1. Aminopeptidase-N/CD13 (EC 3.4.11.2) inhibitors: Chemistry, biological evaluations, and therapeutic prospects
- Author
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Brigitte Bauvois, Daniel Dauzonne, Signalisation cellulaire, dynamique circulatoire et athérosclérose précoce (SCDCAP), and Université Pierre et Marie Curie - Paris 6 (UPMC)-Centre National de la Recherche Scientifique (CNRS)
- Subjects
MESH: Hydroxamic Acids ,natural inhibitor ,Angiogenesis ,medicine.medical_treatment ,Pharmacology ,Hydroxamic Acids ,01 natural sciences ,MESH: Tyrosine ,0302 clinical medicine ,MESH: Curcumin ,Drug Discovery ,MESH: Animals ,Disulfides ,Receptor ,Neprilysin ,0303 health sciences ,aminopeptidase ,MESH: Protease Inhibitors ,MESH: Neprilysin ,Chemistry ,MESH: Antigens, CD13 ,General Medicine ,Transmembrane protein ,3. Good health ,030220 oncology & carcinogenesis ,MESH: Oligopeptides ,Molecular Medicine ,medicine.symptom ,Pentacyclic Triterpenes ,Oligopeptides ,MESH: Neovascularization, Physiologic ,hormones, hormone substitutes, and hormone antagonists ,Cell type ,bestatin ,Curcumin ,animal structures ,Neovascularization, Physiologic ,Inflammation ,ectoenzyme ,[SDV.BC]Life Sciences [q-bio]/Cellular Biology ,CD13 Antigens ,Article ,03 medical and health sciences ,Immune system ,Leucine ,MESH: Cell Proliferation ,synthetic inhibitor ,medicine ,cancer ,Animals ,Humans ,Protease Inhibitors ,MESH: Disulfides ,Secretion ,Betulinic Acid ,Cell Proliferation ,030304 developmental biology ,MESH: Humans ,Protease ,010405 organic chemistry ,Cell growth ,MESH: Triterpenes ,Triterpenes ,0104 chemical sciences ,MESH: Leucine ,inflammation ,Tyrosine - Abstract
Aminopeptidase N (APN)/CD13 (EC 3.4.11.2) is a transmembrane protease present in a wide variety of human tissues and cell types (endothelial, epithelial, fibroblast, leukocyte). APN/CD13 expression is dysregulated in inflammatory diseases and in cancers (solid and hematologic tumors). APN/CD13 serves as a receptor for coronaviruses. Natural and synthetic inhibitors of APN activity have been characterized. These inhibitors have revealed that APN is able to modulate bioactive peptide responses (pain management, vasopressin release) and to influence immune functions and major biological events (cell proliferation, secretion, invasion, angiogenesis). Therefore, inhibition of APN/CD13 may lead to the development of anti‐cancer and anti‐inflammatory drugs. This review provides an update on the biological and pharmacological profiles of known natural and synthetic APN inhibitors. Current status on their potential use as therapeutic agents is discussed with regard to toxicity and specificity. © 2005 Wiley Periodicals, Inc. Med Res Rev
- Published
- 2005
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