期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 61, 期 15, 页码 6468-6490出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b00782
关键词
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资金
- University Grants Commission (UGC), New Delhi, India
- University with Potential for Excellence (UPE) Phase II Program of UGC, New Delhi
Aminopeptidase N (APN) is an important metalloenzyme. It regulates multivariate cellular functions by different mechanisms such as enzymatic cleavage of peptides. This may play a role in endocytosis and regulate signal transduction. APN, a member of the MI zinc metallopeptidase family, plays crucial roles in a variety of functions such as migration and invasion, and angiogenesis and metastasis of tumor cells. Therefore, APN inhibitors may be useful for the treatment of cancer. In this Perspective, structure activity relationships of APN inhibitors are discussed to get an idea of possible lead candidates. APN inhibitors should possess an aryl hydrophobic function along with a zinc binding group attached to the hydrophobic group(s) to achieve high potency. This and other design aspects of APN inhibitors are discussed in this Perspective.
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