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1.
Acta Pharmaceutica Sinica ; (12): 407-419, 2019.
Article in Chinese | WPRIM | ID: wpr-780134

ABSTRACT

Reprogramming of metabolism is one of the most critical features in tumorigenesis and tumor growth. Many types of cancer show an increased demand for specific amino acids, rely on exogenous supplies, or alter amino acid metabolic pathways, leading to changes in corresponding amino acid levels to meet the need of tumorigenesis. Therefore, if the level of tumor growth-dependent amino acids can be effectively controlled, a new treatment strategy can be developed from the perspective of cell metabolism. At present, remarkable progress has been made in this field. This paper outlines the amino acid metabolic pathways closely related to tumorigenesis and tumor growth, and summarizes the corresponding regulatory mechanisms and active molecules. Finally, the direction of the field is discussed and prospected for future development.

2.
Acta Pharmaceutica Sinica ; (12): 2012-2025, 2018.
Article in Chinese | WPRIM | ID: wpr-780084

ABSTRACT

Currently, single-target drugs are often difficult to achieve the desired results in the treatment of multifactorial diseases such as tumors, cardiovascular and endocrine diseases, and may also cause toxicity. Multi-target drugs can improve the efficacy, reduce side effect and drug resistance by regulating multiple links of the disease, showing good prospects for the application. The main aim of this article is to review the strategies of designing multi-target directed ligands (MTDLs) (including conjugated-pharmacophore, fused-pharmacophore and merged-pharmacophore) and the research progress in recent years. The existing problems and challenges of multi-target drugs are also discussed, to provide new ideas for the study of multi-target drugs.

3.
Acta Pharmaceutica Sinica ; (12): 293-302, 2014.
Article in Chinese | WPRIM | ID: wpr-245086

ABSTRACT

Designing of natural product-like compounds using natural products as template structures is an important strategy for the discovery of new drugs. Gambogic acid (GA), which is a Garcinia natural product with a unique caged xanthone scaffold, inhibits potent antitumor activity both in vitro and in vivo. This review summarized the researches on the identification of the antitumor pharmacophore of GA, and the design, structural optimization and structure-activity relationship (SAR) of natural product-like caged xanthones based on it.


Subject(s)
Humans , Antineoplastic Agents , Chemistry , Pharmacology , Biological Products , Chemistry , Pharmacology , Cell Line, Tumor , Cell Proliferation , Drug Screening Assays, Antitumor , Garcinia , Chemistry , Molecular Structure , Structure-Activity Relationship , Xanthones , Chemistry , Pharmacology
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