What are GPCRs? GPCRs are the Mighty Receptors of Neurotransmitters

Learn more about what GPCRs are and how psychedelics interact with GPCRs like the serotonin receptor to do what they do

GPCRs, if you start looking into the science of psychedelics, are everywhere. They are each and every neurotransmitter receptor that responds to a neurotransmitter or drug.

The epinephrine receptor was the first human GPCR to be studied, with it purified to obtain a structure of the beta-2 adrenergic receptor in 2007.

GPCRs have been studied since the 1980s with the first G-protein coupled receptor to be isolated being the bovine rhodopsin receptor, an enzyme found in the eyes of bovine. In the case of rhodopsin, the GPCR senses light. In the case, of serotonin receptor, the GPCR recognizes the serotonin molecule.

Let’s get into what GPCRs are — G-protein coupled receptors — and the 3 most important things to know, from a scientific wellness perspective.

G-protein coupled receptor: GPCRs are proteins, meaning they are chains of amino acids. If you want to know more about proteins, protein structure, and the basics of enzymology, the place for that is @psychedelic.chemistry over at Instagram.

The G in G-protein isn’t gangster or grand, it’s G as in guanosine, one of the bases found in DNA and RNA nucleosides, oligonucleotides, mRNAs, and chromosomal DNA, among other kinds of nucleic acid chains. So the “G-protein” is coupled to several other subsections, usually called domains, of the protein, this chain of amino acids.

G protein-coupled receptors (GPCRs) are a large and diverse family of cell membrane proteins that play a crucial role in cellular signaling and communication. This means they live in the membranes of the cells where they’re found.

GPCRs have a certain appearance, because sections of how the GPCR fold and clump together does so in a way in which there are 7 sections. These 7 sections cross the plane of the membrane of the cell, so they are sometimes called “7 transmembrane” proteins or 7-TM proteins. Those “clumps” mentioned there, those are actually helices made of certain repeating amino acids that form the so-called “alpha” helices.

From a scientific wellness perspective, there are three important aspects to consider when discussing GPCRs:

1. Role in physiological processes: GPCRs are involved in a wide range of physiological processes, including neurotransmission, immune response, and hormonal regulation.
   • They are critical for maintaining the overall balance and functioning of the human body. Many drugs, including some psychedelic substances, target GPCRs to modulate their effects, which can influence various aspects of human wellness, such as mood regulation, pain perception, and appetite control.
2. Drug targets: GPCRs are the target of approximately 30-40% of all marketed drugs.
   • They are an essential component of the pharmaceutical industry’s efforts to develop new treatments for a variety of diseases and disorders, including mental health conditions. By understanding the molecular mechanisms through which GPCRs operate, researchers can develop more effective and targeted therapies with fewer side effects, leading to improved patient outcomes and overall wellness.
3. Personalized medicine: Genetic variations in GPCRs can influence an individual’s response to certain medications and treatments, including those related to mental health and wellness.
   • By examining an individual’s unique genetic makeup and understanding how it may affect GPCR function, personalized medicine has the potential to optimize treatment strategies and improve health outcomes. This approach can lead to more tailored therapies, addressing the unique needs of each patient and ensuring that they receive the most effective and appropriate care for their specific conditions.

The range of companies seeking GPCR research is staggering, due to the fact that 30% to 40% of drug targets are aimed at GPCRs. A few leaders include Sosei Heptares, Domain Therapeutics, and Microbiotix with Septerna a recent entrant, founded in 2021.

Enthereal supports businesses as well as patient stakeholder groups. Enthereal does this by advocating for and innovating on access for more people to meaningful interpretation and ownership of genetic information with privacy-for-patient-first approaches. Ask our consultants about how we explore and realize the best options available. Enthereal can support your readiness as well as your operational capacity with our modular delivery packages.