Article
Biochemistry & Molecular Biology
In Hwan Lim, Seung Jae Lee, Byoung-Soo Shin, Hyun Goo Kang
Summary: This study aimed to confirm clopidogrel resistance (CR), identify its influencing factors, and evaluate the effect of combination therapy with ilaprazole on clopidogrel. The results showed that age and alcohol consumption were factors influencing clopidogrel metabolism, and the combination of ilaprazole and clopidogrel did not interfere with clopidogrel metabolism.
Review
Multidisciplinary Sciences
Ningna Weng, Zhe Zhang, Yunhan Tan, Xiaoyue Zhang, Xiawei Wei, Qing Zhu
Summary: This article summarizes the background, aim, and key scientific concepts of repurposing antifungal drugs for cancer therapy, and discusses the challenges and perspectives for their future development and clinical applications.
JOURNAL OF ADVANCED RESEARCH
(2023)
Review
Biochemistry & Molecular Biology
Vladlena S. Makeeva, Nadezhda S. Dyrkheeva, Olga I. Lavrik, Suren M. Zakian, Anastasia A. Malakhova
Summary: The spectrum of neurodegenerative diseases is extensive, and their research and treatment are complex and diverse. Despite years of research on common pathologies, like Alzheimer's and Parkinson's, cures have not been found. However, Huntington's disease, although affecting a smaller population, still attracts researchers. Understanding the mechanisms of this orphan disease is challenging, but accumulated data provide a foundation for further research.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Lui Ng, Dominic Chi-Chung Foo, Carlos King-Ho Wong, Abraham Tak-Ka Man, Oswens Siu-Hung Lo, Wai-Lun Law
Summary: This study investigated the potential of DPP4-inhibitors in treating CRC patients, and found that DPP4-inhibitor treatment was associated with a significantly better 5-year prognosis following curative resection compared to metformin treatment. The study also showed an association between patient prognosis and immune cell population features, suggesting that immune cell profiles may serve as a biomarker for predicting patient prognosis in response to DPP4-inhibitor treatment.
Review
Oncology
Vikram Shaw, Suyash Srivastava, Sanjay K. Srivastava
Summary: The recent development of high throughput compound screening has allowed for drug repurposing, leading to the discovery of FDA-approved antipsychotic drugs like fluspirilene, penfluridol, and pimozide, which have shown promising anti-cancer effects in various cancer types by inhibiting proliferation and inducing apoptosis and suppressing metastasis.
SEMINARS IN CANCER BIOLOGY
(2021)
Article
Chemistry, Medicinal
Hafiza N. Saleem, Summara Kousar, Ammar Hassan Jiskani, Iqra Sohail, Amir Faisal, Muhammad Saeed
Summary: Dengue fever, a neglected vector-borne disease, is more prevalent in Asia and currently has no specific treatment. Drug repurposing from a library of small anticancer molecules found four potent inhibitors of the dengue virus NS2B/NS3 protease, namely ABT263, ABT737, AT101, and TW37. These inhibitors have the potential to be developed into specific anti-dengue therapeutics.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Muratcan Mentes, Cihangir Yandim
Summary: In this study, potential inhibitors for PPA1 enzyme were identified through molecular docking and subsequent molecular dynamics analyses. Devazepide and quinotolast were found to have higher binding affinities and could be considered for repurposing studies. These results not only reveal the clinical potential of PPA1 inhibition, but also provide valuable insights for future compound development.
JOURNAL OF CELLULAR BIOCHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Muthu Kumar Thirunavukkarasu, Utid Suriya, Thanyada Rungrotmongkol, Ramanathan Karuppasamy
Summary: The RAS-RAF-MEK-ERK pathway plays a key role in tumor progression. MEK inhibition is a promising strategy, but drug resistance remains a major challenge. This study used virtual screening to discover dual-targeting therapy and identified lead compounds with significant binding capability to both MEK and PIM1. The results suggest that these compounds could be of therapeutic interest in overcoming drug resistance in the future.
Article
Pharmacology & Pharmacy
Noor Mazin Abdulkareem, Raksha Bhat, Reid T. Powell, Soumya Chikermane, Soham Yande, Lisa Trinh, Hala Y. Abdelnasser, Mantasha Tabassum, Alexis Ruiz, Mary Sobieski, Nghi D. Nguyen, Jun Hyoung Park, Camille A. Johnson, Benny A. Kaipparettu, Richard A. Bond, Michael Johnson, Clifford Stephan, Meghana V. Trivedi
Summary: Drug repurposing can overcome the challenges of cost and time in new drug discovery for cancer treatment. In this study, GPCR-targeting drugs were evaluated for their potential in triple-negative breast cancer and drug-resistant HER2+ breast cancer. Nebivolol, a beta-adrenergic receptor-targeting drug, was identified as a promising candidate with inhibitory effects on growth and metastasis in breast cancer cell lines.
