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[PMID]:28743461
[Au] Autor:Liu XH; Wang ZJ; Jin L; Huang J; Pu DY; Wang DS; Zhang YG
[Ad] Endereço:Key Laboratory of Freshwater Fish Reproduction and Development (Ministry of Education), Key Laboratory of Aquatic Science of Chongqing, Southwest University School of Life Sciences, Chongqing 400715, China.
[Ti] Título:Effects of subchronic exposure to waterborne cadmium on H-P-I axis hormones and related genes in rare minnows (Gobiocypris rarus).
[So] Source:Comp Biochem Physiol C Toxicol Pharmacol;202:1-11, 2017 Nov.
[Is] ISSN:1532-0456
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The H (hypothalamic)-P (pituitary)-I (interrenal) axis is critical in the stress response and other activities of fish. To further investigate cadmium (Cd) toxicity on the H-P-I axis and to identify its potential regulatory genes in fish, the adult female rare minnows (Gobiocypris rarus) were exposed to subchronic (5weeks) levels of waterborne Cd in the present study. This kind of treatment caused dose-dependent decline in fish growth, with significance in the high dose group (100µg/L). Correspondingly, low dose (5-50µg/L) waterborne Cd disrupted the endocrine system of H-P-I axis just at the secretion level, while high dose Cd disrupted both the secretion and synthesis of cortisol and its downstream signals in rare minnows, revealed by the significantly upregulation and positive correlation of corticosteroidogenic genes including MC2R, StAR, CYP11A1, and CYP11B1 in the kidney (including the interrenal tissue) (P<0.05), and the significant alteration of Glcci1, Hsp90AA and Hsp90AB in the hepatopancreas, gill and intestine as well (P<0.05). The expression of Glcci1 was significantly decreased in hepatopancreas, gill and intestine of tested fish following treatment, and its positive correlation with GR (Glucocorticoid receptor) suggested its potential regulation on the cortisol and/or H-P-I axis in fish. The expression of FKBP5 in the intestine was positively and significantly correlated with that of Hsp90AA (P<0.05), and the Hsp90AB transcript in the hepatopancreas was positively correlated with that of Hsp90AA (P<0.05), which indicated that Hsp90AA and Hsp90AB were more likely to serve as cofactors of GR and FKBP5 in response to Cd exposure.
[Mh] Termos MeSH primário: Cloreto de Cádmio/toxicidade
Cyprinidae/fisiologia
Sistema Hipotálamo-Hipofisário/efeitos dos fármacos
Glândula Inter-Renal/efeitos dos fármacos
[Mh] Termos MeSH secundário: Hormônio Adrenocorticotrópico/genética
Hormônio Adrenocorticotrópico/metabolismo
Animais
Cloreto de Cádmio/administração & dosagem
Hormônio Liberador da Corticotropina/genética
Hormônio Liberador da Corticotropina/metabolismo
Esquema de Medicação
Feminino
Regulação da Expressão Gênica/efeitos dos fármacos
Hidrocortisona/genética
Hidrocortisona/metabolismo
Sistema Hipotálamo-Hipofisário/fisiologia
Glândula Inter-Renal/fisiologia
Hormônios Estimuladores de Melanócitos/genética
Hormônios Estimuladores de Melanócitos/metabolismo
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Proteínas de Ligação a Tacrolimo/genética
Proteínas de Ligação a Tacrolimo/metabolismo
Poluentes Químicos da Água/toxicidade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (RNA, Messenger); 0 (Water Pollutants, Chemical); 9002-60-2 (Adrenocorticotropic Hormone); 9002-79-3 (Melanocyte-Stimulating Hormones); 9015-71-8 (Corticotropin-Releasing Hormone); EC 5.2.1.- (Tacrolimus Binding Proteins); J6K4F9V3BA (Cadmium Chloride); WI4X0X7BPJ (Hydrocortisone)
[Em] Mês de entrada:1801
[Cu] Atualização por classe:180109
[Lr] Data última revisão:
180109
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170727
[St] Status:MEDLINE


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[PMID]:28851749
[Au] Autor:Dore R; Levata L; Gachkar S; Jöhren O; Mittag J; Lehnert H; Schulz C
[Ad] Endereço:Department of Internal Medicine ICenter of Brain, Behavior and Metabolism (CBBM), University of Lübeck, Lübeck, Germany.
