TASK Channels Pharmacology: New Challenges in Drug Design

Bedoya, Mauricio; Rinne, Susanne; Kiper, Aytug K.; Decher, Niels; Gonzalez, Wendy; Ramirez, David

Abstract

Rational drug design targeting ion channels is an exciting and always evolving research field. New medicinal chemistry strategies are being implemented to explore the wild chemical space and unravel the molecular basis of the ion channels modulators binding mechanisms. TASK channels belong to the two-pore domain potassium channel family and are modulated by extracellular acidosis. They are extensively distributed along the cardiovascular and central nervous systems, and their expression is up- and downregulated in different cancer types, which makes them an attractive therapeutic target. However, TASK channels remain unexplored, and drugs designed to target these channels are poorly selective. Here, we review TASK channels properties and their known blockers and activators, considering the new challenges in ion channels drug design and focusing on the implementation of computational methodologies in the drug discovery process.

Más información

Título según WOS: TASK Channels Pharmacology: New Challenges in Drug Design
Título según SCOPUS: TASK Channels Pharmacology: New Challenges in Drug Design
Título de la Revista: JOURNAL OF MEDICINAL CHEMISTRY
Volumen: 62
Número: 22
Editorial: AMER CHEMICAL SOC
Fecha de publicación: 2019
Página de inicio: 10044
Página final: 10058
Idioma: English
DOI:

10.1021/acs.jmedchem.9b00248

Notas: ISI, SCOPUS