Potential clinical use of kisspeptin

Prague, Julia K.; Dhillo, Waljit S.

doi:10.1159/000439133

Cited by 26Hypothalamic control of reproductive hormonesNeuropeptides and Animal PhysiologyReproductive Biology and Fertility

Potential clinical use of kisspeptin

Prague, Julia K., Dhillo, Waljit S.·2015·Neuroendocrinology

DOI 10.1159/000439133

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Abstract

Over the last 10 years, kisspeptins--peptide products of varying lengths encoded by the KISS1 gene--have been found to be key regulators of normal reproductive function throughout life in animals and humans. By activating the kisspeptin receptor [previously known as orphan G protein-coupled receptor 54 (GPR54)], they elicit an effect on the central gonadotropin-releasing hormone neurons. Administration of kisspeptin by either the subcutaneous or intravenous route potently stimulates endogenous gonadotropin hormone release in healthy men and women as well as in animals. Kisspeptin also stimulates endogenous release of gonadotropins in subfertile as well as healthy volunteers, and therefore it has potential as a novel therapeutic agent in reproductive disorders. Further human studies have shown that chronic, high-dose administration of kisspeptin causes desensitisation with rapid subsequent suppression of the hypothalamic-pituitary-gonadal axis, and therefore high-dose long-acting analogues may have a clinical role in treating sex hormone-dependent malignancies. By further elucidating the intricacies and mechanisms of the kisspeptin signalling system, and the tissues it acts on during different phases of the reproductive timeline (including during puberty, fertility, pregnancy and menopause), pharmacologic analogues could become clinically useful.

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Kisspeptin has been used in clinical studies to induce ovulation in infertile women.
“For example, kisspeptin has been used in clinical studies to induce ovulation in infertile women.112”
From Pubertal development and regulation (2016) · cites this paper as [112]

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Torricelli, M., Galleri, L., Voltolini, C., Biliotti, G., Florio, P., Bonis, M. D., & Petraglia, F. (2008) · Reproductive Sciences · doi:10.1177/1933719108322442 · Cited by 39 · see citing works
Kisspeptin and Gonadotropin-Releasing Hormone Neuronal Excitability: Molecular Mechanisms Driven by 17β-Estradiol
Rønnekleiv, O. K., Zhang, C., Bosch, M. A., & Kelly, M. J. (2014) · Neuroendocrinology · doi:10.1159/000370311 · Cited by 36 · see citing works
Pharmacologic profiles of investigational kisspeptin/metastin analogues, TAK-448 and TAK-683, in adult male rats in comparison to the GnRH analogue leuprolide
Matsui, H., Masaki, T., Akinaga, Y., Kiba, A., Takatsu, Y., Nakata, D., Tanaka, A., Ban, J., Matsumoto, S.-I., Kumano, S., et al. (2014) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2014.03.058 · Cited by 33 · see citing works
Association of kisspeptin-10 levels with abortus imminens: a preliminary study
Kavvasoglu, S., Özkan, Z. S., Kumbak, B., Şımşek, M., & İlhan, N. (2011) · Archives of Gynecology and Obstetrics · doi:10.1007/s00404-011-2061-0 · Cited by 32 · see citing works
KISS1 expression in human female adipose tissue
Cockwell, H., Wilkinson, D. A., Bouzayen, R., Imran, S. A., Brown, R., & Wilkinson, M. (2012) · Archives of Gynecology and Obstetrics · doi:10.1007/s00404-012-2514-0 · Cited by 32 · see citing works
The Effects of Kisspeptin on Gonadotropin Release in Non-human Mammals
Abbara, A., Ratnasabapathy, R., Jayasena, C. N., & Dhillo, W. S. (2013) · Advances in experimental medicine and biology · doi:10.1007/978-1-4614-6199-9_4 · Cited by 29 · see citing works
Real-Time GnRH Gene Transcription in GnRH Promoter-Driven Luciferase-Expressing Transgenic Mice: Effect of Kisspeptin
Choe, H. K., Chun, S. K., Kim, J., Kim, D., Kim, H.-D., & Kim, K. (2015) · Neuroendocrinology · doi:10.1159/000371805 · Cited by 6 · see citing works

