In vitro and in vivo effects of kisspeptin antagonists p234, p271, p354, and p356 on GPR54 activation.

Albers-Wolthers CHJ, de Gier J, Walen M, van Kooten PJS, Lambalk CB, Leegwater PAJ, Roelen BAJ, Schaefers-Okkens AC, Rutten VPMG, Millar RPM, Kooistra HS

PloS one26 Jun 2017Cited by 23 (Europe PMC)

PMID28650956PMCIDPMC5484485DOI10.1371/journal.pone.0179156PepBankPUB-28650956

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Summary

Kisspeptins (KPs) and their receptor (GPR54 or KiSS1R) play a key-role in regulation of the hypothalamic-pituitary-gonadal axis and are therefore interesting targets for therapeutic interventions in the field of reproductive endocrinology. As dogs show a rapid and robust LH response after the administration of KP10, they can serve as a good animal model for research concerning KP signaling. The aims of the present study were to test the antagonistic properties of KP analogs p234, p271, p354, and p356 in vitro, by determining the intracellular Ca2+ response of CHEM1 cells that stably express human GPR54, and to study the in vivo effects of these peptides on basal plasma LH concentration and the KP10-induced LH response in female dogs. Exposure of the CHEM1 cells to KP-10 resulted in a clear Ca2+ response. P234, p271, p354, and p356 did not prevent or lower the KP10-induced Ca2+ response. Moreover, the in vivo studies in the dogs showed that none of these supposed antagonists lowered the basal plasma LH concentration and none of the peptides lowered the KP10-induced LH response. In conclusion, p234, p271, p354, and p356 had no antagonistic effects in vitro nor any effect on basal and kisspeptin-stimulated plasma LH concentration in female dogs.

CC BYText from Europe PMC. Highlighted sentences are the source of results.

Results from this study3

1 result from studies that gave the peptide. No result from this study comes from people.

01LabIn vitro (cells)Activity measurement
In CHEM1 cells expressing human GPR54, kisspeptin‑10 produced a clear intracellular Ca2+ response.
In plain wordsIn cells carrying the human kisspeptin receptor, kisspeptin‑10 caused a clear calcium response.
Peptide
Kisspeptin-10
Outcome
IncreaseIntracellular Ca2+ response
Study
n: not reported in source
CHEM1 cells stably expressing human GPR54
Outcome group
Receptor activity and mechanism · Pharmacology
Studied dose
Dose not stated
Source sentences
Summary
Exposure of the CHEM1 cells to KP-10 resulted in a clear Ca2+ response.
Show in the study text Report a problemFND-2865095601

Studies that did not test the peptide alone2

In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. These results are not evidence about taking Kisspeptin-10.

02AnimalNot a test of Kisspeptin-10 aloneAnimal study (in vivo)Efficacy outcome
In female dogs, none of the four candidate antagonists lowered the LH response induced by kisspeptin‑10.
In plain wordsIn female dogs, none of four candidate blockers reduced the rise in luteinizing hormone caused by kisspeptin‑10.
Peptide
Kisspeptin-10
Outcome
No significant changeKP10-induced LH response with candidate antagonists
Study
dogn: not reported in source
Female dogs
Outcome group
Sex hormones and fertility · Endocrine and hormones
Source sentences
Summary
none of the peptides lowered the KP10-induced LH response.
1 context sentence(design, population, supporting numbers)
Summary · context
The aims of the present study were to test the antagonistic properties of KP analogs p234, p271, p354, and p356 in vitro, by determining the intracellular Ca2+ response of CHEM1 cells that stably express human GPR54, and to study the in vivo effects of these peptides on basal plasma LH concentration and the KP10-induced LH response in female dogs.
In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Kisspeptin-10.
Show in the study text Report a problemFND-2865095603
03LabNot a test of Kisspeptin-10 aloneIn vitro (cells)Activity measurement
In CHEM1 cells, the analogs p234, p271, p354 and p356 did not prevent or lower the kisspeptin‑10-induced Ca2+ response.
In plain wordsIn cells, four candidate blockers did not stop or reduce the calcium response caused by kisspeptin‑10.
Peptide
Kisspeptin-10
Outcome
No significant changeCandidate antagonists against KP10-induced Ca2+ response
Study
n: not reported in source
CHEM1 cells stably expressing human GPR54
Outcome group
Receptor activity and mechanism · Pharmacology
Source sentences
Summary
P234, p271, p354, and p356 did not prevent or lower the KP10-induced Ca2+ response.
In this study, Kisspeptin-10 was a lab tool or a carrier, part of a mix, or the subject of a lab method. This result is not evidence about taking Kisspeptin-10.
Show in the study text Report a problemFND-2865095602

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Version history

PepBank keeps every version of the data on this study. Status changes from Retraction Watch, Europe PMC and Crossref are listed with their source.

Version 2Current
10 Oct 2026, 09:43 UTC
Study results updated
Version 1
9 Oct 2026, 03:04 UTC
First added · source update from Europe PMC

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