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.
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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.
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Target identifiers
No target identifier beyond the verified name and aliases is declared in this Phase 1A record.
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Related compounds
Compound
GIP(1-42)
GIP is a 42-residue endogenous incretin hormone and the native ligand of the GIP receptor.
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.
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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
- LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept.current
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
- Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial.current
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
- 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.current
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
- Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial.current
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
- Pharmacology, physiology, and mechanisms of incretin hormone action.current
Campbell JE, Drucker DJ
Cell metabolism · 2013-05-16 · Review
- How May GIP Enhance the Therapeutic Efficacy of GLP-1?current
Samms RJ, Coghlan MP, Sloop KW
Trends in endocrinology and metabolism: TEM · 2020-03-16 · Review
- Structural basis for ligand recognition of incretin receptors.current
Underwood CR, Parthier C, Reedtz-Runge S
Vitamins and hormones · 2010 · Review
- Glucose-dependent insulinotropic polypeptide (GIP).current
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
- Structural determinants of dual incretin receptor agonism by tirzepatide.current
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
- 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.current
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
- Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist.current
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
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Related glossary terms
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