[Ti] Título:The thermogenic effect of nesfatin-1 requires recruitment of the melanocortin system.
[So] Source:J Endocrinol;235(2):111-122, 2017 Nov.
[Is] ISSN:1479-6805
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:Nesfatin-1 is a bioactive polypeptide expressed both in the brain and peripheral tissues and involved in the control of energy balance by reducing food intake. Central administration of nesfatin-1 significantly increases energy expenditure, as demonstrated by a higher dry heat loss; yet, the mechanisms underlying the thermogenic effect of central nesfatin-1 remain unknown. Therefore, in this study, we sought to investigate whether the increase in energy expenditure induced by nesfatin-1 is mediated by the central melanocortin pathway, which was previously reported to mediate central nesfatin-1´s effects on feeding and numerous other physiological functions. With the application of direct calorimetry, we found that intracerebroventricular nesfatin-1 (25 pmol) treatment increased dry heat loss and that this effect was fully blocked by simultaneous administration of an equimolar dose of the melanocortin 3/4 receptor antagonist, SHU9119. Interestingly, the nesfatin-1-induced increase in dry heat loss was positively correlated with body weight loss. In addition, as assessed with thermal imaging, intracerebroventricular nesfatin-1 (100 pmol) increased interscapular brown adipose tissue (iBAT) as well as tail temperature, suggesting increased heat production in the iBAT and heat dissipation over the tail surface. Finally, nesfatin-1 upregulated pro-opiomelanocortin and melanocortin 3 receptor mRNA expression in the hypothalamus, accompanied by a significant increase in iodothyronine deiodinase 2 and by a nonsignificant increase in uncoupling protein 1 and peroxisome proliferator-activated receptor gamma coactivator-1 alpha mRNA in the iBAT. Overall, we clearly demonstrate that nesfatin-1 requires the activation of the central melanocortin system to increase iBAT thermogenesis and, in turn, overall energy expenditure.
[Mh] Termos MeSH primário: Proteínas de Ligação ao Cálcio/metabolismo
Proteínas de Ligação a DNA/metabolismo
Melanocortinas/metabolismo
Proteínas do Tecido Nervoso/metabolismo
Termogênese/fisiologia
[Mh] Termos MeSH secundário: Animais
Biomarcadores
Proteínas de Ligação ao Cálcio/genética
Proteínas de Ligação a DNA/genética
Orelha
Hipotálamo/metabolismo
Masculino
Hormônios Estimuladores de Melanócitos/farmacologia
Proteínas do Tecido Nervoso/genética
RNA Mensageiro/genética
RNA Mensageiro/metabolismo
Ratos
Ratos Wistar
Receptores de Melanocortina/antagonistas & inibidores
Receptores de Melanocortina/genética
Receptores de Melanocortina/metabolismo
Cauda
Proteína Desacopladora 1/genética
Proteína Desacopladora 1/metabolismo
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 0 (Calcium-Binding Proteins); 0 (DNA-Binding Proteins); 0 (Melanocortins); 0 (Nerve Tissue Proteins); 0 (RNA, Messenger); 0 (Receptors, Melanocortin); 0 (Ucp1 protein, rat); 0 (Uncoupling Protein 1); 0 (nucleobindin); 168482-23-3 (SHU 9119); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170925
[Lr] Data última revisão:
170925
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170831
[St] Status:MEDLINE
[do] DOI:10.1530/JOE-17-0151


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[PMID]:28715181
[Au] Autor:Cai M; Marelli UK; Mertz B; Beck JG; Opperer F; Rechenmacher F; Kessler H; Hruby VJ
[Ad] Endereço:Department of Chemistry and Biochemistry, University of Arizona , Tucson, Arizona 85721, United States.
