Archive for the ‘HERG’ Category

KCR1 blocks drug HERG binding

February 28, 2007

Individualized medicine to reduce the risk of adverse side effects of certain drugs will hopefully find a place in drug development in the near future. Had this approach been available in the past there would be a number of drugs that would not have been pulled from the market due to unacceptable side effects in a small percentage of patients. In the past decade HERG blockage has arisen as a major concern, which has probably stopped a number of drugs from being developed.

In a recent paper in J. Biol. Chem. expression of the protein KCR1 (K+ channel regulatory) tends toprotect HERG from being blocked by dofetilide.  There is a “gain of function” polymorphism that is observed in the gene that codes for this protein which leads to a lower risk of acquired drug induced QT prolongation. Therefore, drugs associated with QT prolongation might be safe for people having this polymorphism.