Kisspeptin antagonists: Unraveling the role of kisspeptin in reproductive physiology

Brain Research

Volumn 1364, Issue , 2010, Pages 81-89

  Millar, Robert P ^a   Roseweir, Antonia K ^a   Tello, Javier A ^a   Anderson, Richard A ^a   George, Jyothis T ^a   Morgan, Kevin ^a   Pawson, Adam J ^a  

^a UNIVERSITY OF EDINBURGH   (United Kingdom)

Author keywords

GPR54; Kisspeptin; Reproduction

Indexed keywords

G PROTEIN COUPLED RECEPTOR 54; HORMONE RECEPTOR BLOCKING AGENT; KISSPEPTIN; KISSPEPTIN ANTAGONIST 234; LUTEINIZING HORMONE; SEX HORMONE; UNCLASSIFIED DRUG;

BLOOD BRAIN BARRIER; CELL FUNCTION; GONADECTOMY; GONADORELIN RELEASE; HORMONAL REGULATION; LUTEINIZING HORMONE RELEASE; NEGATIVE FEEDBACK; NERVE CELL; NONHUMAN; OVULATION; PATHOPHYSIOLOGY; PRIORITY JOURNAL; PUBERTY; REPRODUCTION; REVIEW; STRESS;

ANIMALS; BLOOD-BRAIN BARRIER; ELECTROPHYSIOLOGICAL PHENOMENA; FEEDBACK, PHYSIOLOGICAL; FEMALE; GONADOTROPIN-RELEASING HORMONE; HUMANS; MALE; NEURONS; PUBERTY; REPRODUCTION; TUMOR SUPPRESSOR PROTEINS;

PYRONIA TITHONUS;

EID: 78649510825     PISSN: 00068993     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.brainres.2010.09.044     Document Type: Review

References (55)

