Latest ArticlesProstate cancer is the most common malignant tumor of male reproductive system, which seriously threatens men's health. It has been shown that the existence of zinc ions can inhibit the growth of prostate cancer cells. In addition, photothermal treatment of cancer is attracting more and more attention due to its high accuracy and efficiency. In this study, zinc ions loaded black phosphorus nanosheets (BP-Zn) were prepared, and the photothermal therapy efficiency of the system on human prostate cancer cells (PC-3) was evaluated. The inhibition effect of zinc ions on PC-3 cells was studied. It was demonstrated that the toxicity of zinc ions on PC-3 cells was concentration- and time-dependent. Moreover, it can be seen from in vitro photothermal therapy that the treatment effect of black phosphorus assisted by zinc ions is superior to that of black phosphorus alone. This study further studied the in vivo therapeutic effect of BP-Zn. The results once again confirmed that the combinational photothermal treatment of zinc ions and BP had excellent anti-tumor effect. The animal procedures were approved by the Animal Ethics Committee of Tsinghua Shenzhen International Graduate School.
The complexity of tumor microenvironment brings both challenges and opportunities for targeted drug delivery. On the one hand, using the special characteristic as stimuli, we can construct a variety of responsive drug delivery systems for tumor targeting. On the other hand, the abnormal vasculature and dense extracellular matrix in solid tumor become formidable barriers to the nanoparticles delivery, which greatly reduces the drug delivery efficiency. Lots of researches focus on regulating the tumor microenvironment to make it more conducive to drug delivery. In this review, we will highlight the recent advances both in tumor microenvironment responsive nano-drug delivery systems design and tumor microenvironment regulation to improve tumor targeted delivery efficiency, and discuss the existing problems and future development.
Two-pore domain potassium channels (K2P) make up a subfamily of potassium channels discovered in the 1990s, and TREK-1 is the most widely studied subtype of K2P. TREK-1 is widely expressed in the body and especially in the central nervous system, where its main role is to control cell excitability and maintain the membrane potential below the depolarization threshold. It thereby participates in regulating various physiological and pathological processes. TREK-1 is also a potential drug target in many diseases. It is known that many marketed drugs can affect the function of TREK-1, but currently there are no specific TREK-1 modulators or drugs. We review the structure, distribution and regulation of TREK-1 and focus on recent progress in understanding the pharmacology of TREK-1 and its role in neuroprotection, depression, anesthesia and epilepsy. The research status of TREK-1 modulators is discussed.
Puerarin, also known as daidzein 8-C-glucoside, is a major isoflavone glycoside from Pueraria lobata. Puerarin has been shown to possess a variety of pharmacological activities. It has been widely used for the treatment of cardiovascular and cerebrovascular diseases. However, the further applications are limited due to its low water solubility and poor bioavailability. Structural modification is thus regarded as an efficient approach to improve the solubility and bioavailability of puerarin. Unlike chemical modifications, enzyme-assisted modifications, namely biocatalysis, is a promising alternative for the regioselective synthesis of puerarin derivatives due to its high selectivity. Up to date, acylation, glycosylation and hydroxylation of puerarin had been achieved through enzyme-based biocatalysis. Diverse active puerarin derivatives with improved solubility and bioavailability have been thus developed. Based on modification groups, this paper focused on the progress in the preparation of puerarin derivatives by biocatalysis, in which the whole-cells or pure enzymes were used as the biocatalysts. This article was expected to provide new ideas for the synthesis and development of puerarin drugs.
To identify potential serum proteins that might serve as biomarkers for Alzheimer's disease (AD), we performed comparative proteomic profiling of sera from AD and healthy control subjects using label-free LC-MS/MS. Our study identified 387 proteins, 61 of which showed significant changes in the serum of AD patients compared to healthy controls. Gene ontology (GO) enrichment analysis showed that some GO terms related to the pathogenesis of AD were significantly enriched in differentially expressed proteins, including cholesterol and lipid metabolism, inflammation, coagulation and hemostasis processes, and immune responses. Therefore, based on the above results and the consistency of protein content changes in the 8 comparison groups, 18 proteins were selected as candidate biomarkers. Protein-protein interaction results suggest that these 18 proteins can directly or indirectly interact with APP. Therefore, changes in the levels or functions of these proteins may affect Aβ metabolism and participate in the occurrence of AD, and have the potential to become AD blood biomarkers.
