Cited by 50Diabetes Treatment and ManagementPharmacology and Obesity TreatmentRegulation of Appetite and Obesity

Selection and progression of unimolecular agonists at the GIP, GLP-1, and glucagon receptors as drug candidates

Knerr, Patrick J., Mowery, Stephanie A., Finan, Brian, Perez-Tilve, Diego, Tschöp, Matthias H., DiMarchi, Richard D.·2020·Peptides

Abstract

The continued global growth in the prevalence of obesity coupled with the limited number of efficacious and safe treatment options elevates the importance of innovative pharmaceutical approaches. Combinatorial strategies that harness the metabolic benefits of multiple hormonal mechanisms have emerged at the preclinical and more recently clinical stages of drug development. A priority has been anti-obesity unimolecular peptides that function as balanced, high potency poly-agonists at two or all the cellular receptors for the endocrine hormones glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and glucagon. This report reviews recent progress in this area, with emphasis on what the initial clinical results demonstrate and what remains to be addressed.

Integrity signals

Registry

Crossref · 10.1016/j.peptides.2019.170225

Cites

119 of 119 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

We couldn’t retrieve this paper’s full text, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

  • Differences in in vitro cAMP potencies between human receptors and those of different pre-clinical models, particularly GIPR, can complicate translation of pre-clinical results to a clinical setting.

    “However, differences in in vitro cAMP potencies between human receptors and those of different pre-clinical models, particularly with regard to GIPR, can complicate translation of pre-clinical results to a clinical setting [44].”

Cites

Flagged first, then by citations

3 of the 122 references couldn’t be matched to a known paper.

Cited by

Sorted by citations

Authors
Knerr, P. J., Mowery, S. A., Finan, B., Perez-Tilve, D., Tschöp, M. H., & DiMarchi, R. D.
Affiliations
  • Helmholtz Munich (DE)
  • Indiana University Bloomington (US)
Corresponding author
DiMarchi, Richard D.
Venue
Peptides
Publisher
Elsevier BV
Published
2020-03
Volume
125
Pages
170225
ISSN
0196-9781 (ISSN-L)
OpenAlex
W2989619493
Cited by
49
References
122
Citations by year
2026: 3 · 2025: 5 · 2024: 5 · 2023: 5 · 2022: 11 · 2021: 13 · 2020: 6
FWCI
1.20
Type
journal article
Language
en
Open access
closed
Locations
  • Peptides (publishedVersion)
  • PubMed (publishedVersion)
  • mediaTUM (Technical University of Munich) (submittedVersion)
  • Site cant be reached (submittedVersion)
  • PuSH - Publication Server of Helmholtz Zentrum München (submittedVersion)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Diabetes Treatment and Management
  • Health Sciences › Medicine › Pharmacology › Pharmacology and Obesity Treatment
  • Life Sciences › Neuroscience › Endocrine and Autonomic Systems › Regulation of Appetite and Obesity
Keywords
GLP-1 receptor, glucose-dependent insulinotropic polypeptide receptor, glucagon receptor, obesity treatment, GIP/GLP-1 receptor agonist, peptide agonists
MeSH terms
Animals, Diabetes Mellitus, Type 2, Gastric Inhibitory Polypeptide, Glucagon, Humans, Obesity, Peptide Fragments, Receptors, Gastrointestinal Hormone, Structure-Activity Relationship, Drug Design, Receptors, Glucagon

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review