Nuclear Hormone Receptors/NHRs as Drug Target

Nuclear Hormone Receptors/NHRs as Drug Target Background

Nuclear hormone receptors (NHRs) are ligand-activated transcription factors which are involved in crucial physiological processes such as cancer, diabetes, rheumatoid arthritis, asthma or hormoneresistance syndromes. Therefore, these nuclear hormone receptors are still of great interest in modern biomedical research and drug discovery.

Nuclear Hormone Receptors (NHRs) are soluble proteins that can regulate gene expression by interacting with specific DNA sequences, and that's why therapeutic drugs can act on specific targets at the level of transcription.

In contrast to other transcription factors, the activity of nuclear hormone receptors can be modulated by binding to the corresponding ligands – small lipophilic molecules that easily penetrate biological membranes. A number of nuclear receptors identified in recent years do not have any known ligands. These so-called orphan receptors have attracted considerable interest since they could lead to the discovery of new endocrine regulatory systems.

Nuclear Hormone Receptors/NHRs as Drug Target Table

Name Drug Target Ligand
Thyroid hormone receptor THRA
THRB
thyroid hormone
thyroid hormone
Retinoic acid receptor RARA
RARB
RARG
retinoic acid
retinoic acid
retinoic acid
Peroxisome proliferator-activated receptor PPARA
PPARG
PPARD
fatty acids, leukotriene B4
fatty acids, prostaglandin J2
fatty acids
Nuclear receptor subfamily NR1D1
NR1D2
orphan
orphan
Retinoic acid receptor-related
orphan receptor
RORA
RORB
RORC
cholesterol
retinoic acid
retinoic acid
Liver X receptor NR1H3
NR1H2
oxysterols
oxysterols
Farnesoid X receptor NR1H4 bile acids
Vitamin D receptor VDR vitamin D
Pregnane X receptor NR1I2 xenobiotics
Constitutive androstane receptor NR1I3 xenobiotics
Human nuclear factor 4 HNF4A
HNF4G
orphan
orphan
Retinoid X receptor RXRA
RXRB
RXRG
retinoic acid
retinoic acid
retinoic acid
Testis receptor NR2C1
NR2C2
orphan
orphan
Chicken ovalbumin upstream
promoter-transcription factor
NR2F1
NR2F2
orphan
orphan
ErbA2-related gene-2 NR2F6 orphan
Estrogen receptor ESR1
ESR2
estradiol
estradiol
Estrogen receptor-related receptor ESRRA
ESRRB
ESRRG
orphan
orphan
orphan
Glucocorticoid receptor NR3C1 cortisol
Mineralocorticoid receptor NR3C2 aldosterone
Progesterone receptor PGR progesterone
Androgen receptor AR testosterone
Nerve growth factor-induced factor B NR4A1 orphan
Nur-related factor 1 NR4A2 orphan
Neuron-derived orphan receptor 1 NR4A3 orphan
Steroidogenic factor-1 NR5A1 orphan
Liver receptor homologous protein 1 NR5A2 orphan
Germ cell nuclear factor NR6A1 orphan
DSS-AHC critical region on the
chromosome gene 1
NR0B1 orphan
Short heterodimeric partner NR0B2 orphan
Receptors
Receptors Classification
Receptors by Differentiation Cells
Receptors by Drug Target
GPCRs as Drug Target
GPCR Ligands as Drug Target
Nuclear Hormone Receptors as Drug Target
Cell Adhesion Receptors as Drug Target
Host Defense Receptors as Drug Target
Enzyme-Linked Receptors as Drug Target+
- Receptor Tyrosine Kinases as Drug Target
- Receptor Serine/Threonine Kinases as Drug Target
- Receptor Tyrosine Phosphatases as Drug Target
Other Receptors as Drug Target
Receptors by Functions
Receptors Reagent Products
Receptors by Species