[Ti] Título:Structural Insights into Selective Ligand-Receptor Interactions Leading to Receptor Inactivation Utilizing Selective Melanocortin 3 Receptor Antagonists.
[So] Source:Biochemistry;56(32):4201-4209, 2017 Aug 15.
[Is] ISSN:1520-4995
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:Systematic N-methylated derivatives of the melanocortin receptor ligand, SHU9119, lead to multiple binding and functional selectivity toward melanocortin receptors. However, the relationship between N-methylation-induced conformational changes in the peptide backbone and side chains and melanocortin receptor selectivity is still unknown. We conducted comprehensive conformational studies in solution of two selective antagonists of the third isoform of the melanocortin receptor (hMC3R), namely, Ac-Nle-c[Asp-NMe-His -d-Nal(2') -NMe-Arg -Trp -Lys]-NH (15) and Ac-Nle-c[Asp-His -d-Nal(2') -NMe-Arg -NMe-Trp -NMe-Lys]-NH (17). It is known that the pharmacophore (His -DNal -Arg -Trp ) of the SHU-9119 peptides occupies a ß II-turn-like region with the turn centered about DNal -Arg . The analogues with hMC3R selectivity showed distinct differences in the spatial arrangement of the Trp side chains. In addition to our NMR studies, we also carried out molecular-level interaction studies of these two peptides at the homology model of hMC3R. Earlier chimeric human melanocortin 3 receptor studies revealed insights regarding the binding and functional sites of hMC3R selectivity. Upon docking of peptides 15 and 17 to the binding pocket of hMC3R, it was revealed that Arg and Trp side chains are involved in a majority of the interactions with the receptor. While Arg forms polar contacts with D154 and D158 of hMC3R, Trp utilizes π-π stacking interactions with F295 and F298, located on the transmembrane domain of hMC3R. It is hypothesized that as the frequency of Trp -hMC3R interactions decrease, antagonistic activity increases. The absence of any interactions of the N-methyl groups with hMC3R suggests that their primary function is to modulate backbone conformations of the ligands.
[Mh] Termos MeSH primário: Hormônios Estimuladores de Melanócitos/química
Simulação de Acoplamento Molecular
Receptor Tipo 3 de Melanocortina/antagonistas & inibidores
Receptor Tipo 3 de Melanocortina/química
[Mh] Termos MeSH secundário: Sítios de Ligação
Seres Humanos
Receptor Tipo 3 de Melanocortina/genética
Receptor Tipo 3 de Melanocortina/metabolismo
Relação Estrutura-Atividade
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Receptor, Melanocortin, Type 3); 168482-23-3 (SHU 9119); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170718
[St] Status:MEDLINE
[do] DOI:10.1021/acs.biochem.7b00407


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[PMID]:28699792
[Au] Autor:Zhou Y; Cai M
[Ad] Endereço:a Department of Chemistry and Biochemistry , University of Arizona , Tucson , AZ USA.
[Ti] Título:Novel approaches to the design of bioavailable melanotropins.
[So] Source:Expert Opin Drug Discov;12(10):1023-1030, 2017 Oct.
[Is] ISSN:1746-045X
[Cp] País de publicação:England
[La] Idioma:eng
[Ab] Resumo:INTRODUCTION: The melanocortin system is a primordial and critical system for survival, involved in a wide variety of physiological functions. It includes melanocortin receptors (MCRs) and melanotropin ligands (MCLs). MCRs are important drug targets that can regulate several key physiological processes. Extensive efforts have been made to develop peptide and peptidomimetics targeting melanocortin receptors including MC1R, MC3R, MC4R and MC5R. Most research is focused on developing potent and selective melanotropins. However, developing bioavailable melanotropins remains challenging. Areas covered: Herein, the authors summarize promising strategies for developing bioavailable MCLs by using cyclized N-methylated melanotropins, and using cyclotide and tetrapeptide as templates. They discuss their unique advantages in oral availability and targeting MCRs in the central nervous system or in peripheral tissues. Finally, they discuss the observed differences in thepharmacology of MCRs between in vitro and in vivo tests. Expert opinion: N-methylated cyclized melanotropins have great potential to become bio- available drugs targeting MCRs in the brain, while MCR-grafted cyclotides tend to target MCRs in peripheral tissue. A better understanding of the biased signaling process is a new challenge and opportunity for the future discovery of bioavailable MCLs.
