Journal of Evolutionary Biochemistry and Physiology, Journal Year: 2023, Volume and Issue: 59(5), P. 1810 - 1823
Published: Sept. 1, 2023
Language: Английский
International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(7), P. 6187 - 6187
Published: March 24, 2023
Allosteric regulation is critical for the functioning of G protein-coupled receptors (GPCRs) and their signaling pathways. Endogenous allosteric regulators GPCRs are simple ions, various biomolecules, protein components GPCR (G proteins β-arrestins). The stability functional activity complexes also due to multicenter interactions between protomers. complexity effects caused by numerous differing in structure, availability, mechanisms action predetermines multiplicity different topology sites GPCRs. These can be localized extracellular loops; inside transmembrane tunnel its upper lower vestibules; cytoplasmic on outer, membrane-contacting surface domain. They involved basal orthosteric agonist-stimulated receptor activity, biased agonism, GPCR-complex formation, endocytosis. targets a large number synthetic modulators, including those constructed using molecular docking. review devoted principles regulation, topology, endogenous regulators, autoantibodies pepducins. chemokine receptors, proteinase-activated thyroid-stimulating luteinizing hormone beta-adrenergic described more detail.
Language: Английский
Citations
28
Сибирский научный медицинский журнал, Journal Year: 2025, Volume and Issue: 45(1), P. 129 - 138
Published: Feb. 27, 2025
Impaired cardiovascular function in metabolic syndrome (MS) and type 2 diabetes mellitus (T2DM) is not adequately studied, data on changes electrocardiogram (ECG) parameters, including rodent models of MS T2DM, are contradictory ambiguous. Aim the study was to investigate ECG parameters T2DM identify possible correlations between impaired glucose tolerance severity parameters. Material methods. Male Wistar rats were used experiments. induced by a high-fat diet (HFD) for 17 weeks; combination HFD streptozotocin injection (HFD + STZ): 11 weeks followed an continued another 6 weeks. Control animals kept standard diet. Results. The test confirmed development prediabetic level group diabetic HFD+STZ group. found only group: significant (compared control group) increase amplitude area T wave shown. Conclusions. Pronounced abnormalities develop model but model.
Language: Английский
Citations
0
Toxicology and Applied Pharmacology, Journal Year: 2025, Volume and Issue: unknown, P. 117337 - 117337
Published: April 1, 2025
Language: Английский
Citations
0
International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(23), P. 16618 - 16618
Published: Nov. 22, 2023
Gonadotropins, including human chorionic gonadotropin (hCG), are used to induce ovulation, but they have a number of side effects, ovarian hyperstimulation syndrome (OHSS). A possible alternative is allosteric luteinizing hormone (LH)/hCG receptor agonists, the compound TP4/2 we developed, which remains active when administered orally. The aim was study effectiveness (orally, 40 mg/kg) as an ovulation inducer in FSH-stimulated immature female rats, compared with hCG (s.c., 15 IU/rat). stimulated progesterone production and corpus luteum formation; time-dependently increased expression steroidogenic genes (Star, Cyp11a1, Cyp17a1) involved regulation (Adamts-1, Cox-2, Egr-1, Mt-1); content metalloproteinase ADAMTS-1 ovaries. These effects were similar those hCG, although some cases less pronounced. TP4/2, contrast maintained normal LH levels LH/hCG gene, indicating preservation sensitivity LH, did not cause sustained increase vascular endothelial growth factor-A OHSS. Thus, effective that, unlike has lower risk OHSS resistance due its moderate stimulating effect on steroidogenesis.
Language: Английский
Citations
6
Journal of Evolutionary Biochemistry and Physiology, Journal Year: 2023, Volume and Issue: 59(1), P. 57 - 68
Published: Jan. 1, 2023
Language: Английский
Citations
5
Frontiers in Pharmacology, Journal Year: 2024, Volume and Issue: 15
Published: July 11, 2024
Introduction: Propolis has a wide range of biological and pharmacological actions, including antioxidant properties—particularly its phenolic flavonoid constituents—that could potentially protect the reproductive system from oxidative damage. Method: Four groups were allocated 40 male Wistar rats each. The vehicle was given to first group’s normal control negative control. second, third, fourth diabetic (diabetic control) propolis orally at 50 100 mg/kg, respectively, for 8 weeks. Diabetes induced in via injection nicotinamide streptozotocin (STZ). Fasting blood glucose (FBG) insulin levels, homeostatic model assessment resistance (HOMA-IR), semen analysis assessed. In addition, assessments serum hormones, total testosterone (TTST), estradiol (E2), follicle-stimulating hormone luteinizing (LH), prolactin (PRL), measured end study. Tissue testosterone, E2, dihydrotestosterone also evaluated. Serum tissue enzymes, catalase (CAT), superoxide dismutase, glutathione peroxidase activities, examined, malondialdehyde content determined. pancreatic testicular tissues histopathologically proliferating cell nuclear antigen (PCNA) B-cell lymphoma 2 (Bcl-2) immunohistochemically analyzed. Testicular examined DNA integrity using comet assay. Results: Compared STZ-control group, greatly decreased FBG levels improved glycemic status rats. comparison STZ-DC increased number sperm cells percent morphologically viable rats, improving their fertility. restored islets, protected testis stress, hormones blood, especially testosterone. Moreover, high doses demonstrated strong positive response Bcl-2 expression spermatogenic cells. Conclusion: data obtained strongly indicate that STZ causes severe impairments whereas propolis, acting as an antioxidant, protects against adverse effects on testis.
Language: Английский
Citations
1
Doklady Biochemistry and Biophysics, Journal Year: 2022, Volume and Issue: 507(1), P. 345 - 349
Published: Dec. 1, 2022
Language: Английский
Citations
6
Journal of Evolutionary Biochemistry and Physiology, Journal Year: 2023, Volume and Issue: 59(3), P. 904 - 913
Published: May 1, 2023
Language: Английский
Citations
3
Journal of Evolutionary Biochemistry and Physiology, Journal Year: 2023, Volume and Issue: 59(S1), P. S1 - S106
Published: Dec. 1, 2023
Language: Английский
Citations
2
The Journal of Clinical Pharmacology, Journal Year: 2022, Volume and Issue: 62(11), P. 1364 - 1371
Published: May 23, 2022
Males with early-onset androgenic alopecia are characterized by elevated androgen levels. The aim of the present study was to investigate whether presence this condition modulates impact metformin on pituitary hormone production. This compared 2 groups young men prediabetes, matched for age, blood pressure, and insulin sensitivity: 23 subjects male-pattern baldness (group 1) 25 individuals normal hair growth 2). Throughout study, both were treated 6 months. Circulating levels glucose, insulin, glycated hemoglobin, gonadotropins, thyrotropin, prolactin, adrenocorticotropic hormone, insulin-like factor-1 androgens determined at beginning months later. At entry, luteinizing (LH), LH/follicle-stimulating ratio, total testosterone, bioavailable dehydroepiandrosterone sulfate higher in group 1 than 2. effect fasting sensitivity, hemoglobin more pronounced 1. Only 1, reduced LH ratio. Metformin did not affect plasma remaining hormones. In untreated 3, n = 22), glucose homeostasis markers remained similar throughout period. obtained results suggest that gonadotroph secretory function is stronger growth. treatment may protect against development hyperplasia and/or focal testicular changes.
Language: Английский
Citations
3