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Last update 08 May 2025

NR2E1

Last update 08 May 2025

Basic Info

Synonyms

hTll, NR2E1, nuclear receptor subfamily 2 group E member 1

+ [7]

Introduction

Orphan receptor that binds DNA as a monomer to hormone response elements (HRE) containing an extended core motif half-site sequence 5'-AAGGTCA-3' in which the 5' flanking nucleotides participate in determining receptor specificity (By similarity). May be required to pattern anterior brain differentiation. Involved in the regulation of retinal development and essential for vision. During retinogenesis, regulates PTEN-Cyclin D expression via binding to the promoter region of PTEN and suppressing its activity (By similarity). May be involved in retinoic acid receptor (RAR) regulation in retinal cells.

Drugs associated with NR2E1

US20240067625

Patent Mining

Target

NR2E1

Mechanism

NR2E1 modulators

Active Org.

Baylor College of Medicine

Originator Org.

Baylor College of Medicine

Active Indication

Metabolic Diseases [+3]

Inactive Indication-

Drug Highest PhaseDiscovery

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

100 Clinical Results associated with NR2E1

100 Translational Medicine associated with NR2E1

0 Patents (Medical) associated with NR2E1

240

Literatures (Medical) associated with NR2E1

14 Mar 2025·ACS Pharmacology & Translational Science

Comparative Evaluation and Profiling of Chemical Tools for the Nuclear Hormone Receptor Family 2

Article

Author: Busch, Romy ; Lewandowski, Max ; Marschner, Julian A. ; Merk, Daniel

Nuclear receptors regulate transcription in response to ligand signals and enable the pharmacological control of gene expression. However, many nuclear receptors are still poorly explored and are not accessible to ligand-based target identification studies. In particular, most members of the NR2 family are among the least studied proteins of the class, and apart from the retinoid X receptors (RXR), validated NR2 ligands are very rare. Here, we gathered the NR2 modulators reported in literature for comparative profiling in uniform test systems. Most candidate compounds displayed insufficient on-target activity or selectivity to be used as chemical tools for NR2 receptors underscoring the urgent need for further NR2 ligand development. Nevertheless, a small NR2 modulator set could be assembled for application in a chemogenomic fashion. There are 48 ligand-activated transcription factors in humans forming the superfamily of nuclear receptors (NRs, Figure 1a),^1,2 which translate (endogenous) ligand signals into changes in gene expression patterns.³ The multifaceted roles of NRs span pivotal physiological processes, encompassing metabolism, inflammation, and cellular differentiation.⁴ Over decades, the NR1 and NR3 receptor families, including (steroid) hormone receptors and lipid sensors, have emerged as well-explored therapeutic targets of essential drugs like, for example, glucocorticoids as anti-inflammatory drugs, estrogen receptor modulators as contraceptives and anticancer agents, and PPAR agonists as oral antidiabetics.^5-7 Despite this progress, a significant portion of the NR superfamily remains understudied, particularly within the NR2 family which comprises the hepatocyte nuclear factor-4 receptors (HNF4α/γ; NR2A1/2), the retinoid X receptors (RXRα/β/γ; NR2B1-3), the testicular receptors (TR2/4; NR2C1/2), the tailless-like receptors (TLX and PNR; NR2E1/3), and the COUP-TF-like receptors (COUP-TF1/2, V-erBA-related gene; NR2F1/2/6).^8,9 Apart from RXR, all NR2 receptors are considered as orphan, and their ligands remain widely elusive. Therefore, chemical tools for most NR2 receptors are rare and poorly annotated posing an obstacle to target identification and validation studies. To enable chemogenomics on NR2 receptors and improve annotation, of the few available ligands, we gathered a scarce collection of NR2 modulators (agonists, antagonists, inverse agonists) for comparative evaluation and profiling. While the NR2B family (RXR) is well covered with high-quality ligands and a few early tools are available for NR2E1, we found the available ligands of the NR2A and NR2C families of insufficient quality to be used as chemical tools.

01 Jan 2025·Cell Reports

Chromatin-site-specific accessibility: A microtopography-regulated door into the stem cell fate

Article

Author: Wang, Qianchun ; Ji, Baohua ; Wang, Xianliu ; Wang, Xiaozhao ; Sun, Wei ; Zhou, Wenyan ; Zhang, Xiaoan ; Lin, Junxin ; Zhu, Qiuwen ; Yao, Xudong ; Ouyang, Hongwei ; Yan, Yiyang

Biomaterials that mimic extracellular matrix topography are crucial in tissue engineering. Previous research indicates that certain biomimetic topography can guide stem cells toward multiple specific lineages. However, the mechanisms by which topographic cues direct stem cell differentiation remain unclear. Here, we demonstrate that microtopography influences nuclear tension in mesenchymal stem cells (MSCs), shaping chromatin accessibility and determining lineage commitment. On aligned substrates, MSCs exhibit high cytoskeletal tension along the fiber direction, creating anisotropic nuclear stress that opens chromatin sites for neurogenic, myogenic, and tenogenic genes via transcription factors like Nuclear receptor TLX (TLX). In contrast, random substrates induce isotropic nuclear stress, promoting chromatin accessibility for osteogenic and chondrogenic genes through Runt-related transcription factors (RUNX). Our findings reveal that aligned and random microtopographies direct site-specific chromatin stretch and lineage-specific gene expression, priming MSCs for distinct lineages. This study introduces a novel framework for understanding how topographic cues govern cell fate in tissue repair and regeneration.

01 Sep 2024·Advances in Medical Sciences

Lack of Nr2e1 expression in hepatocytes impaired cell survival and aggravated palmitate-induced oxidative stress

Article

Author: Song, Linyang ; Xiong, Qing ; Wang, Huawei ; Feng, Jieyuan ; Xu, Yancheng ; Wu, Guijun

PURPOSENuclear receptor subfamily 2 group E member 1 (Nr2e1) has been regarded as an essential regulator in neural stem cells. However, its function is still not clear in hepatocytes. This study aimed to clarify the effects of Nr2e1-deficiency in hepatocytes in lipotoxic conditions.MATERIALS/METHODSNr2e1-knockdown AML12 cells were generated by lentiviral vector transfection. The influences of Nr2e1-deficiency on hepatocyte survival were determined by cell cycle progression and cell apoptosis rate using flow cytometry. Real-time quantitative PCR and Western blot were used to examine the genes and protein expression related to apoptosis, lipid metabolism, and oxidative stress. Meanwhile, RNA sequencing was adopted in liver samples from Nr2e1-knockout (Nr2e1-KO) mice.RESULTSNr2e1 expression was observed with a significant decrease in AML12 cells after palmitic acid-stimulation. Knockdown of Nr2e1 in AML12 cells resulted in increased sensitivity to lipotoxicity, evidenced by a partial G0/G1 cell-cycle arrest and higher rates of cell apoptosis. Moreover, Nr2e1-knockdown AML12 cells presented increased gene expressions relative to lipid synthesis but decreased levels of β-oxidation related genes. Lack of Nr2e1 augmented palmitate-induced oxidative stress in hepatocytes. In vivo, differential genes in Nr2e1-KO mice liver were enriched in pathways associated with liver regeneration and cell proliferation.CONCLUSIONSThis study indicated that hepatocytes lacking Nr2e1 were more susceptible to lipotoxic-mediated damage. Nr2e1 may serve as a potential target for the development of novel therapies for lipotoxicity-induced liver injury.

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NR2E1

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