4.5 Review

Aminopeptidase N (EC 3.4.11.2) inhibitors (2006-2010): a patent review

Journal

EXPERT OPINION ON THERAPEUTIC PATENTS
Volume 21, Issue 8, Pages 1241-1265

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.1517/13543776.2011.587002

Keywords

aminopeptidase N; analgesia; angiogenesis; bestatin; degradation; dual inhibition; enkephalin; enzyme activity; inhibitor; invasion; neutral endopeptidase; selectivity; tumor; ZBG

Funding

  1. National Natural Science Foundation Research of China [9071304]
  2. National Science and Technology Major Project [2009-2X09103-118]

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Introduction: Aminopeptidase N (APN/CD13) acts as an exopeptidase and has been studied for decades. In recent years, it has been seen not only as a tumor-related target but also as a potential functional protein in various other physiological or pathological processes, such as analgesia, virus infection and inflammation. Areas covered: In this review, APN inhibitors in the patents publicized during 2006 - 2010 are introduced. Readers will gain information on the patent inhibitors, including chemical structures, original sources or synthetic methods, biological assays and application potential. Expert opinion: It is difficult to identify compounds that interact with the function not relevant with peptide-hydrolysis of APN in the enzyme activity assay, and such compounds have not been reported in the patents during the past 5 years. The progress of protein-small molecule interaction detecting means, such as surface plasmon resonance, will possibly help develop such compounds for the treatment of relevant diseases or new molecular probes in mechanism investigation.

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