2. Academic Validation
  3. TASK Channels Pharmacology: New Challenges in Drug Design

TASK Channels Pharmacology: New Challenges in Drug Design

  • J Med Chem. 2019 Nov 27;62(22):10044-10058. doi: 10.1021/acs.jmedchem.9b00248.
Mauricio Bedoya 1,  Susanne Rinné 2,  Aytug K Kiper 2,  Niels Decher 2,  Wendy González 1 3,  David Ramírez 4
Affiliations

Affiliations

  • 1 Centro de Bioinformática y Simulación Molecular (CBSM) , Universidad de Talca , 1 Poniente No. 1141 , 3460000 Talca , Chile.
  • 2 Institute for Physiology and Pathophysiology, Vegetative Physiology and Marburg Center for Mind, Brain and Behavior, MCMBB , Philipps-University of Marburg , Deutschhausstraße 2 , Marburg 35037 , Germany.
  • 3 Millennium Nucleus of Ion Channels-Associated Diseases (MiNICAD) , Universidad de Talca , 1 Poniente No. 1141 , 3460000 Talca , Chile.
  • 4 Instituto de Ciencias Biomédicas, Facultad de Ciencias de la Salud , Universidad Autónoma de Chile , El Llano Subercaseaux 2801, Piso 6 , 8900000 Santiago , Chile.
PMID: 31260312 DOI: 10.1021/acs.jmedchem.9b00248
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.

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