RESUMEN
Natural products are important sources for the discovery of anti-tumor drugs. Evodiamine is the main alkaloid component of the traditional Chinese herb Wu-Chu-Yu, and it has weak antitumor activity. In recent years, a number of highly active antitumor candidates have been discovered with a significant progress. This article reviews the research progress of evodiamine-based antitumor drug design strategies, in order to provide reference for the development of new drugs with natural products as leads.
RESUMEN
Cancer seriously threatens human life and health, it is urgent for the development of rapid detection, precise localization and effective treatment of tumors. Chemical fluorescent probes that are sensitive to tumor-specific microenvironments have important significance in tumor theranostics and a variety of such probes have been developed. In this review, we classified chemical fluorescent probes that are sensitive to tumor microenvironments according to biological characteristics and microenvironmental changes while combining spectroscopy or response mechanisms, and systematically introduced the research progress of chemical fluorescent probes with sensitivity to hypoxia, low polarity, high viscosity, abnormal pH values and abundant reactive oxygen species in tumor microenvironments, in order to provide references for the development and applications of these probes.
RESUMEN
The composition of intestinal microflora is closely related to the occurrence and development of colorectal cancer (CRC). Among them, Fusobacterium nucleatum (Fn) has been proved directly related to the recurrence, metastasis and chemotherapy resistance of CRC. Therefore, it is of great significance for the prevention and treatment of colorectal cancer by the exploration potential anti-Fn drug targets and discovery small molecule drugs. However, no selective anti-Fn small molecule inhibitors have been reported so far as well as their anti-Fn thereby "anti-Fn further anticancer" mechanisms are unclear. Herein, this article reviews the potential therapeutic targets and small molecule ligands of Fn in order to provide a reference for the development of anti-Fn and anti-CRC small molecule drugs.
RESUMEN
Protein-protein interaction (PPI) plays an important role in the regulation of life. Most of the PPI interfaces are large and discontinuous, and it is difficult for small molecules to specifically bind to them. Peptides are critical in PPI surface interactions due to their higher affinity and specificity. However, peptides have some defects such as easy hydrolysis by protease and poor membrane permeability. Due to good biocompatibility and chemical diversity, cyclic peptides play an important role in drug discovery. Therefore, the development of efficient cyclic peptide construction methods has become a frontier issue in peptide drug research. In recent years, a series of new progresses have been made in the synthesis strategy and the application of cyclic peptides, providing powerful technical tools for the research and development of cyclic peptide drugs. In this review, the synthesis strategies of cyclic peptides and their application will be reviewed from four aspects: synthesis strategies, property improvement, biological activity and prospect.