Amphetamine-Decreased Progesterone and Estradiol Release in Rat Granulosa Cells: The Regulatory Role of cAMP- and Ca2+-Mediated Signaling Pathways

Chen, Chien Rung; Chen, Chiao Nan; Wang, Paulus S.; Mündel, Toby; Liao, Yi Hung; Tsai, Shau‐Wei

doi:10.3390/biomedicines9050493

Cited by 3 publications

(1 citation statement)

References 57 publications

(102 reference statements)

Supporting

Mentioning

Contrasting

Order By: Relevance

“…7A). [35][36][37] Moreover, in positive and negative feedback regulation pathways, excessive E2 will act on the estrogen receptors in the hypothalamus and thereby downregulate the expression of FSH and LH to maintain the hormone balance. In this study, SCPH increased the expression of Mapk1 in the hypothalamus of normal female mice but failed to affect GnRH expression (Fig.…”

Section: Food and Function Papermentioning

confidence: 99%

The evaluation of sea cucumber (Acaudina leucoprocta) peptide on sex hormone regulation in normal and premature ovarian failure female mice

et al. 2023

View full text Add to dashboard Cite

show abstract

Section: Food and Function Papermentioning

confidence: 99%

The evaluation of sea cucumber (Acaudina leucoprocta) peptide on sex hormone regulation in normal and premature ovarian failure female mice

et al. 2023

View full text Add to dashboard Cite

show abstract

Hormonal and Allosteric Regulation of the Luteinizing Hormone/Chorionic Gonadotropin Receptor

Shpakov

2024

Front. Biosci. (Landmark Ed)

View full text Add to dashboard Cite

Luteinizing hormone (LH) and human chorionic gonadotropin (CG), like follicle-stimulating hormone, are the most important regulators of the reproductive system. They exert their effect on the cell through the LH/CG receptor (LHCGR), which belongs to the family of G protein-coupled receptors. Binding to gonadotropin induces the interaction of LHCGR with various types of heterotrimeric G proteins (Gs, Gq/11, Gi) and β-arrestins, which leads to stimulation (Gs) or inhibition (Gi) of cyclic adenosine monophosphate-dependent cascades, activation of the phospholipase pathway (Gq/11), and also to the formation of signalosomes that mediate the stimulation of mitogen-activated protein kinases (β-arrestins). The efficiency and selectivity of activation of intracellular cascades by different gonadotropins varies, which is due to differences in their interaction with the ligand-binding site of LHCGR. Gonadotropin signaling largely depends on the status of N- and O-glycosylation of LH and CG, on the formation of homo- and heterodimeric receptor complexes, on the cell-specific microenvironment of LHCGR and the presence of autoantibodies to it, and allosteric mechanisms are important in the implementation of these influences, which is due to the multiplicity of allosteric sites in different loci of the LHCGR. The development of low-molecular-weight allosteric regulators of LHCGR with different profiles of pharmacological activity, which can be used in medicine for the correction of reproductive disorders and in assisted reproductive technologies, is promising. These and other issues regarding the hormonal and allosteric regulation of LHCGR are summarized and discussed in this review.

show abstract

Multiple mechanisms of allosteric regulation of the luteninizing hormone receptor

Shpakov,

Derkach

2024

Uspehi fiziologičeskih nauk

View full text Add to dashboard Cite

The regulatory effects of luteinizing hormone (LH) and chorionic gonadotropin (CG) are realized through the activation of the G-protein coupled LH/CG receptor (LH/CG-R). The result of this is the activation of various types of G proteins, which leads to stimulation (Gs) or inhibition (Gi) of the cAMP-dependent pathway and stimulation of calcium signaling (Gq/11, Gi), and the recruitment of β-arrestins, which prevent G protein signaling through receptor internalization and downregulation, but can also activate the mitogen-activated protein kinase cascade. Despite a certain similarity in the effects of LH and CG, there are differences between them both in efficiency and in the pattern of regulation of LH/CG-R. This is a consequence of differences in the affinity of LH and CG to the orthosteric site of the receptor, as well as differences at the level of allosteric regulation of the receptor, which is due to the presence of a C-terminal extension in the β-subunit of CG, including sites for O-glycosylation, and the variability of N-glycosylation of α- and β-subunits of gonadotropins. Moreover, the number of N-glycans, the degree of their branching and charge differ, which leads to different efficiency of activation of intracellular cascades, affecting the physiological response of the reproductive system to gonadotropins. Of great importance is the formation of homodi(oligo)meric complexes of LH/CG-R and its heterocomplexes with the follicle-stimulating hormone receptor, where protomers allosterically influence the efficiency of LH/CG-R activation and the bias of signal transduction. Taking into account the large number of allosteric sites in LH/CG-R, the development of low-molecular allosteric regulators is underway, including agonists based on thieno[2,3-d]-pyrimidine and peptides derived from the cytoplasmic loops of LH/CG-R. These regulators can become prototypes of drugs for correcting the functions of the reproductive system. This review is devoted to the analysis of data on the similarities and differences in the signaling and physiological effects of gonadotropins with LH activity, the role of allosteric mechanisms in this, and the prospects for creating allosteric regulators of LH/CG-R.

show abstract

Amphetamine-Decreased Progesterone and Estradiol Release in Rat Granulosa Cells: The Regulatory Role of cAMP- and Ca2+-Mediated Signaling Pathways

Cited by 3 publications

References 57 publications

The evaluation of sea cucumber (Acaudina leucoprocta) peptide on sex hormone regulation in normal and premature ovarian failure female mice

The evaluation of sea cucumber (Acaudina leucoprocta) peptide on sex hormone regulation in normal and premature ovarian failure female mice

Hormonal and Allosteric Regulation of the Luteinizing Hormone/Chorionic Gonadotropin Receptor

Multiple mechanisms of allosteric regulation of the luteninizing hormone receptor

Contact Info

Product

Resources

About