Current and future applications of GnRH, kisspeptin and neurokinin B analogues

Exploring the pathophysiology of hypogonadism in men with type 2 diabetes: Kisspeptin-10 stimulates serum testosterone and LH secretion in men with type 2 diabetes and mild biochemical hypogonadism

(2012) Jyothis T. George et al.   CLINICAL ENDOCRINOLOGY

Direct Regulation of GnRH Neuron Excitability by Arcuate Nucleus POMC and NPY Neuron Neuropeptides in Female Mice

(2012) Juan Roa et al.   ENDOCRINOLOGY

Chronic Administration of the Metastin/Kisspeptin Analog KISS1-305 or the Investigational Agent TAK-448 Suppresses Hypothalamic Pituitary Gonadal Function and Depletes Plasma Testosterone in Adult Male Rats

(2012) Hisanori Matsui et al.   ENDOCRINOLOGY

Uncovering Novel Reproductive Defects in Neurokinin B Receptor Null Mice: Closing the Gap Between Mice and Men

(2012) Jasmine J. Yang et al.   ENDOCRINOLOGY

Kisspeptin-10 stimulation of gonadotrophin secretion in women is modulated by sex steroid feedback

(2012) J. T. George et al.   HUMAN REPRODUCTION

Kisspeptin Restores Pulsatile LH Secretion in Patients with Neurokinin B Signaling Deficiencies: Physiological, Pathophysiological and Therapeutic Implications

(2012) Jacques Young et al.   NEUROENDOCRINOLOGY

InactivatingKISS1Mutation and Hypogonadotropic Hypogonadism

(2012) A. Kemal Topaloglu et al.   NEW ENGLAND JOURNAL OF MEDICINE

Kisspeptins and Reproduction: Physiological Roles and Regulatory Mechanisms

(2012) Leonor Pinilla et al.   PHYSIOLOGICAL REVIEWS

New Insights into the Control of Pulsatile GnRH Release: The Role of Kiss1/Neurokinin B Neurons

(2012) Víctor M. Navarro   Frontiers in Endocrinology

Regulation of NKB Pathways and Their Roles in the Control of Kiss1 Neurons in the Arcuate Nucleus of the Male Mouse

(2011) V. M. Navarro et al.   ENDOCRINOLOGY

Kisspeptin Is Essential for the Full Preovulatory LH Surge and Stimulates GnRH Release from the Isolated Ovine Median Eminence

(2011) Jeremy T. Smith et al.   ENDOCRINOLOGY

Developmental Changes in GnRH Release in Response to Kisspeptin Agonist and Antagonist in Female Rhesus Monkeys (Macaca mulatta): Implication for the Mechanism of Puberty

(2011) Kathryn A. Guerriero et al.   ENDOCRINOLOGY

Kisspeptin-10 Is a Potent Stimulator of LH and Increases Pulse Frequency in Men

(2011) J. T. George et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Discovery of 1-{4-[1-(2,6-Difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a Potent, Orally Active, Non-Peptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

(2011) Kazuhiro Miwa et al.   JOURNAL OF MEDICINAL CHEMISTRY

Frequency-Dependent Recruitment of Fast Amino Acid and Slow Neuropeptide Neurotransmitter Release Controls Gonadotropin-Releasing Hormone Neuron Excitability

(2011) X. Liu et al.   JOURNAL OF NEUROSCIENCE

Neuroendocrine control by kisspeptins: role in metabolic regulation of fertility

(2011) Victor M. Navarro et al.   Nature Reviews Endocrinology

Evidence from the Agonadal Juvenile Male Rhesus Monkey (Macaca mulatta) for the View that the Action of Neurokinin B to Trigger Gonadotropin-Releasing Hormone Release Is Upstream from the Kisspeptin Receptor

(2011) Suresh Ramaswamy et al.   NEUROENDOCRINOLOGY

Is there still a future for neurokinin 3 receptor antagonists as potential drugs for the treatment of psychiatric diseases?

(2011) Guy Griebel et al.   PHARMACOLOGY & THERAPEUTICS

Synthesis and structure–activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54

(2010) Toshitake Kobayashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

2-Acylamino-4,6-diphenylpyridine derivatives as novel GPR54 antagonists with good brain exposure and in vivo efficacy for plasma LH level in male rats

(2010) Toshitake Kobayashi et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Kisspeptin antagonists: Unraveling the role of kisspeptin in reproductive physiology

(2010) Robert P. Millar et al.   BRAIN RESEARCH

Neurokinin B Acts via the Neurokinin-3 Receptor in the Retrochiasmatic Area to Stimulate Luteinizing Hormone Secretion in Sheep

(2010) Heather J. Billings et al.   ENDOCRINOLOGY

Minireview: Kisspeptin/Neurokinin B/Dynorphin (KNDy) Cells of the Arcuate Nucleus: A Central Node in the Control of Gonadotropin-Releasing Hormone Secretion

(2010) Michael N. Lehman et al.   ENDOCRINOLOGY

Evolution of GnRH: Diving deeper

(2010) Graeme J. Roch et al.   GENERAL AND COMPARATIVE ENDOCRINOLOGY

TAC3/TACR3Mutations Reveal Preferential Activation of Gonadotropin-Releasing Hormone Release by Neurokinin B in Neonatal Life Followed by Reversal in Adulthood

