Article
Multidisciplinary Sciences
Lynette Steele, Aarren J. Mannion, Gary Shaw, Kenneth A. Maclennan, Graham P. Cook, Christopher E. Rudd, Alison Taylor
Summary: GSK-3 plays a crucial role in T cell function and tumor immunity, with the isoforms GSK-3α and GSK-3β having differential effects on immune responses and tumor infiltration, working together to control PD-1 expression and tumor growth.
Article
Biochemistry & Molecular Biology
Wagdy M. Eldehna, Sara T. Al-Rashood, Tarfah Al-Warhi, Razan O. Eskandrani, Amal Alharbi, Ahmed M. El Kerdawy
Summary: In this study, three series of oxindole-benzofuran hybrids were designed and synthesised as dual CDK2/GSK-3 beta inhibitors targeting breast cancer. The N-1 -unsubstituted oxindole derivatives showed potent cytotoxic activity, while the N-1-substituted derivatives exhibited moderate to weak activity on breast cancer cell lines. The most potent compounds caused cell cycle arrest in the G2/M phase by inhibiting CDK2/GSK-3 beta, as demonstrated by enzyme inhibition assays and molecular docking studies.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2021)
Review
Oncology
Alberto M. Martelli, Camilla Evangelisti, Francesca Paganelli, Francesca Chiarini, James A. McCubrey
Summary: GSK-3 consists of two isoforms, alpha and beta, that are constitutively active but can be inactivated through phosphorylation by upstream kinases. It was initially considered a tumor suppressor, but it has also been found to have oncogenic properties in promoting pathways critical for cancer cell proliferation, survival, and drug-resistance.
Article
Chemistry, Medicinal
Richard A. Hartz, Vijay T. Ahuja, Guanglin Luo, Ling Chen, Prasanna Sivaprakasam, Hong Xiao, Carol M. Krause, Wendy J. Clarke, Songmei Xu, John S. Tokarski, Kevin Kish, Hal Lewis, Nicolas Szapiel, Ramu Ravirala, Sayali Mutalik, Deepa Nakmode, Devang Shah, Catherine R. Burton, John E. Macor, Gene M. Dubowchik
Summary: Glycogen synthase kinase-3 (GSK-3) is a crucial regulator of cellular functions, implicated in diseases such as Alzheimer's disease, mood disorders, diabetes, and cancer. Its role in the production of abnormal tau protein in neurofibrillary tangles associated with Alzheimer's disease has been established. The synthesis and evaluation of pyrimidine-based GSK-3 inhibitors led to the identification of highly potent compounds that effectively lowered phosphorylated tau levels in a mouse model of Alzheimer's disease.
JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Dilipkumar Pal, Souvik Mukherjee, In-Ho Song, Satish B. Nimse
Summary: Alzheimer's disease is a common form of dementia caused by cognitive function impairment, with research suggesting the involvement of GSK-3 in the hyper-phosphorylation of tau proteins, making it a potential target for AD treatment. Inhibitors of GSK-3 have received significant attention for their potential therapeutic applications in AD and other diseases.
CURRENT DRUG TARGETS
(2021)
Review
Pharmacology & Pharmacy
Chandi C. Kandar, Debanjan Sen, Arindam Maity
Summary: GSK-3 is a crucial protein kinase with two isoforms, GSK-3α and GSK-3β. It plays important roles in cell signaling, gene induction, apoptosis, protein translation, glycogen metabolism, and inflammatory processes.
CURRENT DRUG TARGETS
(2021)
Article
Neurosciences
Shaohui Wang, Yao Jiang, Yabo Liu, Qianhui Liu, Hongwei Sun, Mengjie Mei, Xiaomei Liao
Summary: This study demonstrates that ferroptosis promotes abnormal aggregation of tau protein and may serve as a promising therapeutic target for tauopathies.