1. S. Adachi, S. Yamada, Y. Takatsu, H. Matsui, M. Kinoshita, K. Takase, H. Sugiura, T. Ohtaki, H. Matsumoto, Y. Uenoyama, H. Tsukamura, K. Inoue, and K.I. Maeda Involvement of anteroventral periventricular metastin/kisspeptin neurons in estrogen positive feedback action on luteinizing hormone release in female rats J. Reprod. Dev. 53 2007 367 378 (Pubitemid 46743563)
2. J.E. Bowe, A.J. King, J.S. Kinsey-Jones, V.L. Foot, X.F. Li, K.T. O'Byrne, S.J. Persaud, and P.M. Jones Kisspeptin stimulation of insulin secretion: mechanisms of action in mouse islets and rats Diabetologia 52 2009 855 862
3. J.M. Castellano, V.M. Navarro, R. Fernandez-Fernandez, R. Nogueiras, S. Tovar, J. Roa, M.J. Vazquez, E. Vigo, F.F. Casanueva, E. Aguilar, L. Pinilla, C. Dieguez, and M. Tena-Sempere Changes in hypothalamic KiSS-1 system and restoration of pubertal activation of the reproductive axis by kisspeptin in undernutrition Endocrinology 146 2005 3917 3925 (Pubitemid 41175762)
4. J.M. Castellano, V.M. Navarro, J. Roa, R. Pineda, M.A. Sanchez-Garrido, D. Garcia-Galiano, E. Vigo, C. Dieguez, E. Aguilar, L. Pinilla, and M. Tena-Sempere Alterations in hypothalamic KiSS-1 system in experimental diabetes: early changes and functional consequences Endocrinology 150 2009 784 794
5. G. Cheng, L.M. Coolen, V. Padmanabhan, R.L. Goodman, and M.N. Lehman The kisspeptin/neurokinin B/dynorphin (KNDy) cell population of the arcuate nucleus: sex differences and effects of prenatal testosterone in sheep Endocrinology 151 2010 301 311
6. J. Clarkson, and A.E. Herbison Postnatal development of kisspeptin neurons in mouse hypothalamus; sexual dimorphism and projections to gonadotropin-releasing hormone neurons Endocrinology 147 2006 5817 5825 (Pubitemid 44833498)
7. A.C. Dalkin, D.J. Haisenleder, G.A. Ortolano, T.R. Ellis, and J.C. Marshall The frequency of gonadotropin-releasing-hormone stimulation differentially regulates gonadotropin subunit messenger ribonucleic acid expression Endocrinology 125 1989 917 924
8. N. de Roux, E. Genin, J.C. Carel, F. Matsuda, J.L. Chaussain, and E. Milgrom Hypogonadotropic hypogonadism due to loss of function of the KiSS1-derived peptide receptor GPR54 Proc. Natl. Acad. Sci. U. S. A. 100 2003 10972 10976 (Pubitemid 37140137)
9. W.S. Dhillo, O.B. Chaudhri, M. Patterson, E.L. Thompson, K.G. Murphy, M.K. Badman, B.M. McGowan, V. Amber, S. Patel, M.A. Ghatei, and S.R. Bloom Kisspeptin-54 stimulates the hypothalamic-pituitary gonadal axis in human males J. Clin. Endocrinol. Metab. 90 2005 6609 6615 (Pubitemid 41759323)
10. W.S. Dhillo, O.B. Chaudhri, E.L. Thompson, K.G. Murphy, M. Patterson, R. Ramachandran, G.K. Nijher, V. Amber, A. Kokkinos, M. Donaldson, M.A. Ghatei, and S.R. Bloom Kisspeptin-54 stimulates gonadotrophin release most potently during the preovulatory phase of the menstrual cycle in women J. Clin. Endocrinol. Metab. 92 2007 3958 3966 (Pubitemid 47607647)
11. G.J. Dockray The expanding family of RF-amide peptides and their effects on feeding behaviour Exp. Physiol. 89 2004 229 235
12. P. Drakakis, D. Loutradis, A. Beloukas, V. Sypsa, V. Anastasiadou, G. Kalofolias, H. Arabatzi, E. Kiapekou, K. Stefanidis, D. Paraskevis, A. Makrigiannakis, A. Hatzakis, and A. Antsaklis Early hCG addition to rFSH for ovarian stimulation in IVF provides better results and the cDNA copies of the hCG receptor may be an indicator of successful stimulation Reprod. Biol. Endocrinol. 7 2009 110
13. C.I. Durnerin, K. Erb, R. Fleming, H. Hillier, S.G. Hillier, C.M. Howles, J.N. Hugues, A. Lass, H. Lyall, P. Rasmussen, J. Thong, I. Traynor, L. Westergaard, and R. Yates Effects of recombinant LH treatment on folliculogenesis and responsiveness to FSH stimulation Hum. Reprod. 23 2008 421 426 (Pubitemid 351651260)