[Mh] Termos MeSH primário: Desenho de Drogas
Hormônios Estimuladores de Melanócitos/síntese química
Receptores de Melanocortina/metabolismo
[Mh] Termos MeSH secundário: Animais
Disponibilidade Biológica
Ciclotídeos/síntese química
Ciclotídeos/farmacocinética
Ciclotídeos/farmacologia
Seres Humanos
Ligantes
Hormônios Estimuladores de Melanócitos/química
Hormônios Estimuladores de Melanócitos/farmacocinética
Peptídeos/síntese química
Peptídeos/farmacocinética
Peptídeos/farmacologia
Peptidomiméticos/síntese química
Peptidomiméticos/farmacocinética
Peptidomiméticos/farmacologia
Distribuição Tecidual
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Cyclotides); 0 (Ligands); 0 (Peptides); 0 (Peptidomimetics); 0 (Receptors, Melanocortin); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170922
[Lr] Data última revisão:
170922
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170713
[St] Status:MEDLINE
[do] DOI:10.1080/17460441.2017.1351940


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[PMID]:28578648
[Au] Autor:Eberle AN; Rout B; Qi MB; Bigliardi PL
[Ad] Endereço:Department of Biomedicine, University of Basel, Switzerland.
[Ti] Título:Synthetic Peptide Drugs for Targeting Skin Cancer: Malignant Melanoma and Melanotic Lesions.
[So] Source:Curr Med Chem;24(17):1797-1826, 2017.
[Is] ISSN:1875-533X
[Cp] País de publicação:Netherlands
[La] Idioma:eng
[Ab] Resumo:BACKGROUND: Peptides play decisive roles in the skin, ranging from host defense responses to various forms of neuroendocrine regulation of cell and organelle function. Synthetic peptides conjugated to radionuclides or photosensitizers may serve to identify and treat skin tumors and their metastatic forms in other organs of the body. In the introductory part of this review, the role and interplay of the different peptides in the skin are briefly summarized, including their potential application for the management of frequently occurring skin cancers. Special emphasis is given to different targeting options for the treatment of melanoma and melanotic lesions. Radionuclide Targeting: α-Melanocyte-stimulating hormone (α-MSH) is the most prominent peptide for targeting of melanoma tumors via the G protein-coupled melanocortin-1 receptor that is (over-)expressed by melanoma cells and melanocytes. More than 100 different linear and cyclic analogs of α-MSH containing chelators for 111In, 67/68Ga, 64Cu, 90Y, 212Pb, 99mTc, 188Re were synthesized and examined with experimental animals and in a few clinical studies. Linear Ac-Nle-Asp-His-D-Phe-Arg-Trp-Gly-Lys-NH2 (NAP-amide) and Re-cyclized Cys- Cys-Glu-His-D-Phe-Arg-Trp-Cys-Arg-Pro-Val-NH2 (Re[Arg11]CCMSH) containing different chelators at the N- or C-terminus served as lead compounds for peptide drugs with further optimized characteristics. Alternatively, melanoma may be targeted with radiopeptides that bind to melanin granules occurring extracellularly in these tumors. Photosensitizer targeting: A more recent approach is the application of photosensitizers attached to the MSH molecule for targeted photodynamic therapy using LED or coherent laser light that specifically activates the photosensitizer. Experimental studies have demonstrated the feasibility of this approach as a more gentle and convenient alternative compared to radionuclides.
