Napredna pretraga

Pregled bibliografske jedinice broj: 701903

Dipotassium-trioxohydroxytetrafluorotriborate, K2[B3O3F4OH], is a potent inhibitor of human carbonic anhydrases


Vullo, Daniela; Miloš, Mladen; Galić, Borivoj; Scozzafava, Andrea; Supuran, Claudiu T.
Dipotassium-trioxohydroxytetrafluorotriborate, K2[B3O3F4OH], is a potent inhibitor of human carbonic anhydrases // Journal of enzyme inhibition and medicinal chemistry, 30 (2015), 2; 341-344 doi:10.3109/14756366.2014.918610 (međunarodna recenzija, članak, znanstveni)


Naslov
Dipotassium-trioxohydroxytetrafluorotriborate, K2[B3O3F4OH], is a potent inhibitor of human carbonic anhydrases
(Dipotassium- trioxohydroxytetrafluorotriborate, K2[B3O3F4OH], is a potent inhibitor of human carbonic anhydrases)

Autori
Vullo, Daniela ; Miloš, Mladen ; Galić, Borivoj ; Scozzafava, Andrea ; Supuran, Claudiu T.

Izvornik
Journal of enzyme inhibition and medicinal chemistry (1475-6366) 30 (2015), 2; 341-344

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, znanstveni

Ključne riječi
Anion ; carbonic anhydrase ; dipotassium-trioxohydroxytetrafluorotriborate ; inhibitor

Sažetak
The boron heterocyclic compound dipotassium- trioxohydroxytetrafluorotriborate (K2[B3O3F4OH]) was investigated as inhibitor of the zinc enzyme, carbonic anhydrase (CA, EC 4.2.1.1). Eleven human (h) CA isoforms, hCA I–IV, VA, VI, VII, IX and XII–XIV, were included in the investigations. The anion, similar to tetraborate or phenylboronic acid, inhibited most of them. hCA III was not inhibited by K2[B3O3F4OH], whereas hCA VA, hCA VI, hCA IX and hCA XIII were inhibited in the submillimolar range, with KIs of 0.31–0.63 mM. hCA I and II (cytosolic, widespread isoforms), hCA IV (membrane-bound isoform), hCA XII (tumor- associated, transmembrane) and hCA XIV (transmembrane) were much more effectively inhibited by this anion, with inhibition constants ranging from 25 to 93 µM. hCA VII, a cytosolic enzyme present in the brain and associated to oxidative stress, was very effectively inhibited by K2[B3O3F4OH], with a KI of 8.0 µM. We propose that K2[B3O3F4OH] binds to the metal ion from the enzyme active site, coordinating to the Zn(II) ion monodentately through its B-OH functionality. We hypothesize that some of the beneficial antitumor effects reported for K2[B3O3F4OH] may be due to the inhibition of CAs present in skin tumors.

Izvorni jezik
Engleski

Znanstvena područja
Kemija



POVEZANOST RADA


Projekt / tema
011-2160547-1330 - Antioksidacijski sastojci i inhibitori kolinesteraza iz aromatičnog bilja (Mladen Miloš, )

Ustanove
Kemijsko-tehnološki fakultet, Split

Autor s matičnim brojem:
Mladen Miloš, (211625)

Časopis indeksira:


  • Current Contents Connect (CCC)
  • Web of Science Core Collection (WoSCC)
    • Science Citation Index Expanded (SCI-EXP)
    • SCI-EXP, SSCI i/ili A&HCI
  • Scopus
  • MEDLINE


Citati