Flagged first, then by citations

Research works printed but not linked: 4

Seminara SB, Messager S, Chatzidaki EE, Thresher RR, Acierno JS, Shagoury JK, Bo- Abbas Y, Kuohung W, Schwinof KM, Hen- drick AG, Zahn D, Dixon J, Kaiser UB, Slau- genhaupt SA, Gusella JF, O'Rahilly S, Carlton MB, Crowley WF Jr, Aparicio SA, Colledge WH: The GPR54 gene as a regulator of pu- berty. N Engl J Med 2003; 349: 1614-1627.
Topaloglu AK, Tello JA, Kotan LD, Ozbek MN, Yilmaz MB, Erdogan S, Gurbuz F, Tem- iz F, Millar RP, Yuksel B: Inactivating KISS1 mutation and hypogonadotropic hypogonad- ism. N Engl J Med 2012; 366: 629-635.
Jayasena CN, Nijher GMK, Chaudhri OB, Murphy KG, Ranger A, Lim A, Patel D, Meh- ta A, Todd C, Ramachandran R, Salem V, Stamp GW, Donaldson M, Ghatei MA, Bloom SR, Dhillo WS: Subcutaneous injec- tion of kisspeptin-54 acutely stimulates go- nadotropin secretion in women with hypo- thalamic amenorrhea, but chronic adminis- tration causes tachyphylaxis. J Clin Endocrinol Metab 2009; 94: 4315-4323.
George JT, Anderson RA, Millar RP: Kiss- peptin-10 stimulation of gonadotropin secre- tion in women is modulated by sex steroid feedback. Hum Reprod 2012; 27: 3552-3559.

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Authors: Prague, J. K., & Dhillo, W. S.
Affiliations: Hammersmith Hospital (GB)
Corresponding author: Dhillo, Waljit S.
ORCID: Prague, Julia K.
Dhillo, Waljit S.
Venue: Neuroendocrinology
Publisher: S. Karger AG
Published: 2015
Volume: 102
Issue: 3
Pages: 238-245
ISSN: 0028-3835 (ISSN-L)
1423-0194
DOI: 10.1159/000439133
OpenAlex: W1107524513
Cited by: 26
References: 70
Citations by year: 2026: 1 · 2025: 1 · 2024: 1 · 2023: 1 · 2022: 3 · 2021: 2 · 2020: 1 · 2019: 2 · 2018: 4 · 2017: 4 · 2016: 3 · 2015: 3
FWCI: 0.71
Type: journal article
Language: en
Open access: closed
Licence: www.karger.com/Services/SiteLicenses (vor)
www.karger.com/Services/SiteLicenses (tdm)
Locations: Neuroendocrinology (publishedVersion)
PubMed (publishedVersion)
Funders: National Institute for Health and Care Research (CDF-2009-02-05, ACF-2012-21-003, RP-2014-05-001)
Topics: Health Sciences › Medicine › Reproductive Medicine › Hypothalamic control of reproductive hormones
Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neuropeptides and Animal Physiology
Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Biology and Fertility
Keywords: kisspeptin, KISS1, kisspeptin receptor, GPR54, GnRH neurons, gonadotropin secretion, hypothalamic-pituitary-gonadal axis, reproductive disorders, puberty, fertility, pregnancy, menopause
MeSH terms: Receptors, Kisspeptin-1, Animals, Female, Humans, Hypothalamus, Infertility, Luteinizing Hormone, Gonadotropin-Releasing Hormone, Male, Neurons, Pituitary Gland, Pregnancy, Pregnancy Complications, Puberty, Reproduction, Sexual Maturation, Receptors, G-Protein-Coupled, Reproductive Physiological Phenomena, Kisspeptins

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