The potential anti-tumorigenic and anti-metastatic side of the proprotein convertases inhibitors.
The setup of tumorigenesis processes is generally associated with various events leading to abnormal expression of oncogenes and/or tumor suppressor genes. Recently, the expression and/or activity of a range of molecules involved in these processes were reported to require proteolytic processing of their precursor proteins by the serine pro-protein convertases (PCs) in order to mediate their biological functions. These include adhesion molecules, proteases, growth factors, cytokines and their receptors. Since their discovery, the identification of new PCs substrates and specific PCs inhibitors became an attractive strategy in cancer therapy. In this review, we will report the implication of these enzymes and the processing of their substrates in tumor progression and metastasis. Newly reported studies on the potential use of the PCs as new therapeutic targets will be also discussed.
Lahlil
Rachid
R
INSERM, U 716, Equipe Avenir. Institut de Génétique Moléculaire, Paris, 75010, France.
Calvo
Fabien
F
Khatib
Abdel-Majid
AM
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D006801:Humans; D009362:Neoplasm Metastasis / Q000517:prevention & control*; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology*; D010982:Platelet-Derived Growth Factor / Q000378:metabolism; D043484:Proprotein Convertases / Q000032:analysis / Q000037:antagonists & inhibitors / Q000502:physiology; D011480:Protease Inhibitors / Q000494:pharmacology*; D020574:Proto-Oncogene Proteins c-sis / Q000378:metabolism; D016212:Transforming Growth Factor beta / Q000378:metabolism; D042461:Vascular Endothelial Growth Factor A / Q000378:metabolism
D000970:Antineoplastic Agents; D010982:Platelet-Derived Growth Factor; D011480:Protease Inhibitors; D020574:Proto-Oncogene Proteins c-sis; D016212:Transforming Growth Factor beta; D042461:Vascular Endothelial Growth Factor A; C075278:platelet-derived growth factor A; D043484:Proprotein Convertases