FRONTIERS IN PHARMACOLOGY
(2022)
Review
Cell Biology
Ziping Han, Lingzhi Li, Yuyou Huang, Haiping Zhao, Yumin Luo
Summary: Accumulating evidence suggests PBK/TOPK plays a role in mitosis and cell-cycle progression, with potential therapeutic implications in cancer. However, further research is needed to understand the applicability of PBK/TOPK inhibitors in clinical practice, given their overexpression in normal and pathological proliferative cells.
Review
Oncology
Liese Vandeborne, Pan Pantziarka, An M. T. Van Nuffel, Gauthier Bouche
Summary: This review summarizes research activities using approved vaccines to treat cancer, with data supporting cancer therapeutic use for 16 vaccines. Clinical trials have been conducted or are ongoing for 10 vaccines, while preclinical evidence supports further evaluation of the remaining 6 vaccines.
FRONTIERS IN ONCOLOGY
(2021)
Review
Chemistry, Medicinal
Hui Zhou, Hongdou Liu, Yan Yu, Xiao Yuan, Ling Xiao
Summary: Drug repurposing, as a more efficient and economical strategy, has been significantly accelerated by the development of information technology. In breast cancer treatment, in silico approaches such as transcriptomic signature matching and simulated structure docking have shown remarkable achievements.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2023)
Article
Pharmacology & Pharmacy
Yuqi Yang, Zhuo-Xun Wu, Jing-Quan Wang, Qiu-Xu Teng, Zi-Ning Lei, Sabrina Lusvarghi, Suresh V. Ambudkar, Zhe-Sheng Chen, Dong-Hua Yang
Summary: OTS964 is a potent inhibitor of TOPK that interacts with ABCG2 to affect multidrug resistance, and has an upregulating effect on ABCG2 transporter. It enhances resistance to ABCG2 substrate-drugs by inhibiting efflux function mediated by ABCG2.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Oncology
Aurora Gonzalez-Fierro, Alfonso Duenas-Gonzalez
Summary: Drug repurposing for cancer therapy is a hot topic of research with potential advantages of being faster, safer, easier, and cheaper. However, economic barriers are the main challenge in clinical development, hindering the acceptance of repositioned drugs as standard therapy at low cost.
SEMINARS IN CANCER BIOLOGY
(2021)
Review
Oncology
Derek B. Oien, Christopher L. Pathoulas, Upasana Ray, Prabhu Thirusangu, Eleftheria Kalogera, Viji Shridhar
Summary: Quinacrine, originally an antimalarial drug, has been rediscovered as an anticancer agent due to its multiple mechanisms including inhibition of cancer cell growth and DNA repair processes. Its potential in treating aggressive tumors such as high grade serous ovarian cancer has been highlighted in recent studies.
SEMINARS IN CANCER BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Wang Wang, Liangliang Xiong, Yutong Li, Zhuorui Song, Dejuan Sun, Hua Li, Lixia Chen
Summary: Three series of lathyrane diterpenoid derivatives were designed and synthesized, with compound 23d showing excellent inhibitory activity and potential as a promising anti-inflammatory agent for further exploration.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Xuechen Zhou, Mengzhu Zheng, Na Zhao, Yixin Hu, Kaiyin Yang, Junfeng Huo, Guangyuan Liu, Jiangeng Huang, Lixia Chen, Yirong Zhou, Hua Li
Summary: Isocitrate dehydrogenases 1 (IDH1) is the most frequently mutated metabolic gene in human cancer, and its mutations interfere with cell metabolism and epigenetic regulation, promoting tumorigenesis. In this study, a series of linear unnatural peptide analogues were designed, synthesized, and evaluated as potential mutant IDH1 inhibitors. Compound 43 showed strong inhibitory activity and binding affinity towards mutant IDH1, and it could effectively decrease the cellular concentration of 2-HG and suppress the proliferation of HT1080 and IDH1 mutant-U-87 cells.
BIOORGANIC CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Wang Wang, Yutong Li, Yan Li, Dejuan Sun, Hua Li, Lixia Chen
Summary: Natural products are important sources of biologically active compounds, with oleanolic acid (OA) being one of the most studied pentacyclic triterpenes. Through chemical modification, derivatives of OA with multiple bioactivities can be prepared. This review summarizes recent studies on OA derivatives (2016-present) and their biological effects and mechanisms of action in vitro and in vivo models, as well as discusses the design of novel and potent derivatives.
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Zhuorui Song, Yueying Yang, Yanli Wu, Mengzhu Zheng, Dejuan Sun, Hua Li, Lixia Chen
Summary: This review summarizes the structure and function of GOT1 and its important roles in cell proliferation and cancer progression, and also discusses the characteristics of GOT1 inhibitors. It provides new insights into the discovery of potential anti-GOT1 drugs for cancer treatment.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2022)
Review
Chemistry, Medicinal
Wang Wang, Yueying Yang, Yang Liu, Dejuan Sun, Hua Li, Lixia Chen
Summary: Researchers have prepared numerous bioactive derivatives of andrographolide through chemical modification and classified them according to their biological activities. These studies contribute to the development of novel therapeutic drugs.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Gui-Yang Xia, Shi-Jie Cao, Li-Xia Chen, Feng Qiu
Summary: This review summarizes the latest progress and perspectives on the promising natural withanolides, covering structural classification, biological activities and mechanisms, metabolism and pharmacokinetic investigations, biosynthesis, chemical synthesis and structural modifications, as well as future research directions.