14. K.M. Estrada, C.M. Clay, S. Pompolo, J.T. Smith, and I.J. Clarke Elevated KiSS-1 expression in the arcuate nucleus prior to the cyclic preovulatory gonadotrophin-releasing hormone/lutenising hormone surge in the ewe suggests a stimulatory role for kisspeptin in oestrogen-positive feedback J. Neuroendocrinol. 18 2006 806 809 (Pubitemid 44340517)
15. R. Fernandez-Fernandez, A.C. Martini, V.M. Navarro, J.M. Castellano, C. Dieguez, E. Aguilar, L. Pinilla, and M. Tena-Sempere Novel signals for the integration of energy balance and reproduction Mol. Cell. Endocrinol. 254-255 2006 127 132 (Pubitemid 44041763)
16. I. Franceschini, D. Lomet, M. Cateau, G. Delsol, Y. Tillet, and A. Caraty Kisspeptin immunoreactive cells of the ovine preoptic area and arcuate nucleus co-express estrogen receptor alpha Neurosci. Lett. 401 2006 225 230 (Pubitemid 43729526)
17. S. Franks Polycystic ovary syndrome N. Eng. J. Med. 333 1995 853 861
18. S. Funes, J.A. Hedrick, G. Vassileva, L. Markowitz, S. Abbondanzo, A. Golovko, S. Yang, F.J. Monsma, and E.L. Gustafson The KiSS-1 receptor GPR54 is essential for the development of the murine reproductive system Biochem. Biophys. Res. Commun. 312 2003 1357 1363 (Pubitemid 37490966)
19. J.T. George, R.A. Anderson, S.B. Seminara, and R.P. Millar Kisspeptin 10 Rapidly and Potently Stimulates LH Secretion in Men ENDO 2010: The 92nd Annual Meeting, San Diego, CA 2010
20. J.T. George, R.P. Millar, and R.A. Anderson Hypothesis: kisspeptin mediates male hypogonadism in obesity and type 2 diabetes Neuroendocrinology 91 2010 302 307
21. R.L. Goodman, M.N. Lehman, J.T. Smith, L.M. Coolen, C.V. de Oliveira, M.R. Jafarzadehshirazi, A. Pereira, J. Iqbal, A. Caraty, P. Ciofi, and I.J. Clarke Kisspeptin neurons in the arcuate nucleus of the ewe express both dynorphin A and neurokinin B Endocrinology 148 2007 5752 5760 (Pubitemid 350146171)
22. S.K. Han, M.L. Gottsch, K.J. Lee, S.M. Popa, J.T. Smith, S.K. Jakawich, D.K. Clifton, R.A. Steiner, and A.E. Herbison Activation of gonadotropin- releasing hormone neurons by kisspeptin as a neuroendocrine switch for the onset of puberty J. Neurosci. 25 2005 11349 11356
23. M.S. Irwig, G.S. Fraley, J.T. Smith, B.V. Acohido, S.M. Popa, M.J. Cunningham, M.L. Gottsch, D.K. Clifton, and R.A. Steiner Kisspeptin activation of gonadotropin releasing hormone neurons and regulation of KiSS-1 mRNA in the male rat Neuroendocrinology 80 2004 264 272
24. M. Kinoshita, H. Tsukamura, S. Adachi, H. Matsui, Y. Uenoyama, K. Iwata, S. Yamada, K. Inoue, T. Ohtaki, H. Matsumoto, and K. Maeda Involvement of central metastin in the regulation of preovulatory luteinizing hormone surge and estrous cyclicity in female rats Endocrinology 146 2005 4431 4436 (Pubitemid 41324041)
25. M. Kotani, M. Detheux, A. Vandenbogaerde, D. Communi, J.M. Vanderwinden, E. Le Poul, S. Brezillon, R. Tyldesley, N. Suarez-Huerta, F. Vandeput, C. Blanpain, S.N. Schiffmann, G. Vassart, and M. Parmentier The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54 J. Biol. Chem. 276 2001 34631 34636 (Pubitemid 37384458)
26. X.F. Li, J.S. Kinsey-Jones, Y. Cheng, Y. Knox, Y. Lin, N.A. Petrou, A.K. Roseweir, S.F. Lightman, S.R. Milligan, R.P. Millar, and K.T. O'Byrne Kisspeptin signalling in the hypothalamic arcuate nucleus regulates GnRH pulse generator frequency PLoS ONE 16 2009 e8334
27. E.J. Mead, J.J. Maguire, R.E. Kuc, and A.P. Davenport Kisspeptins are novel potent vasoconstrictors in humans, with a discrete localization of their receptor GPR54, to atherosclerosis prone vessels Endocrinology 148 2007 140 147
28. S. Messager, E.E. Chatzidaki, D. Ma, A.G. Hendrick, D. Zahn, J. Dixon, R.R. Thresher, I. Malinge, D. Lomet, M.B. Carlton, W.H. Colledge, A. Caraty, and S.A. Aparicio Kisspeptin directly stimulates gonadotropin-releasing hormone release via G protein-coupled receptor 54 Proc. Natl. Acad. Sci. U. S. A. 102 2005 1761 1766 (Pubitemid 40209241)
