Pharmacological Modulation of Calcium Homeostasis in Familial Dilated Cardiomyopathy: An In Vitro Analysis From an RBM20 Patient-Derived iPSC Model

Clin Transl Sci. 2016 Jun;9(3):158-67. doi: 10.1111/cts.12393. Epub 2016 Apr 22.

Abstract

For inherited cardiomyopathies, abnormal sensitivity to intracellular calcium (Ca(2+) ), incurred from genetic mutations, initiates subsequent molecular events leading to pathological remodeling. Here, we characterized the effect of β-adrenergic stress in familial dilated cardiomyopathy (DCM) using human-induced pluripotent stem cell (hiPSC)-derived cardiomyocytes (CMs) from a patient with RBM20 DCM. Our findings suggest that β-adrenergic stimulation accelerated defective Ca(2+) homeostasis, apoptotic changes, and sarcomeric disarray in familial DCM hiPSC-CMs. Furthermore, pharmacological modulation of abnormal Ca(2+) handling by pretreatment with β-blocker, carvedilol, or Ca(2+) -channel blocker, verapamil, significantly decreased the area under curve, reduced percentage of disorganized cells, and decreased terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick-end labeling (TUNEL)-positive apoptotic loci in familial DCM hiPSC-CMs after β-adrenergic stimulation. These translational data provide patient-based in vitro analysis of β-adrenergic stress in RBM20-deficient familial DCM hiPSC-CMs and evaluation of therapeutic interventions to modify heart disease progression, which may be personalized, but more importantly generalized in the clinic.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Apoptosis / drug effects
  • Calcium / metabolism*
  • Calcium Signaling / drug effects
  • Carbazoles / pharmacology
  • Cardiomyopathy, Dilated / metabolism*
  • Cardiomyopathy, Dilated / pathology*
  • Carvedilol
  • Homeostasis* / drug effects
  • Humans
  • Induced Pluripotent Stem Cells / metabolism*
  • Models, Biological*
  • Myocytes, Cardiac / drug effects
  • Myocytes, Cardiac / metabolism
  • Myocytes, Cardiac / pathology
  • Norepinephrine / pharmacology
  • Propanolamines / pharmacology
  • RNA-Binding Proteins / metabolism*
  • Receptors, Adrenergic, beta / metabolism
  • Sarcomeres / drug effects
  • Sarcomeres / metabolism
  • Stress, Physiological
  • Verapamil / pharmacology

Substances

  • Carbazoles
  • Propanolamines
  • RNA-Binding Proteins
  • Receptors, Adrenergic, beta
  • ribonucleic acid binding motif protein 20, human
  • Carvedilol
  • Verapamil
  • Calcium
  • Norepinephrine

Supplementary concepts

  • Familial dilated cardiomyopathy