Wang, Zhihao Liu, Luoting Yu
Summary: The study describes the design and synthesis of pyrido[1,2-a]pyrimidinone derivatives as potent FGFR inhibitors, with candidate 23d showing excellent potency and kinase selectivity for the FGFR family. 23d also exhibited potent antitumor activity in FGFR2-amplified gastric cancer xenograft model, suggesting it as a promising candidate for further drug development.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Shuo Yuan, Bo Wang, Qing-Qing Dai, Xiao-Nan Zhang, Jing-Ya Zhang, Jia-Hui Zuo, Hui Liu, Zhe-Sheng Chen, Guo-Bo Li, Shaomeng Wang, Hong-Min Liu, Bin Yu
Summary: YS-370 is a highly effective P-gp inhibitor capable of reversing multidrug resistance and achieving good results when administered orally. The inhibitor does not alter the expression or subcellular localization of P-gp, but increases the intracellular accumulation of drugs.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Zihao Shen, Yu-Hang Yan, Shuo Yang, Sang Zhu, Yuan Yuan, Zhiqiang Qiu, Huan Jia, Ruiqiong Wang, Guo-Bo Li, Honglin Li
Summary: Protein kinases play a central role in signal transduction and are important drug targets for therapeutic intervention. The ProfKin web server, based on the KinLigDB database, provides a versatile tool for structure-based kinase profiling, offering a wealth of information to guide drug discovery and development.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Rong Hu, Wan-Li Wang, Ying-Yue Yang, Xia-Tong Hu, Qi-Wei Wang, Wei-Qiong Zuo, Ying Xu, Qiang Feng, Ning-Yu Wang
Summary: This study designed and synthesized a specific and potent BRD4-PROTAC with excellent selective cytotoxicity, showing significant anticancer activity in prostate cancer cell lines, which could be a promising drug candidate for AR-positive prostate cancer.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Wei Wei, Zhanzhan Feng, Zhihao Liu, Xinyue Li, Hualong He, Kai Ran, Yaojie Shi, Yongxia Zhu, Tinghong Ye, Chao Gao, Ningyu Wang, Luoting Yu
Summary: Focal adhesion kinase (FAK) is a potential therapeutic target for ovarian cancer. This study discovered a potent FAK inhibitor (36) that showed inhibitory activities against FAK signaling in vitro and demonstrated potential for treating ovarian cancer in in vivo studies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Gen Li, Qing-Qing Dai, Guo-Bo Li
Summary: Metalloenzymes are enzymes that rely on metal ions, and comparing their active sites is crucial for enzyme design, function research, and inhibitor development. MeCOM is a method for comparing metalloenzyme active sites, which can accurately identify and compare active sites, evaluate similarity, and establish new associations between metalloenzymes.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Article
Chemistry, Medicinal
You-Cai Xiao, Jun-Lin Yu, Qing-Qing Dai, Gen Li, Guo-Bo Li
Summary: Metalloenzymes play critical roles in biological processes and are important therapeutic targets. This perspective focuses on the importance of exploiting metal-binding pharmacophores, specifically boron-containing MBPs, in inhibitor development targeting metalloenzymes. The challenges and design concepts regarding boron-containing MBPs are discussed, with emphasis on the unique binding modes with metalloenzyme active sites.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Medicine, Research & Experimental
Qiangsheng Zhang, Xinyi Chen, Xi Hu, Xianjie Duan, Guoquan Wan, Lu Li, Qiang Feng, Yiqian Zhang, Ningyu Wang, Luoting Yu
Summary: This study designed and synthesized a new series of compounds, among which SKLB-03176 was identified as a potent EZH2 covalent inhibitor. It was found that SKLB-03176 selectively bound to the SAM pocket of EZH2, exhibited weak activity against other targets, and inhibited the expression of H3K27Me3 in cells without cytotoxicity to normal cells.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Chemistry, Medicinal
Shu-Yan Zhou, Xin-Yi Chen, Yan Chen, Na-Na Meng, Xin Tao, Hua-Long He, Zhi-Hao Liu, Ning-Yu Wang, Luo-Ting Yu
Summary: This study developed a fixed-dose combination treatment for chronic hepatitis C, containing two inhibitors, and improved the dissolution behavior of one of the drugs through co-micronizing. Pharmacokinetic studies showed that the characteristics of the combination treatment were similar to those of tablets containing the drugs separately.
Article
Chemistry, Multidisciplinary
Qiangsheng Zhang, Xi Hu, Lu Li, Lidan Zhang, Guoquan Wan, Qiang Feng, Yongxia Zhu, Ningyu Wang, Zhihao Liu, Luoting Yu
Summary: SKLB-0335 displays high paralog-selectivity on EZH2 by targeting its unique Cys663, covalently binding to EZH2 at its S-adenosylmethionine (SAM) pocket and inhibiting H3K27Me3. This compound could serve as an effective chemical probe to further investigate the specific biological functions of EZH2.
CHEMICAL COMMUNICATIONS
(2021)
Review
Oncology
Xinru Zhou, Yin Jia, Chuanbin Mao, Shanrong Liu
Summary: Small extracellular vesicles (sEVs), such as exosomes, have emerged as crucial targets for liquid biopsy and promising drug delivery vehicles in tumor progression. They can serve as biomarkers for tumor diagnosis and as drug carriers for cancer treatment.
Article
Oncology
Ruochan Chen, Ju Zhu, Xiao Zhong, Jie Li, Rui Kang, Daolin Tang
Summary: The interplay between autophagy and apoptosis plays a crucial role in tumorigenesis and cancer therapy, with HMGB1 serving as a key regulator in these processes.
Article
Oncology
Zongfu Pan, Xixuan Lu, Tong Xu, Jinming Chen, Lisha Bao, Ying Li, Yingying Gong, Yulu Che, Xiaozhou Zou, Zhuo Tan, Ping Huang, Minghua Ge
Summary: This study uncovered the emerging role of HN1 in promoting dedifferentiation of anaplastic thyroid cancer (ATC) cells. HN1 negatively regulated the thyroid differentiation markers and had an inhibitory effect on the transcriptional activation of CTCF, thereby influencing the chromatin accessibility of thyroid differentiation genes.
Article
Oncology
Yi Qin, Shengjun Xiong, Jun Ren, Gautam Sethi
Summary: Autophagy plays an important regulatory role in glioblastoma, and its dysregulation can lead to drug resistance and radioresistance. It also affects stem cell characteristics, overall growth, and metastasis. Therefore, autophagy is a promising target for glioblastoma therapy.
Article
Oncology
Katsuya Nagaoka, Xuewei Bai, Dan Liu, Kevin Cao, Joud Mulla, Chengcheng Ji, Hongze Chen, Muhammad Azhar Nisar, Amalia Bay, William Mueller, Grace Hildebrand, Jin-Song Gao, Shaolei Lu, Hiroko Setoyama, Yasuhito Tanaka, Jack R. Wands, Chiung-Kuei Huang
Summary: This study found that serum 2-OG levels in cholangiocarcinoma patients are associated with the effectiveness of chemotherapy. Patients with progressive disease showed significantly higher levels of serum 2-OG compared to stable disease and partial response patients. The study also revealed that overexpression of ASPH mimics the effects of 2-OG, and knockdown of ASPH improves chemotherapy. Targeting ASPH enhances the effects of chemotherapy by modulating ATM and ATR, two key regulators of DDRs.