Author/Editor		Oblak, Marko; Šolmajer, Tomaž
Title		Matrične metaloproteinaze - nove tarče antitumornih učinkovin
Translated title		Matrix metalloproteinases - novel targets of antitumor drugs
Type		članek
Source		Farm Vestn
Vol. and No.		Letnik 53, št. 1
Publication year		2002
Volume		str. 29-40
Language		slo
Abstract		Matrix metalloproteinases (MMP) comprise a family of endoproteinases responsible for remodelling and degradation of extracellular matrix. Under normal physiological conditions the action of these enzymes is precisely regulated by the endogenous tissue inhibitors of metalloproteinases (TIMP). Abnormal expression and activity of MMPs have been linked to several inflammatory diseases, tumor growth and metastasis. Therefore the inhibition of MMPs offers the alternative therapeutic option in treatment of these diseases. The focus of this review are the activation pathways and structural properties of MMPs that enabled the rational drug design of the MMP inhibitors. Also, examples of MMP inhibitors in clinical trials are presented.
Summary		Matrične metaloproteinaze (MMP) so družina endoproteinaz, ki sodelujejo pri preoblikovanju in razgradnji ekstracelularnega matriksa. V normalnem fiziološkem stanju delovanje teh encimov strogo nadzorujejo endogeni tkivni inhibitorji metaloproteinaz (TIMP). Nenadzorovano ekspresijo in aktivnost posameznih MMP so opazili pri številnih vnetnih in rakavih obolenjih, zato inhibicija MMP predstavlja novo terapevtsko možnost v boju s temi boleznimi. Članek opisuje aktivacijske mehanizme in strukturne značilnosti MMP, ki so omogočili racionalno načrtovanje njihovih inhibitorjev. Predstavljeni so tudi primeri inhibitorjev MMP, ki so že v kliničnih testiranjih.
Descriptors		ANTINEOPLASTIC AGENTS METALLOPROTEINASES DRUG DESIGN CATALYSIS PROTEASE INHIBITORS