2020 - Drug effects on human Na+/Ca2+ exchanger and implications for testing new drug candidates
SURFE²R N1 and SURFE²R 96SE poster, Safety Pharmacology Society Virtual Meeting 2020 (1.2 MB)
The Na+/Ca2+-exchanger (NCX) plays an important role in cellular calcium homeostasis. Under physiological conditions NCX removes Ca2+ from the cell lumen of excitable cells and is involved in regulatory processes. Under pathological conditions, NCX can reverse direction and contribute to cell damage by Ca2+ overloading. These critical functions have fueled the debate over the pharmacological potential of NCX since many years. Inhibition of the reversed mode of NCX is thought to be beneficial in ischemia/reperfusion injury. Moreover, inhibition of NCX has been proposed to exhibit an antiarrhythmic effect. On the other hand the risk of inadvertent NCX inhibition as a secondary drug effect is poorly investigated and unspecific NCX inhibition is usually not tested during drug development.
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