Latest ArticlesHypoxia is one of the most significant characteristics of solid tumors. Hypoxia microenvironment can lead to the overexpression of hypoxia inducible factor-1α (HIF-1α). As the most critical transcription factor in the hypoxia response, HIF-1α activates downstream gene expression resulting in abnormal tumor cell proliferation, tumor angiogenesis, unusual energy metabolism, increased drug resistance, invasion, and metastasis. Down-regulation of HIF-1α expression is considered as a promising approach for the treatment of solid tumors, whereas the clinical efficacy of most existing HIF-1α inhibitors is restricted in low efficacy and high toxicity. Therefore, it is particularly important to develop powerful and safe novel drugs against the overexpression of HIF-1α. In recent years, numbers of studies have proved that a variety of chemical components of traditional Chinese medicine can directly or indirectly inhibit the activation of HIF-1α, which has a broad prospect in the fight against hypoxia-induced tumor progression. In this review, we summarized various anti-tumor active components of traditional Chinese medicines responsible for inhibiting the expression of HIF-1α in last ten years and analyzed the corresponding mechanism, with a view to further research as a reference.
Transient receptor potential vanilloid ion channel subtypes 2 (TRPV2) is a calcium permeable nonselective cation channel. TRPV2 is expressed in nerves, blood vessels, spleen, and other organs, and participates in the regulation of a variety of important physiological functions, such as nociception, neural development, and immune response. Here we reviewed the research progress on the structure, modulators, and physiological functions of TRPV2 channel to provide references for future research.
Growth differentiation factor 15 (GDF15) is an endocrine hormone that belongs to the transforming growth factor β (TGFβ) superfamily, which plays a role by binding to the glial cell line derived neurotrophic factor (GDNF)-family receptor α-like (GFRAL)-rearranged during transfection (RET) heterodimer receptor. A number of studies have confirmed that GDF15, as a biomarker for obesity, diabetes, tumors, non-alcoholic fatty liver disease, ischemic diseases, and so on, has become a new target for new drug discovery. At present, pharmaceutical companies around the world are carrying out drug discovery with GDF15 as a new therapeutic target involving many therapeutic areas such as anti-obesity, anti-tumor, and treatment of anorexia syndrome. Comprehensive analysis of the advantages and disadvantages of the GDF15 target, discussion, and objective evaluation of research and development of new drugs based on GDF15 will provide a scientific basis for the discovery of innovative drugs that could relieve the human suffering from illness.
Protein disulfide isomerase (PDI), also named PDIA1, is an archetype member of protein disulfide isomerase family, which mainly exists in endoplasmic reticulum and plays an important role in pathophysiological progress via enzyme activity and molecular chaperone function helping protein folding correctly. Amyotrophic lateral sclerosis (ALS) is a kind of neurodegenerative diseases characterized by abnormal protein aggregation. Recently, PDI mutants have been found in ALS patients and the important role of PDI protein in the development of ALS has also been confirmed. Here, we focus on the recent studies of PDI in ALS hoping to provide a novel target for the treatment of ALS.
The structural modification of natural product represents a powerful tool for anti-cancer drug discovery. Noscapine, as a phthalideisoquinoline alkaloid from opium, has been used as an over-the-counter antitussive drug with excellent oral bioavailability and low toxicity. Recently, the potential of this compound as a particularly attractive lead for anti-cancer drug discovery has been demonstrated. Multiple mechanisms, especially the interference of tubulin polymerization, might be involved. Thereafter, various structural modifications based on semisynthetic routes, which aims to improve the anti-cancer activity and pharmacokinetic properties, as well as to probe the mechanism, has been performed. Several analogues are emerging as possible candidates as novel anticancer therapies. This perspective mainly discusses the advancing noscapine and related analogues in the fight against malignant disease in recent years. Furthermore, the future directions of this evolving field were also preliminary prospected.
In recent years, the research on myocardial ischemia disease is increasingly in-depth, and there are more and more drugs related to the anti-myocardial ischemia, among which natural medicines play an important role. In order to deal with myocardial ischemia diseases caused by a variety of pathogenic causes, the research on natural medicines is more and more deep. At present, natural medicines containing saponins, flavonoids, alkaloids and other compounds are the research objects. At the same time, great progress has been made in the research on the clinical application of natural drugs against myocardial ischemia. This article reviews the research progress of natural medicines against myocardial ischemia at home and abroad in the past ten years.
Cancer is a malignant disease threatening human health and life. Early diagnosis of carcinoma plays an important role in the treatment of carcinoma, so tumor imaging agents have been the focus of research in this field. Mannose receptor is a C-type lectin receptor, which expressed in various tumor tissues, sentinel lymph nodes and has become an important tumor marker. In recent years, a variety of imaging agents targeting mannose receptors have been designed and developed. This review summarizes the representative achievements.
As one of the most critical post-translational modifications, glycosylation of therapeutic proteins has a profound impact on their safety, efficacy and consistent. However, glycosylation is not a template-driven process, therefore variability in the glycosylation pattern of a protein can arise. This makes challenges of glycan analysis and control. Here, we review the overall control strategy, basic requirements for standardized protocols and the novel technologies of glycosylation analysis to accelerate the development of therapeutic glycoproteins.
The activity and expression of drug metabolizing enzymes and transporters changes significantly under high altitude hypoxia. The gut microbiota is an important factor affecting the metabolism of drugs through direct and indirect actions, changing the bioavailability, biological activity or toxicity of drugs and affecting the efficacy and safety of drugs. High altitude hypoxia significantly changes the structure and diversity of the gut microbiota, which may play a role in drug metabolism. This article reviews the effects of high-altitude hypoxia on the gut microbiota and the effects these changes on drug metabolism.
We provide a new preclinical pharmacodynamic evaluation method of cerebral thrombolytics using beagle dogs with acute thrombotic cerebrovascular occlusion. An intracranial large vessel occlusion animal model was generated by pushing an autologous thrombus to the left carotid artery under X-ray angiography. The experiments were approved by the Animal Care and Welfare Committee Institute of Materia Medica, China Academy of Medical Sciences (CAMS), Peking Union Medical College. According to the degrees of cerebral blood flow reperfusion, the new method has 0, Ⅰ, Ⅱ (Ⅱa and Ⅱb), Ⅲ levels. Respectively, 0 level represents no blood flow through the area of vascular occlusion; Ⅰ level has low perfusion; Ⅱa level is less than half the infusion; Ⅱb level is more than half perfusion; Ⅲ level is completely recanalization perfusion. Alteplase was used as a positive drug to verify the accuracy of the method. Our results suggest that 100% of dogs reached the level of grade I and below in the model group, while 83% reached the level of grade IIa and above in the alteplase group. Results of a rank sum test showed that alteplase significantly improved the reperfusion of occluded cerebral vessels. We propose a method to evaluate the efficacy of thrombolytic drugs on dogs with middle cerebral artery occlusion.
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