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Deep learning-based drug screening for the discovery of potential therapeutic agents for Alzheimer's disease.
J Pharm Anal
October 2024
College of Pharmaceutical Engineering of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 301617, China.
Alzheimer's disease (AD) is gradually increasing in prevalence and the complexity of its pathogenesis has led to a lengthy process of developing therapeutic drugs with limited success. Faced with this challenge, we proposed using a state-of-the-art drug screening algorithm to identify potential therapeutic compounds for AD from traditional Chinese medicine formulas with strong empirical support. We developed four deep neural network (DNN) models for AD drugs screening at the disease and target levels.
View Article and Find Full Text PDFCombining in vitro, in vivo, and in silico approaches to evaluate the effect of serotonergic-based topical therapies on mild to moderate psoriasis.
Eur J Pharm Sci
January 2025
Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Professor Gama Pinto, 1649-003 Lisboa, Portugal. Electronic address:
Psoriasis, a chronic inflammatory skin disease, poses a significant burden on patients' quality of life and healthcare systems. While mild-to-moderate cases are treated topically, usually combined with phototherapy, severe cases require systemic treatment with immunosuppressants, retinoids or biologics. However, all available treatments have drawbacks in terms of efficiency and side effects.
View Article and Find Full Text PDFSynthesis and Biological Evaluation of Peripheral HTR2A Antagonists for Colorectal Cancer.
J Med Chem
January 2025
Department of Chemistry, Gwangju Institute of Science and Technology, Gwangju 61005, Republic of Korea.
Colorectal cancer is a prevalent and prominent contributor to global cancer-related fatalities with challenges in drug resistance and metastasis. Recent research highlights the potential relationship between serotonin and cancer. 5-Hydroxytryptamine receptor 2A (HTR2A) mRNA expression in colorectal cancer cells was found to be notably elevated compared to that in normal colon cells.
View Article and Find Full Text PDFFacilitating microglia M2 polarization alleviates p-Synephrine-induced depressive-like behaviours in CSDS mice via the 5-HT6R-FYN-ERK1/2 pathway.
Int Immunopharmacol
December 2024
State Key Laboratory of Traditional Chinese Medicine Syndrome, Guangdong Provincial Key Laboratory of Translational Cancer Research of Chinese Medicines, International Institute for Translational Chinese Medicine, School of Pharmaceutical Science, Guangzhou University of Chinese Medicine, Guangzhou, Guangdong, China. Electronic address:
In recent years, modulation of microglial phenotype transformation has emerged as a promising strategy for treating central nervous system disorders. Aurantii Fructus Immaturus (Zhishi), a traditional Chinese medicine with versatile applications, contains p-Synephrine (p-SYN) as its principal bioactive compound, recognized for its anti-inflammatory efficacy. However, the molecular mechanisms underlying these effects remain unclear.
View Article and Find Full Text PDF5-Hydroxytryptophan artificial synaptic vesicles across the blood-brain barrier for the rapid-acting treatment of depressive disorder.
Mater Today Bio
December 2024
School of Life Science and Technology, Xidian University and Engineering Research Center of Molecular and Neuro Imaging, Ministry of Education, Xi'an, 710126, PR China.
Conventional antidepressants are slow to work and have serious side effects and poor response rates. As a precursor to 5-hydroxytryptamine (5-HT), 5-hydroxytryptophan (5-HTP) can be safely increased in concentration and rapidly metabolized into 5-HT in the brain, but the effectiveness of 5-HTP is severely limited due to its short half-life and lack of targeting. To traverse the blood-brain barrier (BBB) and achieve effective targeting, we designed a near-infrared (NIR) light-responsive artificial synaptic vesicles functionalized with an aptamer and loaded with 5-HTP and IR780.
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