[Mh] Termos MeSH primário: Melanoma/tratamento farmacológico
Peptídeos/uso terapêutico
Neoplasias Cutâneas/tratamento farmacológico
[Mh] Termos MeSH secundário: Animais
Quelantes/química
Seres Humanos
Lactamas/química
Hormônios Estimuladores de Melanócitos/química
Hormônios Estimuladores de Melanócitos/metabolismo
Melanoma/radioterapia
Metais/química
Peptídeos/síntese química
Peptídeos/química
Fármacos Fotossensibilizantes/síntese química
Fármacos Fotossensibilizantes/química
Fármacos Fotossensibilizantes/uso terapêutico
Compostos Radiofarmacêuticos/síntese química
Compostos Radiofarmacêuticos/química
Compostos Radiofarmacêuticos/uso terapêutico
Neoplasias Cutâneas/metabolismo
Neoplasias Cutâneas/patologia
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Chelating Agents); 0 (Lactams); 0 (Metals); 0 (Peptides); 0 (Photosensitizing Agents); 0 (Radiopharmaceuticals); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1709
[Cu] Atualização por classe:170908
[Lr] Data última revisão:
170908
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170606
[St] Status:MEDLINE
[do] DOI:10.2174/0929867324666170605105942


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[PMID]:28438719
[Au] Autor:Shipp SL; Wang G; Cline MA; Gilbert ER
[Ad] Endereço:Department of Animal and Poultry Sciences, Virginia Tech, Blacksburg, VA 24061, United States.
[Ti] Título:Chick subcutaneous and abdominal adipose tissue depots respond differently in lipolytic and adipogenic activity to α-melanocyte stimulating hormone (α-MSH).
[So] Source:Comp Biochem Physiol A Mol Integr Physiol;209:56-64, 2017 Jul.
[Is] ISSN:1531-4332
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:In birds, α-MSH is anorexigenic, but effects on adipose tissue are unknown. Four day-old chicks were intraperitoneally injected with 0 (vehicle), 5, 10, or 50µg of α-MSH and subcutaneous and abdominal adipose tissue collected at 60min for RNA isolation (n=10). Plasma was collected post-euthanasia at 60 and 180min for measuring non-esterified fatty acids (NEFA) and α-MSH (n=10). Relative to the vehicle, food intake was reduced in the 50µg-treated group. Plasma NEFAs were greater in 10µg than vehicle-treated chicks at 3h. Plasma α-MSH was 3.06±0.57ng/ml. In subcutaneous tissue, melanocortin receptor 5 (MC5R) mRNA was increased in 10µg, MC2R and CCAAT-enhancer-binding protein ß (C/EBPß) mRNAs increased in 50µg, peroxisome proliferator-activated receptor γ and C/EBPα decreased in 5, 10 and 50µg, and Ki67 mRNA decreased in 50µg α-MSH-injected chicks, compared to vehicle-injected chicks. In abdominal tissue, adipose triglyceride lipase mRNA was greater in 10µg α-MSH- than vehicle-treated chicks. Cells isolated from abdominal fat that were treated with 10 and 100nM α-MSH for 4h expressed more MC5R and perilipin-1 than control cells (n=6). Cells that received 100nM α-MSH expressed more fatty acid binding protein 4 and comparative gene identification-58 mRNA than control cells. Glycerol-3-phosphate dehydrogenase (G3PDH) activity was greater in cells at 9days post-differentiation that were treated with 1 and 100nM α-MSH for 4h than in control cells (n=3). Results suggest that α-MSH increases lipolysis and reduces adipogenesis in adipose tissue.
[Mh] Termos MeSH primário: Gordura Abdominal/metabolismo
Adipogenia/efeitos dos fármacos
Tecido Adiposo/metabolismo
Galinhas/metabolismo
[Mh] Termos MeSH secundário: Gordura Abdominal/efeitos dos fármacos
Tecido Adiposo/efeitos dos fármacos
Animais
Galinhas/fisiologia
Ingestão de Alimentos
Lipólise/efeitos dos fármacos
Hormônios Estimuladores de Melanócitos/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1708
[Cu] Atualização por classe:170804
[Lr] Data última revisão:
170804
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170426
[St] Status:MEDLINE


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[PMID]:28197776
[Au] Autor:Jiang DN; Li JT; Tao YX; Chen HP; Deng SP; Zhu CH; Li GL
[Ad] Endereço:Key Laboratory of Marine Ecology and Aquaculture Environment of Zhanjiang, Key Laboratory of Aquaculture in South China Sea for Aquatic Economic Animal of Guangdong Higher Education Institutes, Fisheries College, Guangdong Ocean University, Zhanjiang, 524088, China.
