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Research Catalog

Molecular mechanism

Glucose-dependent insulinotropic polypeptide receptor

GIPR is a class B G-protein-coupled receptor. The cited discovery and trial records identify it as one of the three receptor relationships declared for retatrutide.

Type: receptorPublished: 2026-09-04Literature/identifier verification: 2026-08-23

See this target on the receptor map

GIPR

01

Neutral molecular overview

GIPR is a class B G-protein-coupled receptor. The cited discovery and trial records identify it as one of the three receptor relationships declared for retatrutide.

02

Target identifiers

No target identifier beyond the verified name and aliases is listed for this mechanism.

03

Related compounds

Compound

GIP(1-42)

GIP is a 42-residue endogenous incretin hormone and the native ligand of the GIP receptor. Horváth et al. (PMID 37528104) place GIP among the gastrointestinal peptides of the glucagon family.

Compound

Retatrutide

Retatrutide, development code LY3437943, is a single peptide characterized as an agonist at GCGR, GIPR, and GLP-1R in its discovery record.

Compound

Tirzepatide

Tirzepatide is a fatty-acid-modified synthetic peptide characterized in its discovery record as having agonist activity at both the GIP receptor and the GLP-1 receptor.

04

Related mechanisms

receptor

Glucagon-like peptide-1 receptor

GLP-1R is a class B G-protein-coupled receptor. The cited structural and pharmacology records characterize semaglutide and retatrutide as peptide agonists at this receptor.

receptor

Glucagon receptor

GCGR is a class B G-protein-coupled receptor. Retatrutide's LY3437943 discovery record characterizes a molecular agonist relationship at GCGR alongside GIPR and GLP-1R.

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Verified bibliography

  1. Reference 1

    LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept.

    Coskun T, Urva S, Roell WC, Qu H, Loghin C, Moyers JS, O'Farrell LS, Briere DA, Sloop KW, Thomas MK, Pirro V, Wainscott DB, Willard FS, Abernathy M, Morford L, Du Y, Benson C, Gimeno RE, Haupt A, Milicevic Z

    Cell metabolism · 2022-08-18 · Journal Article

    current
    PMID 35985340DOI 10.1016/j.cmet.2022.07.013RetatrutideGLP-1RGIPRGCGR

  2. Reference 2

    Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial.

    Jastreboff AM, Kaplan LM, Frías JP, Wu Q, Du Y, Gurbuz S, Coskun T, Haupt A, Milicevic Z, Hartman ML, Retatrutide Phase 2 Obesity Trial Investigators

    The New England journal of medicine · 2023-06-26 · Clinical Trial, Phase II

    current
    PMID 37366315DOI 10.1056/NEJMoa2301972RetatrutideGLP-1RGIPRGCGR

  3. Reference 3

    Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA.

    Rosenstock J, Frias J, Jastreboff AM, Du Y, Lou J, Gurbuz S, Thomas MK, Hartman ML, Haupt A, Milicevic Z, Coskun T

    Lancet (London, England) · 2023-06-26 · Clinical Trial, Phase II

    current
    PMID 37385280DOI 10.1016/S0140-6736(23)01053-XRetatrutideGLP-1RGIPRGCGR

  4. Reference 4

    Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial.

    Sanyal AJ, Kaplan LM, Frias JP, Brouwers B, Wu Q, Thomas MK, Harris C, Schloot NC, Du Y, Mather KJ, Haupt A, Hartman ML

    Nature medicine · 2024-06-10 · Clinical Trial, Phase II

    current
    PMID 38858523PMC11271400DOI 10.1038/s41591-024-03018-2RetatrutideGLP-1RGIPRGCGR

  5. Reference 5

    Pharmacology, physiology, and mechanisms of incretin hormone action.

    Campbell JE, Drucker DJ

    Cell metabolism · 2013-05-16 · Review

    current
    PMID 23684623DOI 10.1016/j.cmet.2013.04.008TirzepatideSemaglutideRetatrutideExenatideLiraglutideGLP-1RGIPR

  6. Reference 6

    How May GIP Enhance the Therapeutic Efficacy of GLP-1?