29. J.D. Mikkelsen, A.H. Bentsen, L. Ansel, V. Simonneaux, and A. Juul Comparison of the effects of peripherally administered kisspeptins Regul. Pept. 152 2009 95 100
30. V.M. Navarro, R. Fernandez-Fernandez, J.M. Castellano, J. Roa, A. Mayen, M.L. Barreiro, F. Gaytan, E. Aguilar, L. Pinilla, C. Dieguez, and M. Tena-Sempere Advanced vaginal opening and precocious activation of the reproductive axis by KiSS-1 peptide, the endogenous ligand of GPR54 J. Physiol. 561 2004 379 386 (Pubitemid 39646528)
31. V.M. Navarro, J.M. Castellano, R. Fernandez-Fernandez, S. Tovar, J. Roa, A. Mayen, M.L. Barreiro, F.F. Casanueva, E. Aguilar, C. Dieguez, L. Pinilla, and M. Tena-Sempere Effects of KiSS-1 peptide, the natural ligand of GPR54, on follicle-stimulating hormone secretion in the rat Endocrinology 146 2005 1689 1697 (Pubitemid 40396875)
32. T. Ohtaki, Y. Shintani, S. Honda, H. Matsumoto, A. Hori, K. Kanehashi, Y. Terao, S. Kumano, Y. Takatsu, Y. Masuda, Y. Ishibashi, T. Watanabe, M. Asada, T. Yamada, M. Suenaga, C. Kitada, S. Usuki, T. Kurokawa, H. Onda, O. Nishimura, and M. Fujino Metastasis suppressor gene KiSS-1 encodes peptide ligand of a G-protein-coupled receptor Nature 411 2001 613 617 (Pubitemid 32531412)
33. J.C. Pallais, Y. Bo-Abbas, N. Pitteloud, W.F. Crowley Jr., and S.B. Seminara Neuroendocrine, gonadal, placental, and obstetric phenotypes in patients with IHH and mutations in the G-protein coupled receptor, GPR54 Mol. Cell. Endocrinol. 254-255 2006 70 77 (Pubitemid 44041755)
34. D. Panidis, D. Rousso, G. Koliakos, A. Kourtis, I. Katsikis, D. Farmakiotis, E. Votsi, and E. Diamanti-Kandarakis Plasma metastin levels are negatively correlated with insulin resistance and free androgens in women with polycystic ovary syndrome Fertil. Steril. 85 2006 1778 1783 (Pubitemid 43816405)
35. R. Pineda, D. Garcia-Galiano, A. Roseweir, M. Romero, M.A. Sanchez-Garrido, F. Ruiz-Pino, K. Morgan, L. Pinilla, R.P. Millar, and M. Tena-Sempere Critical roles of kisspeptins in female puberty and preovulatory gonadotropin surges as revealed by a novel antagonist Endocrinology 151 2010 722 730
36. T.M. Plant, Y. Nakai, P. Belchetz, E. Keogh, and E. Knobil The sites of action of estradiol and phentolamine in the inhibition of the pulsatile, circhoral discharges of LH in the rhesus monkey (Macaca mulatta) Endocrinology 102 1978 1015 1018 (Pubitemid 8317833)
37. T.M. Plant, S. Ramaswamy, and M.J. Dipietro Repetitive activation of hypothalamic G protein-coupled receptor 54 with intravenous pulses of kisspeptin in the juvenile monkey (Macaca mulatta) elicits a sustained train of gonadotropin-releasing hormone discharges Endocrinology 147 2006 1007 1013 (Pubitemid 43113020)
38. S. Pompolo, A. Pereira, K.M. Estrada, and I.J. Clarke Colocalization of kisspeptin and gonadotropin-releasing hormone in the ovine brain Endocrinology 147 2006 804 810 (Pubitemid 43112997)
39. S. Ramaswamy, K.A. Guerriero, R.B. Gibbs, and T.M. Plant Structural interactions between kisspeptin and GnRH neurons in the mediobasal hypothalamus of the male rhesus monkey (Macaca mulatta) as revealed by double immunofluorescence and confocal microscopy Endocrinology 149 2008 4387 4395
40. J. Roa, E. Aguilar, C. Dieguez, L. Pinilla, and M. Tena-Sempere New frontiers in kisspeptin/GPR54 physiology as fundamental gatekeepers of reproductive function Front. Neuroendocrinol. 29 2007 48 69
41. A.K. Roseweir, and R.P. Millar The role of kisspeptin in the control of gonadotrophin secretion Hum. Reprod. Update 15 2009 203 212