[Ti] Título:Effects of melanocortin-4 receptor agonists and antagonists on expression of genes related to reproduction in spotted scat, Scatophagus argus.
[So] Source:J Comp Physiol B;187(4):603-612, 2017 May.
[Is] ISSN:1432-136X
[Cp] País de publicação:Germany
[La] Idioma:eng
[Ab] Resumo:Melanocortin-4 receptor (Mc4r) function related to reproduction in fish has not been extensively investigated. Here, we report on gene expression changes by real-time PCR following treatment with Mc4r agonists and antagonists in the spotted scat (Scatophagus argus). Using in vitro incubated hypothalamus, the Mc4r nonselective agonist NDP-MSH ([Nle , D-Phe ]-α-melanocyte stimulating hormone; 10 M) and selective agonist THIQ (N-[(3R)-1, 2, 3, 4-Tetrahydroisoquinolinium-3-ylcarbonyl]- (1R)-1-(4-chlorobenzyl)-2-[4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl) piperidin-1-yl]-2-oxoethylamine; 10 M) significantly increased the expression of gnrh (Gonadotropin releasing hormone), while the Mc4r nonselective antagonist SHU9119 (Ac-Nle-[Asp-His-DPhe/DNal(2')-Arg-Trp-Lys]-NH2; 10 M) and selective antagonist Ipsen 5i (compound 5i synthesized in Ipsen Research Laboratories; 10 M) significantly inhibited gnrh expression after 3 h of incubation. In incubated pituitary tissue, NDP-MSH and THIQ significantly increased the expression of fshb (Follicle-stimulating hormone beta subunit) and lhb (Luteinizing hormone beta subunit), while SHU9119 and Ipsen 5i significantly decreased fshb and lhb expression after 3 h of incubation. During the in vivo experiment, THIQ (1 mg/kg bw) significantly increased gnrh expression in hypothalamic tissue, as well as the fshb and lhb expression in pituitary tissue 12 h after abdominal injection. Furthermore, Ipsen 5i (1 mg/kg bw) significantly inhibited gnrh expression in hypothalamic tissue, as well as fshb and lhb gene expression in pituitary tissue 12 h after abdominal injection. In summary, Mc4r singling appears to stimulate gnrh expression in the hypothalamus, thereby modulating the synthesis of Fsh and Lh in the pituitary. In addition, Mc4r also appears to directly regulate fshb and lhb levels in the pituitary in spotted scat. Our study suggests that Mc4r, through the hypothalamus and pituitary, participates in reproductive regulation in fish.
[Mh] Termos MeSH primário: Proteínas de Peixes/genética
Perciformes/fisiologia
Receptor Tipo 4 de Melanocortina/agonistas
Receptor Tipo 4 de Melanocortina/antagonistas & inibidores
[Mh] Termos MeSH secundário: Animais
Feminino
Subunidade beta do Hormônio Folículoestimulante/genética
Regulação da Expressão Gênica/efeitos dos fármacos
Hormônio Liberador de Gonadotropina/genética
Hipotálamo/efeitos dos fármacos
Hormônio Luteinizante Subunidade beta/genética
Hormônios Estimuladores de Melanócitos/farmacologia
Técnicas de Cultura de Órgãos/métodos
Receptor Tipo 4 de Melanocortina/genética
Reprodução/efeitos dos fármacos
Reprodução/genética
Tetra-Hidroisoquinolinas/farmacologia
Triazóis/farmacologia
alfa-MSH/análogos & derivados
alfa-MSH/farmacologia
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Fish Proteins); 0 (Follicle Stimulating Hormone, beta Subunit); 0 (Luteinizing Hormone, beta Subunit); 0 (N-(1,2,3,4-tetrahydroisoquinolinium-3-ylcarbonyl)-1-(4-chlorobenzyl)-2-(4-cyclohexyl-4-(1H-1,2,4-triazol-1-ylmethyl)piperidin-1-yl)-2-oxoethylamine); 0 (Receptor, Melanocortin, Type 4); 0 (Tetrahydroisoquinolines); 0 (Triazoles); 168482-23-3 (SHU 9119); 33515-09-2 (Gonadotropin-Releasing Hormone); 581-05-5 (alpha-MSH); 75921-69-6 (MSH, 4-Nle-7-Phe-alpha-); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1707
[Cu] Atualização por classe:170929
[Lr] Data última revisão:
170929
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170216
[St] Status:MEDLINE
[do] DOI:10.1007/s00360-017-1062-0


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[PMID]:28138237
[Au] Autor:Slastnikova TA; Rosenkranz AA; Morozova NB; Vorontsova MS; Petriev VM; Lupanova TN; Ulasov AV; Zalutsky MR; Yakubovskaya RI; Sobolev AS
[Ad] Endereço:Laboratory of Molecular Genetics of Intracellular Transport, Institute of Gene Biology, Russian Academy of Sciences.
