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Research draft

G protein-coupled recepteishon

vr.tr.g-protein-coupled-recepteishon · PHY.MAT

Let an agent explain G protein-coupled receptors, their structure, classes and signalling, relay their roles in physiology and drug action from reference sources, and distinguish them from other receptor families.

Thing Registry Physical world and living systems

Research draft, second pass

A second pass drafted this model: the structure a model of this thing needs, and what is known about it in the world. The line under this one says how the second half was obtained - researched against sources, or recalled without web access, in which case nothing here was read anywhere and every claim is a lead to verify. Unreviewed either way.

written by Claude from model knowledge without web access - no source was read, every claim is a lead to verify

Researched by: Claude

Purpose and description

Let an agent explain G protein-coupled receptors, their structure, classes and signalling, relay their roles in physiology and drug action from reference sources, and distinguish them from other receptor families.

A large family of cell surface receptors with seven transmembrane helices that detect molecules outside the cell, from hormones, neurotransmitters and odorants to light and tastants, and activate intracellular G proteins to trigger signalling; G protein-coupled receptors number about 800 in humans, are grouped into classes A to F, and are the targets of roughly a third of approved drugs.

What it is for: Transmitting signals from outside cells to the inside.

It can be explain structure and signalling; classify receptor families; relay roles in physiology and pharmacology; distinguish from other receptor types.

Distinguishing features

Seven transmembrane helices

G protein activation

Largest receptor family

Major drug targets

What it looks like

Not visible; a protein with seven membrane-spanning helices, shown in structural models.

Physical character

human GPCR genes: about 800 count - including olfactory receptors

share of drug targets: about 30-35 percent - of approved drugs

How it is recognised

Seven transmembrane helices coupled to G proteins

Classes A to F by sequence and structure

Ion channel and enzyme-linked receptors are other families

Related models

is a kind of - the category

cell surface receptor

is a kind of - in registry terms

transmembrane signaling receptor

activates - the transducer

G protein

is targeted by - a third of approved medicines

drug

In practice

Families and kinds

class A rhodopsin-like receptors including adrenergic, opioid and olfactory receptors

class B secretin family including glucagon-like peptide-1 and growth hormone-releasing hormone receptors

class C glutamate family

adhesion and frizzled receptors

taste receptors

orphan receptors with unknown ligands

Identifiers

Pfam PF00001 and others 7tm families

IUPHAR GPCR list nomenclature

Standards and regulation

IUPHAR receptor nomenclature

No regulation of the receptors themselves

Failure modes and hazards

Confusing receptor classes

Overstating drug selectivity

Mutations causing disease

Also called

G protein-coupled receptor 98GPCR, family 2, glucagon-like peptide-1/glucagon receptor7TM GPCR, serpentine receptor class a (Sra)taste receptor type 2GPCR, family 2, growth hormone-releasing hormone receptorG-protein coupled receptor 143TSH/LHCG/FSH receptorMethuselah, N-terminal domain superfamilyTaste receptor type 2 member 38Taste receptor type 2 member 4Taste receptor type 2 member 7leukotriene receptorProstanoid receptorG protein-coupled receptor 176, rhodopsin-like, 7TM, protein familyAdhesion G protein-coupled receptor B, N-terminal domain, protein familyGPCR, family 3Gonadotrophin-releasing hormone receptor familyThyrotropin-releasing hormone receptorThyrotropin receptorFormyl peptide receptor 1melatonin receptor familymelanocortin receptorAdhesion G protein-coupled receptorGPCR family 2, extracellular hormone receptor domain superfamilyFrizzled cysteine-rich domain superfamilytachykinin receptoranaphylatoxin receptorsfungal mating pheromone receptorsGPCR, family 3, extracellular calcium-sensing receptor-relatedlysophospholipid receptorG protein-coupled receptor, rhodopsin-likeGPCR, family 2, secretin-likepituitary adenylate cyclase-activating polypeptide receptorsislet amyloid polypeptide receptorsMethuselah, N-terminal domain, protein familyGPCR, family 3, nine cysteines domain, protein familyGPCR family 3, C-terminal domain, protein familyGPCR, family 2, latrophilin, C-terminal domain, protein familyGPCR, family 2, extracellular hormone receptor domain, protein familyGPCR, cAMP-type, protein family

+122

Where this came from

wikidata · CC0 1.0

Source repository Registry entry point

Drafted structure

Bundle to layer to finding to question, as the second pass will find it: 4 bundles · 8 layers · 8 findings · 16 questions.

Structure Structure and signalling.

Science.

Structure

Structure.

Structure

Structure.

  1. What is the structure of a GPCR, and how does ligand binding change it? definition
  2. Is the receptor a GPCR or another receptor family? boundary

Signalling

Signalling.

Signalling

Signalling.

  1. How do GPCRs activate G proteins and arrestins, and how is signalling terminated? definition
  2. Which entry fits G protein? action
Classify Families.

Classification.

Classes

Classes.

Classes

Classes.

  1. What are the GPCR classes, and what receptors belong to each? definition
  2. Which entry fits the specific receptor? action

Nomenclature

Nomenclature.

Nomenclature

Nomenclature.

  1. How are GPCRs named and catalogued? provenance
  2. Which references are standard? provenance
Function Physiology and medicine.

Application.

Physiology

Roles.

Physiology

Physiology.

  1. What roles do GPCRs play in sensing, hormones and neurotransmission? provenance
  2. Which entry fits the specific system? action

Drugs

Drug targets.

Drugs

Drugs.

  1. How do drugs act on GPCRs, and what does biased signalling mean for drug design? provenance
  2. Which entry fits pharmacology? action
Context History and research.

Context.

History

Discovery.

History

History.

  1. How were GPCRs discovered and characterised, including the 2012 Nobel Prize? provenance
  2. Which entry fits the history of molecular biology? action

Research

Research.

Research

Research.

  1. What are current research directions, such as cryo-EM structures and orphan receptors? provenance
  2. Which sources are cited? provenance

What the second pass must settle

  • Should each receptor class be a separate entry?
  • How should nomenclature databases be linked?
  • The registry entry has merged aliases naming individual receptors and families; should they be split off?
Draft as JSON