MOLECULAR NEUROBIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Davoud Ghazanfari, Mahboubeh S. Noori, Stephen C. Bergmeier, Jennifer Hines, Kelly D. McCall, Douglas J. Goetz
Summary: COB-187 inhibits GSK3 beta via a specific, reversible, time and Cys-199-dependent mechanism, demonstrating high selectivity and potent activity against the target enzyme.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Yuko Nagao, Kikuko Amo-Shiinoki, Hiroko Nakabayashi, Masayuki Hatanaka, Manabu Kondo, Kimie Matsunaga, Masahiro Emoto, Shigeru Okuya, Yukio Tanizawa, Katsuya Tanabe
Summary: Endoplasmic reticulum stress is a key pathogenic factor in type 1 and 2 diabetes. Gsk-3 inhibition prevents proteasomal degradation of ATF4 and alleviates apoptosis by regulating phosphorylation of ATF4-S214. Mechanistically, Gsk-3 inhibition modulates transcription targets of ATF4 and facilitates dephosphorylation of eIF2 alpha under ER stress.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Medicine, Research & Experimental
Nora O. Abdel Rasheed, Weam W. Ibrahim
Summary: This study demonstrates that telmisartan has neuroprotective effects in a rat model of Huntington's disease, improving motor and cognitive dysfunction and reducing oxidative stress, neuro-inflammation, and apoptosis. These effects may be achieved through the activation of peroxisome proliferator activated receptor-gamma and blockade of angiotensin-II receptor type 1.
Article
Chemistry, Medicinal
Zhongwen Luo, Shang Li, Yonglei Zhang, Fucheng Yin, Heng Luo, Xinye Chen, Ningjie Cui, Siyuan Wan, Xinxin Li, Lingyi Kong, Xiaobing Wang
Summary: Neuronal cells overexpressing phosphorylated Tau proteins increase susceptibility to oxidative stress. Regulation of GSK-3 beta and reduction of Tau protein hyperphosphorylation, as well as alleviation of oxidative stress, may be effective in preventing or treating Alzheimer's disease (AD). The compound KWLZ-9e showed potential GSK-3 beta inhibition and neuroprotective capacity, and it could alleviate oxidative stress and improve learning and memory impairments in an AD model, making it a promising lead for AD treatment.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Pharmacology & Pharmacy
Gowru Srivani, Ramyakrishna Sharvirala, Prabhakar Reddy Veerareddy, Dilipkumar Pal, Gangarapu Kiran
Summary: Research has shown that GSK-3 is an effective target for the treatment of diabetes, and its modulation can influence the development of the disease. Synthetic and natural scaffolds play a crucial role in modulating GSK-3 against diabetes.
CURRENT DRUG TARGETS
(2021)
Article
Biochemistry & Molecular Biology
Hsuan-Yeh Pan, Mallika Valapala
Summary: Autophagy is a vital cellular mechanism that ensures cellular maintenance and survival. The GSK-3 signaling pathway regulates autophagy by modulating TFEB and other signaling molecules.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Chemistry, Medicinal
Neha Chauhan, Swati Paliwal, Smita Jain, Kanika Verma, Sarvesh Paliwal, Swapnil Sharma
Summary: Alzheimer's disease is a major health and socioeconomic burden worldwide, characterized by neuronal loss, memory loss, and cognitive impairment. GSK-3 beta plays a significant role in the molecular mechanisms of AD progression, making it a potential therapeutic target for the disease.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2022)
Article
Neurosciences
Xue-Hua Wang, Zhong-Fu Zuo, Lu Meng, Qi Yang, Pan Lv, Li-Pan Zhao, Xiao-Bai Wang, Yu-Fei Wang, Ying Huang, Cong Fu, Wen-Qiang Liu, Xue-Zheng Liu, De-Yu Zheng
Summary: The study aimed to investigate the effects and mechanisms of salidroside on hippocampal neurons in streptozotocin-induced diabetic mice. The results showed that salidroside could improve cognitive function, increase the number of hippocampal neurons, and promote the activation of the PI3K/Akt/GSK-3 beta signaling pathway in diabetic mice. This study revealed a partial mechanism by which salidroside exerts neuroprotective effects in diabetic cognitive dysfunction.
