APN/CD13 inhibitor Ubenimex: A molecular chaperone of antineoplastic chemotherapeutic drugs / 中国药理学通报

Cytotoxic anti-neoplastic drugs are a kind of chemotherapeutic drugs that directly kill or inhibit the growth and proliferation of tumor cells, and it is one of the main drugs for the treatment of malignant tumors. These drugs may have toxic side effects on normal cells of human body (especially those with strong division and proliferation) when they are used to kill tumor cells. And patients may usually have adverse reactions even at a normal dose when using this kind of drugs. Due to the strong toxic side effects of cytotoxic chemotherapeutic drugs, their clinical application is limited. In recent years it has been found that aminopeptidase N inhibitor Ubenimex has a significant synergistic effect with anti-neoplastic chemotherapeutic drugs, which has the advantages of enhancing the therapeutic effect of drugs and reducing the toxic side effects of chemotherapeutic drugs. This review enumerates that the combination of Ubenimex and a variety of cytotoxic drugs can enhance the anti-tumor effect of cytotoxic drugs and reduce the occurrence of adverse reactions. In addition, the mechanism of combined use of Ubenimex in reversing drug resistance is also introduced. At the same time, is is further confirmed the clinical value of Ubenimex as an effective adjuvant in the treatment of malignant tumors, so as to provide a basis for clinical application.

Advances in research on HBV inhibitors based on new targets (2): RNase H and others / 药学学报

Hepatitis B has become one of the major diseases which seriously affect people's health and social development. Hepatitis B, with high incidence and long disease course, cannot be cured by approved drugs such as the nucleoside analogues. Therefore, the discovery of safe and efficient novel HBV inhibitors is of great significance. From the point of view of medicinal chemistry, we summarized and discussed current endeavours towards the discovery and development of anti-HBV agents of RNase H and other novel target inhibitors with various scaffolds or distinct mechanisms of action, besides the existing capsid protein inhibitors.

Advances in research on HBV inhibitors based on new targets (1): capsid protein inhibitors / 药学学报

Hepatitis B virus (HBV) capsid protein plays an important role in the life cycle, thus becoming an ideal target for drug design. Capsid protein inhibitors can exert a synergistic antiviral effect with nucleoside drugs by inhibiting the replication of HBV. This paper reviews the research progress of capsid protein inhibitors with different structural types from the perspective of medicinal chemistry.

Recent progress of inhibitors targeting HIV-1 NCp7 / 药学学报

The acquired immunodeficiency syndrome (AIDS) is a serious infectious disease infected by human immunodeficiency virus type 1 (HIV-1). HIV-1 nucleocapsid protein 7 (HIV-1 NCp7) plays an important role in the progress of virus reverse transcription and integration. Thus, the central role and conservative nature of the NCp7 protein make it an attractive target for development of novel anti-HIV agents. This review summarizes the research progress of HIV-1 NCp7 inhibitors in the past decade.