AT1R blockade in adverse milieus: role of SMRT and corepressor complexes

Am J Physiol Renal Physiol. 2015 Aug 1;309(3):F189-203. doi: 10.1152/ajprenal.00476.2014. Epub 2015 Jun 17.

Abstract

ANG II type 1 receptor blockade (AT1R-BLK) is used extensively to slow down the progression of proteinuric kidney diseases. We hypothesized that AT1R-BLK provides podocyte protection through regulation of silencing mediator of retinoic acid and thyroid hormone receptor (SMRT) and vitamin D receptor (VDR) expression under adverse milieus such as high glucose and human immunodeficiency virus infection. Both AT1R-BLK and VDR agonists (VDAs) stimulated VDR complex formation that differed not only in their composition but also in their functionality. AT1R-BLK-induced VDR complexes contained predominantly unliganded VDR, SMRT, and phosphorylated histone deacetylase 3, whereas VDA-VDR complexes were constituted by liganded VDR and CREB-binding protein/p300. AT1R-BLK-induced complexes attenuated podocyte acetyl-histone 3 levels as well as cytochrome P-450 family 24A1 expression, thus indicating their deacetylating and repressive properties. On the other hand, VDA-VDR complexes not only increased podocyte acetyl-histone 3 levels but also enhanced cytochrome P-450 family 24A1 expression, thus suggesting their acetylating and gene activation properties. AT1R-BLK- induced podocyte SMRT inhibited expression of the proapoptotic gene BAX through downregulation of Wip1 and phosphorylation of checkpoint kinase 2 in high-glucose milieu. Since SMRT-depleted podocytes lacked AT1R-BLK-mediated protection against DNA damage, it appears that SMRT is necessary for DNA repairs during AT1R-BLK. We conclude that AT1R-BLK provides podocyte protection in adverse milieus predominantly through SMRT expression and partly through unliganded VDR expression in 1,25(OH)2D-deficient states; on the other hand, AT1R-BLK contributes to liganded VDR expression in 1,25(OH)2D-sufficient states.

Keywords: angiotensin II; angiotensin II type 1 receptor blockade; glucose; silencing mediator of retinoic acid and thyroid hormone receptor; vitamin D receptor.

Publication types

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

MeSH terms

  • Acetylation
  • Angiotensin II Type 1 Receptor Blockers / pharmacology*
  • Apoptosis Regulatory Proteins / biosynthesis
  • Co-Repressor Proteins / drug effects
  • DNA Damage
  • Dose-Response Relationship, Drug
  • Histones / metabolism
  • Humans
  • Losartan / pharmacology
  • Nuclear Receptor Co-Repressor 2 / physiology*
  • Podocytes / drug effects
  • Podocytes / enzymology
  • Proteasome Endopeptidase Complex / drug effects
  • Protective Agents / pharmacology
  • Receptors, Calcitriol / drug effects
  • Vitamin D3 24-Hydroxylase / biosynthesis
  • Vitamin D3 24-Hydroxylase / metabolism

Substances

  • Angiotensin II Type 1 Receptor Blockers
  • Apoptosis Regulatory Proteins
  • Co-Repressor Proteins
  • Histones
  • NCOR2 protein, human
  • Nuclear Receptor Co-Repressor 2
  • Protective Agents
  • Receptors, Calcitriol
  • Vitamin D3 24-Hydroxylase
  • Proteasome Endopeptidase Complex
  • Losartan