Medicinally active molecules are those that have pharmacological effects. Research on protein targets of these molecules not only clarifies their mechanism of action, but also deepens our understanding of biological systems. Here we review recent advances in protein targets of drugs used in clinical practice or in preclinical research. They have various functions including anti-inflammatory, anti-malarial, anti-tumor and other biological activities. Activity-based protein profiling (ABPP) and cellular thermal shift assay (CETSA) are two useful methods to identify the protein targets of small molecules. ABPP depends on a derivative active molecule probe to pull down the protein targets to reveal the interaction mechanisms between the active molecules and targets. Drug target engagement also can be assessed by means of CETSA based on ligand-induced changes in protein thermal stability. In the CETSA approach, the active molecules do not need to be chemically modified. Combining the CETSA method with quantitative mass spectrometry is an effective approach to study the effect of compounds on the thermal profile of a cellular proteome and identify the protein targets.ABPP and CETSAcan be complementary and effectively clarify the protein targets. The study of protein targets will help reveal the mechanism of action of medicinal molecules, reveal toxic mechanisms and aid in the discovery of new medicinal targets to promote the process of drug development.
Metal-organic frameworks (MOFs) are porous crystalline polymers constructed from the coordination reaction between organic ligands and metal ions. Due to their advantages:adjustable periodic pore structure, large specific surface area and easy functional modification, etc., MOFs have been widely used in the fields of gas storage/separation, catalysis, sensing, biological imaging and drug delivery. In recent years, MOFs have shown great potential in disease diagnosis and treatment. This review summarizes the application of MOFs in the fields of bio-sensing, cell imaging, in vivo imaging, drug delivery, etc., discusses the problems and corresponding solutions in the application of MOFs for biomedicine. We hope this review can provide reference for the designing new methods for disease diagnosis and treatment.
Traditional Chinese medicine (TCM) has made numerous contributions to the prosperity of China. However, the phytochemicals of TCM are complex, and there are significant differences in relative content. The material basis of TCM has restricted the modernization of TCM. Liquid chromatography-mass spectrometry (LCMS) combines the high separation performance of chromatography and the high sensitivity of mass spectrometry. It has been widely used in the analysis of natural medicines and can greatly promote the development of TCM. Many studies have focused on the comprehensive characterization of phytochemicals, building a strategy for the rapid, accurate and systematic analysis of the chemical components of TCM through the integration of different mass spectrometric techniques, and laying the foundation for quality control and rational utilization of TCM.
Reactive oxygen species (ROS) which were partial metabolites of oxygen are highly reactive. Different concentrations of ROS have different effects on tumor development. Tumor cells have a high level of reactive oxygen species. The antioxidant system of tumor is in highly activated state, and thus modulation of reactive oxygen species levels could be an effective strategy to target cancer cells. Treatment with small molecules that disrupt the redox balance can kill tumor cells first. This paper outlines the main ideas of developing anti-tumor drugs based on reactive oxygen species regulation, and summarizes the representative drugs and research progress according to the mechanism of action, in an effort to suggest potential reference and ideas for developing antitumor drugs based on reactive oxygen species regulation.
Uveal melanoma (UM) is one of most common ocular cancers and is extremely malignant; so far there is no effective treatment. Moreover, the survival period is only 2-7 months after metastasis. It has been proven that more than 83% of uveal melanomas harbor mutations in G protein subunit α q (GNAQ) or G protein subunit α 11 (GNA11), among which 95% are a Q209P/L single-site mutation. Q209P/L mutations lead to dysfunction of guanine triphosphatase (GTPase) in the G protein and result in constitutive activation of downstream pathways including mitogen-activated protein kinase (MAPK), phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT), Ras homologue (Rho)/Rho-associated kinase (Rock)/Yes-associated protein (YAP) and others. Therefore, targeting GNAQ/GNA11 mutations are potential strategies for UM treatment. This review will focus on roles of G protein mutations in UM progression, and the potential therapeutic effects of GNAQ/GNA11 inhibitors, and will provide insights into basic and clinical research on UM treatment.
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