Avtor/Urednik		Lukančič, I; Šolmajer, T
Naslov		DNA giraze - tarče antibakterijskih zdravilnih učinkovin
Prevedeni naslov		DNA gyrases - targets of antibacterial drugs
Tip		članek
Vir		Farm Vestn
Vol. in št.		Letnik 49, št. 4
Leto izdaje		1998
Obseg		str. 493-508
Jezik		slo
Abstrakt		Gyrase is an extremly important bacterial enzyme, since the proper activity of this enzyme enables the initiation of replication in DNA and the expression of bacterial genes. Inhibition of gyrase leads to bacterial death, therefore gyrase can act as a target for antibacterial drugs. Gyrase is a member of the topoisomerase family of enzymes. The active gyrase molecule acts as a heterotetramer from two A and B subunits. Both subunits can act as a target for antibacterial drugs. Numerous gyrase inhibitors are known (quinolones, cumarins, cyclothialidines). For the majority of them (quinolones), the inhibition mechanism is still subjected to discussion. In this article a review of gyrase inhibitors is made and recent developments in the elucidation of the mechanism of their action are presented.
Izvleček		Giraza je zelo pomemben bakterijski encim, ker pravilno delovanje tega encima omogoča inicijacijo podvojevanja DNA in ekspresijo genov. Inhibicija giraze vodi v bakterijsko smrt, zato giraza lahko nastopa kot tarča antibakterijskih učinkovin. Giraze sodijo v širšo družino encimov, ki jih imenujemo topoizomeraze. Aktivna molekula giraze je heterotetramer, sestavljen iz dveh A in B podenot. Kot tarči antibakterijskih učinkovin lahko nastopata obe podenoti. Poznani so številni girazni inhibitorji (kinoloni, kumarini, ciklotialidini), vendar je za večino od teh (kinoloni) mehanizem inhibicije še vedno predmet diskusije. V članku smo naredili pregled giraznih inhibitorjev ter predstavili najnovejše izsledke na področju mehanizma delovanja giraze in delovanja giraznih inhibitorjev.
Deskriptorji		DNA TOPOISOMERASE (ATP-HYDROLYSING) ANTIBIOTICS QUINOLINES COUMARINS BACTERIAL INFECTIONS