Desensitization of beta1 adrenergic receptor-nitric oxide signaling in cardiac diseases

NIH RePORTER · VA · I01 · · view on reporter.nih.gov ↗

Abstract

Emerging evidence indicates that nitric oxide (NO) is involved in cardiac β1 adrenergic receptor (β1AR) stimulation of cardiac function. We propose that scaffold protein SAP97 plays a critical role in regulation of cardiac β1AR-induced NOS1-NO signaling cascade via organizing a β1AR- NOS1 signalosome. This pathway is necessary for regulation of cardiac contractile function. We also hypothesize that G-protein kinase 5 (GRK5) promotes phosphorylation of cardiac β1AR PDZ motif and dissociation of the receptor from the SAP97-organized signalosome for activation of NOS1-NO signaling and promotes desensitization of receptor signaling in cardiac diseases. We will test the hypotheses with the following aims. Aim 1. SAP97 regulates β1AR-induced NO signaling in heart. Aim 2. SAP97 maintains the integrity of β1AR-SAP97-NOS1 signalosome to preserve cardiac function. Aim 3. GRK5 promotes desensitization of β1AR-NO signaling via disruption of the receptor-SAP97 signalosome in heart failure.

Key facts

NIH application ID
10121283
Project number
1I01BX005100-01A1
Recipient
VA NORTHERN CALIFORNIA HEALTH CARE SYS
Principal Investigator
YANG Kevin XIANG
Activity code
I01
Funding institute
VA
Fiscal year
2021
Award amount
Award type
1
Project period
2021-04-01 → 2025-03-31