UTS2R - Urotensin 2 Receptor | Elisa - Clia - Antibody - Protein

Background

Urotensin 2 Receptor (UTS2R), also known as GPR14, is a G protein-coupled receptor (GPCR) that binds to urotensin II (UII), a peptide hormone initially discovered in fish and subsequently identified in mammals, including humans. UTS2R is widely expressed in various tissues and organs, including the cardiovascular system, central nervous system, and peripheral tissues. The primary ligand for UTS2R is urotensin II (UII), a cyclic peptide composed of 11 amino acids. UII binds to UTS2R with high affinity and specificity, leading to the activation of intracellular signaling cascades. In summary, Urotensin 2 Receptor (UTS2R) plays important roles in cardiovascular regulation, central nervous system modulation, renal function, and potentially endocrine regulation. Dysregulation of UII signaling and UTS2R activation is implicated in various diseases, making UTS2R a potential therapeutic target for cardiovascular diseases, renal disorders, neurological disorders, and endocrine disorders.

Structural Features:

UTS2R is a seven-transmembrane domain receptor, typical of GPCRs, with an extracellular N-terminus and an intracellular C-terminus. Its structure allows it to interact with UII and activate downstream signaling pathways.

Physiological Functions:

1.   Cardiovascular Regulation: UII and UTS2R play a role in cardiovascular regulation, influencing vascular tone, blood pressure, cardiac contractility, and remodeling. Activation of UTS2R can lead to vasoconstriction, cardiac hypertrophy, and fibrosis.

2.   Central Nervous System Modulation: UTS2R is expressed in various regions of the central nervous system, where it modulates neuronal activity and neurotransmitter release. UII signaling through UTS2R may influence pain perception, locomotion, and stress responses.

3.   Renal Function: UII and UTS2R are involved in renal physiology, including the regulation of renal blood flow, glomerular filtration rate, and sodium excretion. UII-induced vasoconstriction can affect renal hemodynamics.

4.   Endocrine Regulation: UII and UTS2R may play a role in endocrine regulation, although their specific contributions are not fully understood.

Clinical Implications:

• Cardiovascular Diseases: Dysregulation of UII signaling and UTS2R activation is implicated in cardiovascular diseases such as hypertension, heart failure, atherosclerosis, and pulmonary hypertension. UTS2R antagonists are being investigated as potential therapeutic agents for these conditions.
• Renal Disorders: UII and UTS2R may contribute to renal dysfunction in conditions such as chronic kidney disease and diabetic nephropathy, making them potential targets for therapeutic intervention.
• Neurological Disorders: UII and UTS2R have been implicated in neurological disorders such as migraine, neuropathic pain, and neurodegenerative diseases, although their exact roles are still under investigation.
• Endocrine Disorders: UII and UTS2R may be involved in endocrine disorders such as diabetes and obesity, although further research is needed to elucidate their specific contributions.

Therapeutic Potential:

1.   UTS2R Antagonists: Development of UTS2R antagonists as potential therapeutics for cardiovascular diseases, renal disorders, and other conditions associated with UII/UTS2R dysregulation.

2.   Modulation of Vascular Tone: Targeting UII/UTS2R signaling pathways to modulate vascular tone and blood pressure for the treatment of hypertension and other cardiovascular conditions.

3.   Neurological Therapeutics: Investigating the potential of UTS2R modulation for the treatment of neurological disorders associated with pain and neuroinflammation.

4.   Renoprotective Agents: Developing UTS2R antagonists or modulators to protect against renal dysfunction and damage in various renal disorders.