42. A.K. Roseweir, A.S. Kauffman, J.T. Smith, K.A. Guerriero, K. Morgan, J. Pielecka-Fortuna, R. Pineda, M.L. Gottsch, M. Tena-Sempere, S.M. Moenter, E. Terasawa, I.J. Clarke, R.A. Steiner, and R.P. Millar Discovery of potent kisspeptin antagonists delineate physiological mechanisms of gonadotropin regulation J. Neurosci. 29 2009 3920 3929
43. S.B. Seminara, S. Messager, E.E. Chatzidaki, R.R. Thresher, J.S. Acierno Jr., J.K. Shagoury, Y. Bo-Abbas, W. Kuohung, K.M. Schwinof, A.G. Hendrick, D. Zahn, J. Dixon, U.B. Kaiser, S.A. Slaugenhaupt, J.F. Gusella, S. O'Rahilly, M.B. Carlton, W.F. Crowley Jr., S.A. Aparicio, and W.H. Colledge The GPR54 gene as a regulator of puberty N. Engl. J. Med. 349 2003 1614 1627 (Pubitemid 37303886)
44. R.K. Semple, J.C. Achermann, J. Ellery, I.S. Farooqi, F.E. Karet, R.G. Stanhope, S. O'Rahilly, and S.A. Aparicio Two novel missense mutations in g protein-coupled receptor 54 in a patient with hypogonadotropic hypogonadism J. Clin. Endocrinol. Metab. 90 2005 1849 1855 (Pubitemid 40464060)
45. M. Shahab, C. Mastronardi, S.B. Seminara, W.F. Crowley, S.R. Ojeda, and T.M. Plant Increased hypothalamic GPR54 signaling: a potential mechanism for initiation of puberty in primates Proc. Natl. Acad. Sci. U. S. A. 102 2005 2129 2134 (Pubitemid 40262023)
46. J.T. Smith, M.J. Cunningham, E.F. Rissman, D.K. Clifton, and R.A. Steiner Regulation of Kiss1 gene expression in the brain of the female mouse Endocrinology 146 2005 3686 3692 (Pubitemid 41175732)
47. J.T. Smith, H.M. Dungan, E.A. Stoll, M.L. Gottsch, R.E. Braun, S.M. Eacker, D.K. Clifton, and R.A. Steiner Differential regulation of KiSS-1 mRNA expression by sex steroids in the brain of the male mouse Endocrinology 146 2005 2976 2984
48. J.T. Smith, B.V. Acohido, D.K. Clifton, and R.A. Steiner KiSS-1 neurones are direct targets for leptin in the ob/ob mouse J. Neuroendocrinol. 18 2006 298 303
49. M.G. Teles, S.D. Bianco, V.N. Brito, E.B. Trarbach, W. Kuohung, S. Xu, S.B. Seminara, B.B. Mendonca, U.B. Kaiser, and A.C. Latronico A GPR54-activating mutation in a patient with central precocious puberty N. Engl. J. Med. 358 2008 709 715 (Pubitemid 351240750)
50. M. Tena-Sempere KiSS-1 and reproduction: focus on its role in the metabolic regulation of fertility Neuroendocrinology 83 2006 275 281 (Pubitemid 44729784)
51. Y. Tenenbaum-Rakover, M. Commenges-Ducos, A. Iovane, C. Aumas, O. Admoni, and N. de Roux Neuroendocrine phenotype analysis in five patients with isolated hypogonadotropic hypogonadism due to a L102P inactivating mutation of GPR54 J. Clin. Endocrinol. Metab. 92 2007 1137 1144 (Pubitemid 46465693)
52. E.L. Thompson, M. Patterson, K.G. Murphy, K.L. Smith, W.S. Dhillo, J.F. Todd, M.A. Ghatei, and S.R. Bloom Central and peripheral administration of kisspeptin-10 stimulates the hypothalamic-pituitary-gonadal axis J. Neuroendocrinol. 16 2004 850 858 (Pubitemid 39489998)
53. S. Tovar, M.J. Vazquez, V.M. Navarro, R. Fernandez-Fernandez, J.M. Castellano, E. Vigo, J. Roa, F.F. Casanueva, E. Aguilar, L. Pinilla, C. Dieguez, and M. Tena-Sempere Effects of single or repeated intravenous administration of kisspeptin upon dynamic LH secretion in conscious male rats Endocrinology 147 2006 2696 2704 (Pubitemid 43764606)
54. Y. Wakabayashi, T. Nakada, K. Murata, S. Ohkura, K. Mogi, V.M. Navarro, D.K. Clifton, Y. Mori, H. Tsukamura, K. Maeda, R.A. Steiner, and H. Okamura Neurokinin B and dynorphin A in kisspeptin neurons of the arcuate nucleus participate in generation of periodic oscillation of neural activity driving pulsatile gonadotropin-releasing hormone secretion in the goat. J. Neurosci. 30 2010 3124 3132
55. A. West, P.J. Vojta, D.R. Welch, and B.E. Weissman Chromosome localization and genomic structure of the KiSS-1 metastasis suppressor gene (KISS1) Genomics 54 1998 145 148 (Pubitemid 28536204)