Hemorphins Targeting G Protein-Coupled Receptors
Mohammed Akli Ayoub1,2, Ranjit Vijayan1
1Department of Biology, College of Science, United Arab Emirates University, P.O. Box 15551 Al Ain, United Arab Emirates.
Pharmaceuticals (Basel, Switzerland)
|April 3, 2021
Summary
Hemorphins, derived from hemoglobin, interact with G protein-coupled receptors (GPCRs), influencing various physiological systems. This interaction highlights the hemorphin-GPCR axis as a potential therapeutic target.
Area of Science:
- Pharmacology
- Neuroscience
- Endocrinology
Background:
- Hemorphins are peptides from hemoglobin proteolysis with diverse physiological roles.
- They modulate proteins, including enzymes and receptors, impacting nervous and renin-angiotensin systems.
Purpose of the Study:
- To review the pharmacological and functional targeting of G protein-coupled receptors (GPCRs) by hemorphins.
- To explore the implications of hemorphin-GPCR interactions in physiology and pathophysiology.
Main Methods:
- Literature review focusing on hemorphin interactions with various GPCRs.
- Analysis of studies reporting orthosteric and allosteric modulation of GPCRs by hemorphins.
Main Results:
- Hemorphins target opioid receptors, implicated in analgesia.
- Other targeted GPCRs include those for angiotensin II, oxytocin, bombesin, bradykinin, and MAS-related G protein-coupled receptor X1.
- Both direct activation and allosteric modulation of GPCRs by hemorphins have been observed.
Conclusions:
- The hemorphin-GPCR axis is crucial for hemorphin effects in various physiological systems.
- Understanding this axis provides insight into the molecular basis of hemorphin action.
- The hemorphin-GPCR axis represents a viable therapeutic target for diverse conditions.
Related Concept Videos
Transducer Mechanism: G Protein–Coupled Receptors
3.1K
G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
GPCRs are also called heptahelical,...
3.1K
G-protein Coupled Receptors
127.9K
G-protein coupled receptors are ligand binding receptors that indirectly affect changes in the cell. The actual receptor is a single polypeptide that transverses the cell membrane seven times creating intracellular and extracellular loops. The extracellular loops create a ligand specific pocket which binds to neurotransmitters or hormones. The intracellular loops holds onto the G-protein.
127.9K
Opioid Receptors: Overview
2.9K
Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
2.9K
Role of Hematopoietic Growth Factors
2.4K
Hematopoietic growth factors are molecules that regulate the differentiation rate of hematopoietic stem cells (HSCs). Erythropoietin (EPO), primarily produced by the kidneys, plays a crucial role in erythrocyte production. When oxygen levels in the blood are low, EPO is released into the bloodstream, reaching the bone marrow, where it stimulates HSCs to differentiate and mature into erythrocytes, which are vital for oxygen transport.
Thrombopoietin (TPO), mainly released by the liver,...
Thrombopoietin (TPO), mainly released by the liver,...
2.4K
G Protein-coupled Receptors
14.8K
G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
14.8K
Secondary Messengers in Hormone Action
3.8K
Water-soluble hormones cannot cross the plasma membrane, so they rely on protein receptors that span the membrane to trigger intracellular signaling pathways. These pathways then activate second messengers inside the cell, including cAMP or calcium ions.
Many hormones bind to transmembrane G protein-coupled receptors that connect to regulatory G proteins. These G proteins can then activate enzymes such as adenylyl cyclase or phospholipase C. Adenylyl cyclase converts ATP to cAMP, activating...
Many hormones bind to transmembrane G protein-coupled receptors that connect to regulatory G proteins. These G proteins can then activate enzymes such as adenylyl cyclase or phospholipase C. Adenylyl cyclase converts ATP to cAMP, activating...
3.8K


