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ATPases do tipo P como alvos terapêuticos
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Abstract(s)
As ATPases do tipo P ou P-ATPases são enzimas transmembranares que controlam o fluxo de iões, tais como, K+, Na+, H+, Ca2+, em diferentes células e organelos celulares. Esses iões desempenham um papel fundamental no controlo da homeostasia e dos gradientes electroquímicos nas células. Devido a esse seu papel importante as ATPases têm sido alvos de estudo nestas últimas décadas. A sua modulação por inibidores é promissora para o tratamento de doenças, tais como, cancro da próstata, isquemia do coração e doenças gástricas. De 18 principais inibidores das bombas Na+/K+; K+/H+ e Ca2+-ATPase são conhecidos os mecanismos de acção de 10 (palitoxina, omeprazol, PCAB, ácido scopadulcico B, tapsigargina, ácido ciclopiazónico, curcumina, 2,5-(t-butil)-dihidroxibenzeno, ouabaína e vanádio). Para os outros apenas se sabe que inibem ou que se ligam a determinada região mas as alterações conformacionais que promovem continuam incertas. Com a utilização da cristalografia de raio x e de estudos de mutação génica têm sido fabricados inibidores cada vez mais específicos e menos tóxicos para as células. Espera-se que num futuro próximo a utilização de inibidores para ATPases do tipo P seja muito vantajosa para o tratamento de várias patologias.
The ATPases of P type or P-ATPases are transmembrane enzymes which control ions flux, such as K+, Na+, H+, Ca2+, in different cells and cellular organelles. These ions play a fundamental role in control of homeostasis and electrochemical gradients in cells. Due to that important role, ATPases, have been study in these last decades. They modulation by inhibitors is promising for treating diseases, as prostate cancer, heart ischemia and gastric diseases. Of 18 major pump inhibitors are known mechanisms of action of 10 (Palytoxin, Omeprazole, PCAB, Scopadulcic Acid B, Thapsigargin, Cyclopiazonic acid, Curcumin, 2,5-di-(t-butyl)-dihydroxybenzene, ouabain and vanadium). For others only known they inhibit or bind it to a certain region but conformational changes that promote remain uncertain. Through x-ray crystallography and mutagenic studies have been produced inhibitors more specific and less toxic to cells. In near future is expected that utilization of inhibitors for ATPase of P type it’s very advantageous for the treatment of several diseases.
The ATPases of P type or P-ATPases are transmembrane enzymes which control ions flux, such as K+, Na+, H+, Ca2+, in different cells and cellular organelles. These ions play a fundamental role in control of homeostasis and electrochemical gradients in cells. Due to that important role, ATPases, have been study in these last decades. They modulation by inhibitors is promising for treating diseases, as prostate cancer, heart ischemia and gastric diseases. Of 18 major pump inhibitors are known mechanisms of action of 10 (Palytoxin, Omeprazole, PCAB, Scopadulcic Acid B, Thapsigargin, Cyclopiazonic acid, Curcumin, 2,5-di-(t-butyl)-dihydroxybenzene, ouabain and vanadium). For others only known they inhibit or bind it to a certain region but conformational changes that promote remain uncertain. Through x-ray crystallography and mutagenic studies have been produced inhibitors more specific and less toxic to cells. In near future is expected that utilization of inhibitors for ATPase of P type it’s very advantageous for the treatment of several diseases.
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Keywords
P-ATPases Cardiotónicos