    Samms RJ, Coghlan MP, Sloop KW

    Trends in endocrinology and metabolism: TEM · 2020-03-16 · Review

    current
    PMID 32396843DOI 10.1016/j.tem.2020.02.006TirzepatideGIPRGLP-1R

  7. Reference 7

    Structural basis for ligand recognition of incretin receptors.

    Underwood CR, Parthier C, Reedtz-Runge S

    Vitamins and hormones · 2010 · Review

    current
    PMID 21094903DOI 10.1016/B978-0-12-381517-0.00009-6SemaglutideLiraglutideExenatideTirzepatideRetatrutideGLP-1RGIPR

  8. Reference 8

    Glucose-dependent insulinotropic polypeptide (GIP).

    Müller TD, Adriaenssens A, Ahrén B, Blüher M, Birkenfeld AL, Campbell JE, Coghlan MP, D'Alessio D, Deacon CF, DelPrato S, Douros JD, Drucker DJ, Figueredo Burgos NS, Flatt PR, Finan B, Gimeno RE, Gribble FM, Hayes MR, Hölscher C, Holst JJ, Knerr PJ, Knop FK, Kusminski CM, Liskiewicz A, Mabilleau G, Mowery SA, Nauck MA, Novikoff A, Reimann F, Roberts AG, Rosenkilde MM, Samms RJ, Scherer PE, Seeley RJ, Sloop KW, Wolfrum C, Wootten D, DiMarchi RD, Tschöp MH

    Molecular metabolism · 2025-02-28 · Review

    current
    PMID 40024571PMC11931254DOI 10.1016/j.molmet.2025.102118GIPR

  9. Reference 9

    Structural determinants of dual incretin receptor agonism by tirzepatide.

    Sun B, Willard FS, Feng D, Alsina-Fernandez J, Chen Q, Vieth M, Ho JD, Showalter AD, Stutsman C, Ding L, Suter TM, Dunbar JD, Carpenter JW, Mohammed FA, Aihara E, Brown RA, Bueno AB, Emmerson PJ, Moyers JS, Kobilka TS, Coghlan MP, Kobilka BK, Sloop KW

    Proceedings of the National Academy of Sciences of the United States of America · 2022-03-25 · Journal Article

    current
    PMID 35333651PMC9060465DOI 10.1073/pnas.2116506119TirzepatideGIPRGLP-1R

  10. Reference 10

    LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept.

    Coskun T, Sloop KW, Loghin C, Alsina-Fernandez J, Urva S, Bokvist KB, Cui X, Briere DA, Cabrera O, Roell WC, Kuchibhotla U, Moyers JS, Benson CT, Gimeno RE, D'Alessio DA, Haupt A

    Molecular metabolism · 2018-10-03 · Journal Article

    current
    PMID 30473097PMC6308032DOI 10.1016/j.molmet.2018.09.009TirzepatideGIPRGLP-1R

  11. Reference 11

    Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist.

    Willard FS, Douros JD, Gabe MB, Showalter AD, Wainscott DB, Suter TM, Capozzi ME, van der Velden WJ, Stutsman C, Cardona GR, Urva S, Emmerson PJ, Holst JJ, D'Alessio DA, Coghlan MP, Rosenkilde MM, Campbell JE, Sloop KW

    JCI insight · 2020-09-03 · Journal Article

    current
    PMID 32730231PMC7526454DOI 10.1172/jci.insight.140532TirzepatideGIPRGLP-1R

Study models of these references

What kind of experiment each cited paper reports, taken from its abstract unless marked. Not a summary of results.

ReferenceStudy models
Coskun T et al. 2022Study models reported: in vitro; animal (mouse); human participants (interventional) · from the abstract
Jastreboff AM et al. 2023Study models reported: human participants (interventional) · from the abstract
Rosenstock J et al. 2023Study models reported: human participants (interventional) · from the abstract
Sanyal AJ et al. 2024Study models reported: human participants (interventional) · from the abstract
Campbell JE et al. 2013Review article
Samms RJ et al. 2020Review article
Underwood CR et al. 2010Review article
Müller TD et al. 2025Review article
Sun B et al. 2022Study models reported: in vitro · from the abstract
Coskun T et al. 2018Study models reported: in vitro; animal (mouse); human participants (interventional) · from the abstract
Willard FS et al. 2020Study models reported: in vitro · from the full text

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Related glossary terms

AgonistLigandG-protein-coupled receptor

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