PSYCHOPHARMACOLOGY
(2023)
Review
Pharmacology & Pharmacy
Yiming Niu, Qiu Li, Ya Ding, Lei Dong, Chunming Wang
ADVANCED DRUG DELIVERY REVIEWS
(2019)
Article
Engineering, Biomedical
Jingjing Gan, Yunyan Dou, Yurong Li, Zhenzhen Wang, Lintao Wang, Shang Liu, Qiu Li, Heran Yu, Chunyan Liu, Congwei Han, Zhen Huang, Junfeng Zhang, Chunming Wang, Lei Dong
Article
Chemistry, Physical
Qing Ye, Qiu Li, Anhui Gao, Huazhou Ying, Gang Cheng, Jing Chen, Jinxin Che, Jia Li, Xiaowu Dong, Yubo Zhou
CHEMICAL PHYSICS LETTERS
(2019)
Article
Pharmacology & Pharmacy
Zhuojian Sun, Qiu Li, Ranran Hou, Hongxiang Sun, Qihe Tang, Haixia Wang, Zhihui Hao, Songyao Kang, Tianli Xu, Shuang Wu
TOXICOLOGY AND APPLIED PHARMACOLOGY
(2019)
Article
Engineering, Chemical
Ranran Hou, Qiu Li, Jie Liu, Yuanliang Hu
ADVANCES IN POLYMER TECHNOLOGY
(2019)
Article
Biochemistry & Molecular Biology
Yiming Niu, Yuhan Zhang, Wei He, Panfei Xing, Lei Dong, Qiu Li, Chunming Wang
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2020)
Article
Multidisciplinary Sciences
Wei He, Jinzhi Xu, Ruoyu Mu, Qiu Li, Da-lun Lv, Zhen Huang, Junfeng Zhang, Chunming Wang, Lei Dong
NATURE COMMUNICATIONS
(2020)
Article
Pharmacology & Pharmacy
Huan Qin, Wenwen Zhao, Yang Jiao, Haoyi Zheng, Hao Zhang, Jingyu Jin, Qiu Li, Xiuping Chen, Xia Gao, Yantao Han
Summary: The traditional herb pair Salvia miltiorrhiza Bunge-Radix Puerariae (DG) has shown potential in ameliorating osteoporosis by regulating osteoclast differentiation, autophagy, and oxidative stress. This study provides a mechanistic basis for the therapeutic effects of DG on osteoporosis and suggests safe doses for preventing and improving bone diseases.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Xiaoli Huang, Na Guan, Qiu Li
Summary: The study introduced an ECM-mimetic scaffold that accelerated wound healing by enhancing vascularization and regulating inflammation. The PVA/BAP2 fiber demonstrated efficacy in promoting the healing efficiency of diabetic wounds and inducing optimal neo-tissue formation. This engineered biomaterial may inspire the development of new, effective, and safer marine-derived scaffolds for tissue regeneration.
Article
Chemistry, Medicinal
Lili Guo, Na Guan, Wenjun Miao, Wenwen Zhao, Qiu Li
Summary: In this study, innovative multifunctional wound dressing materials loaded with anti-inflammatory ingredients were developed and their effectiveness in treating diabetic wounds was demonstrated. The materials were able to accelerate wound healing by inhibiting inflammatory activity, making them a promising candidate for the treatment of hard-to-heal wounds caused by diabetes.
Article
Biochemistry & Molecular Biology
Xiaoli Huang, Ranran Hou, Wei Pan, Dingtao Wu, Wenwen Zhao, Qiu Li
Summary: The food-derived polysaccharide EJP showed significant protective effects against myocardial ischemia reperfusion injury by exhibiting anti-inflammatory and antioxidative activities, and also demonstrated protective effects on both the heart and kidneys.
Article
Biochemistry & Molecular Biology
Wenjun Miao, Rong Huang, Xiaoli Huang, Fei Gao, Xiangpeng Leng, Qiu Li
Summary: In this study, polysaccharides from grape pomace (GPPs) were characterized and evaluated. GPPs were found to be heteropolysaccharides rich in arabinose, galactose, and glucuronic acid, with irregular clusters on the surface. In vitro assays showed concentration-dependent antioxidant activity of GPPs. In vivo experiments demonstrated that GPPs decreased levels of inflammatory markers and oxidative stress indicators, while increasing levels of antioxidant enzymes in serum and liver tissues. The histopathological examination further confirmed the hepatoprotective effects of GPPs.
Review
Pharmacology & Pharmacy
Na Guan, Zhihai Liu, Yonghui Zhao, Qiu Li, Yitao Wang
Article
Biochemistry & Molecular Biology
Qiu Li, Fenfang Yang, Ranran Hou, Tingting Huang, Zhihui Hao
Article
Biochemistry & Molecular Biology
Wenwen Zhao, Xi . Zeng, Fancheng Meng, Xiaolin Bi, Dahai Xu, Xiuping Chen, Qiu Li, Yantao Han