Novel Anticancer Targets and Drug Discovery in Post Genomic Age

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 16, 12 Issues, 2016

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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Michelle Prudhomme
Universite Blaise Pascal - C.N.R.S
Aubiere Cedex

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Novel Anticancer Targets and Drug Discovery in Post Genomic Age

Anti-Cancer Agents in Medicinal Chemistry, 5(1): 53-63.

Author(s): Qianbin Li and Wenfang Xu.

Affiliation: Department of Medicinal Chemistry, School of Pharmaceutical Sciences, ShanDong University, 44,West Culture Road, 250012, Ji'nan, ShanDong, P.R.China.


Cancer is a serious disease with a complex pathogenesis, which threats human life greatly. Currently, great efforts have been put to the identification of novel anticancer targets and the discovery of anticancer drugs following the progress of chemogenomics, which will be reviewed briefly in this article. Furthermore, during the past 5 years, the global effort of sequencing human genome has provided us with an enormous number of potential targets associated with cancer therapy. As a result, the New Drug Discovery (NDD) is undergoing a transition “from gene to drug”. Accordingly, the targets for anticancer drugs studies now are focused on some biological macromolecular targets associated with cancer and several interactive mechanisms involved in the growth and metastasis of cancer cells as well as tumor angiogenesis, such as Matrix Metalloproteinases (MMPs), Aminopeptidase N (APN), Tyrosine Kinase (TK), Farnesyltransferase (FTase) and cell Signal Transduction Pathway and so forth. Among these targets the MMP-2, -9 and APN are the most extensively studied enzymes in our laboratory. The peptidomimetics Matrix Metalloproteinase Inhibitors (MMPIs) and APN inhibitors (APNIs) with the molecular scaffold of pyrrolidine, 3-amino-2-hydroxy-4-phenyl butyric acid (AHPA) and glutamylide, which have been designed and synthesized in our laboratory, will be described in the review, among which the pyrrolidine scaffold is patented with the IC50 ranging from 1nM to 300nM against MMP-2, and MMP-9.


novel anticancer targets, matrix metalloproteinases, aminopeptidase n, tyrosine kinase, farnesyltransferase, inhibitor /manipulators.

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Article Details

Volume: 5
Issue Number: 1
First Page: 53
Last Page: 63
Page Count: 11
DOI: 10.2174/1568011053352631

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