Article
Na(+),K(+)-ATPase isoform selectivity for digitalis-like compounds is determined by two amino acids in the first extracellular loop.
Chemical research in toxicology - 15 Dec 2014
Weigand Karl M, Laursen Mette, Swarts Herman G P, Engwerda Anthonius H J, Prüfert Christian, Sandrock Julia, Nissen Poul, Fedosova Natalya U, Russel Frans G M, Koenderink Jan B
Abstract excerpt
Digitalis-like compounds (DLCs) comprise a diverse group of molecules characterized by a cis-trans-cis ring-fused steroid core linked to a lactone. They have been used in the treatment of different medical problems including heart failure, where their inotropic effect on heart muscle is attributed to potent Na(+),K(+)-ATPase inhibition. Their application as drugs, however, has declined in recent past years due to...
Topics
- Amino Acids
- Digitalis Glycosides
- Isoenzymes
- Mutation
- Sodium-Potassium-Exchanging ATPase
- Substrate Specificity