(2010) Elena Gianetti et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

TAC3andTACR3Defects Cause Hypothalamic Congenital Hypogonadotropic Hypogonadism in Humans

(2010) Jacques Young et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Leptin’s effect on puberty in mice is relayed by the ventral premammillary nucleus and does not require signaling in Kiss1 neurons

(2010) Jose Donato et al.   JOURNAL OF CLINICAL INVESTIGATION

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

(2010) Y. Wakabayashi et al.   JOURNAL OF NEUROSCIENCE

Hypothesis: Kisspeptin Mediates Male Hypogonadism in Obesity and Type 2 Diabetes

(2010) Jyothis T. George et al.   NEUROENDOCRINOLOGY

Functional Hypothalamic Amenorrhea

(2010) Catherine M. Gordon   NEW ENGLAND JOURNAL OF MEDICINE

Future Prospects for Luteinizing Hormone-Releasing Hormone Analogues in Prostate Cancer Treatment

(2010) Hideyuki Akaza   PHARMACOLOGY

In vitroassessment of metabolic drug–drug interaction potential of AZD2624, neurokinin-3 receptor antagonist, through cytochrome P450enzyme identification, inhibition, and induction studies

(2010) Yan Li et al.   XENOBIOTICA

Kisspeptin Signaling in the Brain

(2009) Amy E. Oakley et al.   ENDOCRINE REVIEWS

Critical Roles of Kisspeptins in Female Puberty and Preovulatory Gonadotropin Surges as Revealed by a Novel Antagonist

(2009) R. Pineda et al.   ENDOCRINOLOGY

Subcutaneous Injection of Kisspeptin-54 Acutely Stimulates Gonadotropin Secretion in Women with Hypothalamic Amenorrhea, But Chronic Administration Causes Tachyphylaxis

(2009) Channa N. Jayasena et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Neurokinin 3 Receptor Immunoreactivity in the Septal Region, Preoptic Area and Hypothalamus of the Female Sheep: Colocalisation in Neurokinin B Cells of the Arcuate Nucleus but not in Gonadotrophin-Releasing Hormone Neurones

(2009) M. Amstalden et al.   JOURNAL OF NEUROENDOCRINOLOGY

Discovery of Potent Kisspeptin Antagonists Delineate Physiological Mechanisms of Gonadotropin Regulation

(2009) A. K. Roseweir et al.   JOURNAL OF NEUROSCIENCE

In Vivo and in Vitro Structure-Activity Relationships and Structural Conformation of Kisspeptin-10-Related Peptides

(2009) E. Gutierrez-Pascual et al.   MOLECULAR PHARMACOLOGY

Kisspeptin Signalling in the Hypothalamic Arcuate Nucleus Regulates GnRH Pulse Generator Frequency in the Rat

(2009) Xiao-Feng Li et al.   PLoS One

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

(2009) Peter Drakakis et al.   Reproductive Biology and Endocrinology

Trafficking of G-protein-coupled receptors to the plasma membrane: insights for pharmacoperone drugs

(2009) P. Michael Conn et al.   TRENDS IN ENDOCRINOLOGY AND METABOLISM

New quinoline NK3 receptor antagonists with CNS activity

(2008) Paul W. Smith et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) Suresh Ramaswamy et al.   ENDOCRINOLOGY

Alterations in Hypothalamic KiSS-1 System in Experimental Diabetes: Early Changes and Functional Consequences

(2008) J. M. Castellano et al.   ENDOCRINOLOGY

Gonadotropin-releasing hormone and ovarian cancer: a functional and mechanistic overview

(2008) Wai-Kin So et al.   FEBS Journal

The role of kisspeptin in the control of gonadotrophin secretion

(2008) A.K. Roseweir et al.   HUMAN REPRODUCTION UPDATE

Suppression of Gonadotropins and Estradiol in Premenopausal Women by Oral Administration of the Nonpeptide Gonadotropin-Releasing Hormone Antagonist Elagolix

(2008) R. Scott Struthers et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Discovery of SodiumR-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (Elagolix), a Potent and Orally Available Nonpeptide Antagonist of the Human Gonadotropin-Releasing Hormone Receptor

(2008) Chen Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

G protein-coupled receptors of the hypothalamic-pituitary-gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands

(2008) Laura H. Heitman et al.   MEDICINAL RESEARCH REVIEWS

TAC3 and TACR3 mutations in familial hypogonadotropic hypogonadism reveal a key role for Neurokinin B in the central control of reproduction

(2008) A Kemal Topaloglu et al.   NATURE GENETICS

Comparison of the effects of peripherally administered kisspeptins

(2008) Jens D. Mikkelsen et al.   REGULATORY PEPTIDES

Mammalian Type I Gonadotropin-Releasing Hormone Receptors Undergo Slow, Constitutive, Agonist-Independent Internalization

(2007) Adam J. Pawson et al.   ENDOCRINOLOGY

Diversity of actions of GnRHs mediated by ligand-induced selective signaling

(2007) Robert P. Millar et al.   FRONTIERS IN NEUROENDOCRINOLOGY

New frontiers in kisspeptin/GPR54 physiology as fundamental gatekeepers of reproductive function

(2007) Juan Roa et al.   FRONTIERS IN NEUROENDOCRINOLOGY