A
nuclear receptor is a protein found inside a cell that acts as a switch to turn genes on or off.
Full definition
The study focused on a small subset
of nuclear receptors, a large family of proteins that regulate gene expression in response to signals from various binding partners, including steroids and fats.
Until this latest study, many researchers believed that
most nuclear receptors are organized like beads on a string.
Based on basic transcriptional studies of midbrain dopamine neurons, Dr. Kim's lab identified the
orphan nuclear receptor Nurr1 as a potential drug target of Parkinson's disease (PD) to develop novel drug candidates for neuroprotective and mechanism - based therapeutics.
Agonists for
nuclear receptor Nurr1 enhance its dual functions and improve behavioral deficits in animal models of Parkinson's disease.
Center
for Nuclear Receptors & Cell Signaling (CNRCS) Assistant Professor Daniel Frigo and his research team recently published a study investigating the processes through which androgen receptors affect prostate cancer progression.
Like
other nuclear receptors, HNF - 4α has a pocket that binds natural signaling molecules or could be targeted with synthetic drugs.
Dietary fibre modifications that are low in fat and glucose reduce the risk for AD by not only effecting cell membranes and nutrient sensing G coupled receptors but also by regulating number of
nuclear receptors such as histone deacetylases (HDAC) and peroxisome proliferator activated receptors (PPAR) that control glucose, fatty acids and cholesterol and have significant effects on the brain cholesterol homeostasis and amyloidosis.
His team has made potent and selective chemical probes for orphan
nuclear receptors widely available in the scientific community.
Thomas Burris, Ph.D., chair of pharmacology and physiology at Saint Louis University and Colin Flaveny, Ph.D., assistant professor of pharmacology and physiology at SLU, study natural hormones that
regulate nuclear receptors.
«Strikingly, treatment with a steroid hormone called Δ7 - dafachronic acid, a chemical that binds to a
parasite nuclear receptor called Ss - DAF - 12, significantly reduced the worm burden in MPA - treated mice,» Dr. Mangelsdorf said.
Nuclear receptors make good drug targets because one region is bound to DNA, while a pocket sits open on another part of the protein, just waiting to hold a signaling molecule.
«
Nuclear receptors bind different types of molecules, and some of these receptors physically interact with each other to integrate different signals,» Kojetin said.
«Previous structural studies of HNF - 4α and
related nuclear receptors only revealed smaller, isolated fragments of these proteins,» said Fraydoon Rastinejad, Ph.D., professor in Sanford - Burnham's Diabetes and Obesity Research Center, located at the Institute's Lake Nona campus in Orlando, Fla., and senior author of the study.
According to the Wolf Prize jury, Evans was selected for his discovery of the gene super-family
encoding nuclear receptors and elucidating the mechanism of action of this class of receptors.
These researchers gave the mice synthetic agonists to
certain nuclear receptors that are involved in controlling expression of circadian clock proteins...
In April 2009 Anouk started her PhD research on «the role of
Nuclear receptor Nur77 during inflammation» at the department of Medical Biochemistry of the Academic Medical Center (AMC) Amsterdam in The Netherlands under the supervision of Prof. Carlie JM de Vries and received her degree in February 2015.
Protecting RPE and Photoreceptors by Targeting a
Novel Nuclear Receptor in Dry AMD Jing Chen, PhD Boston Children's Hospital, Harvard Medical School (Boston, MA)
Although Nurr1 is a ligand -
independent nuclear receptor, Dr. Kim hypothesizes that Nurr1 may have endogenous ligand (s) and is pursuing to identify and characterize potential Nurr1's endogenous ligand (s).
Full Citation: The orphan
nuclear receptor Nr4a1 couples sympathetic and inflammatory cues in CNS - recruited macrophages to limit neuroinflammation.
Dissection of the
LXXLL nuclear receptor - coactivator interaction motif using combinatorial peptide libraries: discovery of peptide antagonists of estrogen receptors alpha and beta
by regulating number
of nuclear receptors such as histone deacetylases (HDAC) and peroxisome proliferator activated receptors (PPAR) that control glucose, fatty acids and cholesterol and have significant effects on the brain cholesterol homeostasis and amyloidosis.
Naringenin, a chemical found in grapefruit and in other citrus fruits, activates proteins
called nuclear receptors that cause the liver to break down fatty acids, study researchers from Hebrew University of Jerusalem and Massachusetts General Hospital in Boston said in a statement.
The vitamin A — RXR - alpha complex «dimerizes» with these
other nuclear receptors, forming a new complex that acts as a transcription factor to turn on gene expression.
Dr. Kim and his group work to identify the defective components from these cells — like the orphan
nuclear receptor Nurr1, which is critical for dopamine neurons and inflammation — in order to understand and reverse the damage.
He led the Glaxo program on
orphan nuclear receptors that uncovered their role in regulation of human metabolism and was co-discoverer of obeticholic acid, a breakthrough medicine for liver diseases targeting FXR.
Muscles: testosterone increases neurotransmitters at the muscle fiber site, stimulates protein synthesis in muscles by interacting with
DNA nuclear receptors, enhances muscle cell receptor sensitivity to effects of free testosterone, and stimulates growth hormone responses that enhance cellular amino acid uptake and protein synthesis in skeletal muscle.
In the course of this work, Burris and Flaveny have explored the roles of
the nuclear receptor REV - ERB, which regulates key processes in the body, from sleep to cholesterol, and, most recently, muscle regeneration.
«Scientists slow progression of fatal form of muscular dystrophy: Hope lies in
nuclear receptor that regulates muscle.»
Inhibiting
a nuclear receptor in the gut could lead to a treatment for a liver disorder that affects almost 30 percent of the Western world's adult population, according to an international team of researchers.
They discovered that
a nuclear receptor protein, estrogen - related receptor γ (ERRγ), occurred in much larger amounts in adult beta cells.
A team of researchers led by Tokyo Medical and Dental University (TMDU) previously found that upon the onset of lactation after birth, milk lipids serve as a ligand to activate
the nuclear receptor peroxisome proliferator - activated receptor (PPAR) α, which is a key transcriptional regulator of liver fat metabolism.
The scientists hope to continue their research to further examine whether drugs interacting with
the nuclear receptors can help to prevent jet lag from affecting bile acid levels in the liver, with the ultimate goal of potentially using them as pharmaceutical strategies to prevent liver cancer in humans.
Originally, however, they were not examining brown fat thermogenesis, but instead were looking for clues to the function of ERRβ, a protein about which little was known at the time, except that it was closely related to ERRα, appeared in brown fat cells, and also worked as a so - called
nuclear receptor — a molecular switch for gene activation that can be turned on by small lipophilic molecules or a signaling protein partner.
The researchers found that circadian clock disruption activated two
nuclear receptors that help regulate liver bile acid metabolism.
The compound targets a pair of
nuclear receptors (RORα and RORγ) that play critical roles in the development of a specific population (Th17) of immune cells associated with the disease.
Therapeutic drugs can also be made to fit these pockets, switching
the nuclear receptor on or off to alter gene expression.
HNF - 4α is a special type of protein called
a nuclear receptor.
The Nuclear Receptor Signaling Atlas (NURSA) is partnering with the NIDDK Information Network (dkNET) to host a dataset challenge, and we invite you to join!
ATRA has been generally known to exert its roles through
their nuclear receptors.