NATURAL PRODUCT REPORTS
(2022)
Article
Chemistry, Applied
Yang Xu, Na Zhang, Liangliang Xiong, Dejuan Sun, Zhuangzhuang Chen, Lixia Chen
Summary: A new compound was isolated from the rhizome of Smilax china, along with twelve known compounds for the first time. The structure of the new compound was elucidated based on chemical evidences and spectral data analysis. In addition, the inhibitory effects of the compounds on NO production were tested, and compound 7 showed significant inhibitory effect.
NATURAL PRODUCT RESEARCH
(2023)
Review
Biochemistry & Molecular Biology
Yutong Li, Linlin Zhang, Wang Wang, Yang Liu, Dejuan Sun, Hua Li, Lixia Chen
Summary: Cage-like compounds found in natural products have diverse structures and significant biological activities, playing an important role in drug discovery. The development and utilization of these compounds have become a research hotspot in the fields of chemistry and biology.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Yang Xu, Huiru Xie, Hongbo Chen, Liangliang Xiong, Kuiru Sa, Xuanbin Wang, Hua Li, Lixia Chen
Summary: A new triterpenoid with anti-inflammatory activity was isolated from Abelia macrotera, along with known terpenoids and phenylpropanoids.
CHEMISTRY & BIODIVERSITY
(2022)
Article
Chemistry, Medicinal
Na Zhang, Liang-Liang Xiong, De-Juan Sun, Man Zhu, Zi-Yuan Zhao, Hua Li, Li-Xia Chen
Summary: Four pairs of undescribed scalemic mixtures of chromane and chromene meroterpenoids (1a/1b-4a/4b) were isolated from Rhododendron dauricum L. The compounds demonstrated anti-inflammatory activity by inhibiting nitric oxide production in LPS-induced macrophage cells. Compound 4b exhibited significant anti-inflammatory activity and could be explored as a potential lead compound for the development of anti-inflammatory drugs.
Review
Cell Biology
Yanmei Chen, Jiahui Zhang, Yueying Yang, Ke Xiang, Hua Li, Dejuan Sun, Lixia Chen
Summary: Kynurenine-3-monooxygenase (KMO) plays a crucial role in the tryptophan metabolism pathway and its dysregulation may be involved in the pathogenesis of various diseases such as neurodegenerative diseases, psychosis, and cancer.
JOURNAL OF CELLULAR PHYSIOLOGY
(2022)
Article
Chemistry, Medicinal
Chunyang Zou, Jinyu Men, Yingjin Qu, Chunfeng Jiang, Yao Wang, Lixia Chen, Lei Yuan
Summary: Using AI78-38 as the lead compound, the researchers designed and synthesized amide derivatives and discovered that compound 10 exhibited strong inhibitory ability against influenza A virus. Compound 10 also showed good bioavailability and improved ADMET properties compared to AI78-38.
MEDICINAL CHEMISTRY RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Yali Wang, Dejuan Sun, Qinghua Jiang, Liangliang Xiong, Na Zhang, Yingni Pan, Hua Li, Lixia Chen
Summary: The Euphorbia plant is a valuable source for natural product drug discovery. This study discovered eight new diterpenoids from Euphorbia wallichii, including a rare pentacyclic diterpenoid with inhibitory activity on NO production. Bioassays and mechanistic studies revealed its potential in suppressing inflammation.
Article
Biochemistry & Molecular Biology
Jing Liang, Mengzhu Zheng, Wei Xu, Yongkang Chen, Piyu Tang, Guoyi Wu, Peng Zou, Hua Li, Lixia Chen
Summary: This study discovered Acriflavine and Proflavine Hemisulfate as inhibitors of Mpro, showing good inhibitory activity against the SARS-CoV-2 virus.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Chengfeng Gao, Man Zhu, Wei Xu, Yali Wang, Liangliang Xiong, Dejuan Sun, Minge Sun, Yu Lin, Hua Li, Lixia Chen
Summary: Amomum villosum Lour. is a medicinal and edible plant. The stems and leaves of A. villosum, which are usually treated as waste, were found to contain various chemical components, including four undescribed compounds and 41 known compounds. Some of these compounds showed anti-inflammatory and antioxidant activities, with the new compound 1 exhibiting significant antioxidant effect through the activation of NRF2/HO-1 pathways. Therefore, the stems and leaves of A. villosum may serve as a potential medicine or dietary supplement for preventing and treating diseases resulting from inflammation and oxidative stress.
BIOORGANIC CHEMISTRY
(2023)
