TR2 nuclear receptor in vitamin A signaling

NIH RePORTER · NIH · R01 · $466,114 · view on reporter.nih.gov ↗

Abstract

Project Summary The grant “TR2 nuclear receptor in vitamin A signaling” (since 08/01/99) was initiated from studying retinoic acid (RA) signaling using an embryonic stem cell-specific orphan receptor TR2’s (NR2C1) as a model to understand RA’s action in developmental regulation. The long-term goal is to comprehensively understand RA signaling pathways in health and diseases. Results first established RA’s activity in chromatin-remodeling via RA receptors (RARs), Retinoid X receptors (RXRs) and TR2. In 2008, we reported a then-mysterious effect of RA that did not involve RAR/RXR - it occurred rapidly in the cytoplasm to modulate ERK signaling, and thus was proposed as “non-canonical”. Previous proposal (05/1/2017-04/30/2022) aimed to i) identify the mediator of this non-canonical activity of RA in modulating ERK signaling and synthetic RA-like ligands specific to this pathway, and ii) determine the physiological relevance. Results (published in 14 papers) have established Cellular Retinoic Acid Binding Protein 1 (CRABP1) as the mediator, characterized RA-CRABP1-RAF-MEK- ERK signaling pathway and CRABP1 ligands specific to this pathway, and revealed physiological relevance in maintaining neuron stem cell pool, adiposity and inflammation, all involving CRABP1-ERK regulation. Recently, a second signaling pathway also directly modulated by CRABP1 was uncovered, calcium/calmodulin- dependent protein kinase II (CaMKII), but in a different physiological context - excitable cells requiring tight regulation of CaMKII such as motor neurons (MNs) and cardiomyocytes. The principal hypothesis is, RA- CRABP1 signalosomes form in specific cellular environments to provide timely (rapid) modulatory mechanisms ensuring homeostatic propagation of intracellular signals that are critical to the survival/function of the cells. Pertinent to CRABP1-CaMKII, our recent data show that CRABP1 is highly expressed in MNs, and CRABP1 knockout (CKO) mice spontaneously develop age-dependent motor deficit resembling motor symptoms of MN degenerative disease Amyotrophic Lateral Sclerosis (ALS), preceded by morphological, structural, and functional deterioration of MNs and neuromuscular junctions (NMJs). We thus engineered a sequenced MN-muscle co-differentiation system on custom-fabricated Hydrogel to generate an in vitro, functional 3D NMJ model for molecular studies. Two aims are to i) dissect molecular mechanisms of RA-CRABP1-CaMKII signalsome action in NMJ and identify CRABP1 ligands specific to this pathway, and ii) determine the physiological action of RA-CRABP1-CaMKII signaling and its disease relevance/therapeutic applications. Aim 1 will employ engineered 3D NMJ model to dissect physiologically relevant signaling pathways and molecular mechanisms. Aim 2 will distinguish “non-canonical” from “canonical” activity of RA by comparing CRABP1 ligands and RA in maintaining healthy NMJs, and determine the therapeutic potential of targeting CRABP1 to improve motor function.

Key facts

NIH application ID
10818552
Project number
5R01NS132277-21
Recipient
UNIVERSITY OF MINNESOTA
Principal Investigator
Li-Na Wei
Activity code
R01
Funding institute
NIH
Fiscal year
2024
Award amount
$466,114
Award type
5
Project period
1999-08-01 → 2028-04-30