[Ti] Título:Preparation, cytotoxicity, and in vivo antitumor efficacy of In-labeled modular nanotransporters.
[So] Source:Int J Nanomedicine;12:395-410, 2017.
[Is] ISSN:1178-2013
[Cp] País de publicação:New Zealand
[La] Idioma:eng
[Ab] Resumo:PURPOSE: Modular nanotransporters (MNTs) are a polyfunctional platform designed to achieve receptor-specific delivery of short-range therapeutics into the cell nucleus by receptor-mediated endocytosis, endosome escape, and targeted nuclear transport. This study evaluated the potential utility of the MNT platform in tandem with Auger electron emitting In for cancer therapy. METHODS: Three MNTs developed to target either melanocortin receptor-1 (MC1R), folate receptor (FR), or epidermal growth factor receptor (EGFR) that are overexpressed on cancer cells were modified with p-SCN-Bn-NOTA and then labeled with In in high specific activity. Cytotoxicity of the In-labeled MNTs was evaluated on cancer cell lines bearing the appropriate receptor target (FR: HeLa, SK-OV-3; EGFR: A431, U87MG.wtEGFR; and MC1R: B16-F1). In vivo micro-single-photon emission computed tomography/computed tomography imaging and antitumor efficacy studies were performed with intratumoral injection of MC1R-targeted In-labeled MNT in B16-F1 melanoma tumor-bearing mice. RESULTS: The three NOTA-MNT conjugates were labeled with a specific activity of 2.7 GBq/mg with nearly 100% yield, allowing use without subsequent purification. The cytotoxicity of In delivered by these MNTs was greatly enhanced on receptor-expressing cancer cells compared with In nontargeted control. In mice with B16-F1 tumors, prolonged retention of In by serial imaging and significant tumor growth delay (82% growth inhibition) were found. CONCLUSION: The specific in vitro cytotoxicity, prolonged tumor retention, and therapeutic efficacy of MC1R-targeted In-NOTA-MNT suggest that this Auger electron emitting conjugate warrants further evaluation as a locally delivered radiotherapeutic, such as for ocular melanoma brachytherapy. Moreover, the high cytotoxicity observed with FR- and EGFR-targeted In-NOTA-MNT suggests further applications of the MNT delivery strategy should be explored.
[Mh] Termos MeSH primário: Antineoplásicos/farmacologia
Radioisótopos de Índio/química
Nanopartículas/química
[Mh] Termos MeSH secundário: Animais
Autorradiografia
Morte Celular/efeitos dos fármacos
Linhagem Celular Tumoral
Eletroforese em Gel de Poliacrilamida
Feminino
Receptores de Folato com Âncoras de GPI/metabolismo
Seres Humanos
Hormônios Estimuladores de Melanócitos/farmacologia
Melanoma Experimental/patologia
Camundongos Endogâmicos C57BL
Receptor do Fator de Crescimento Epidérmico/metabolismo
Receptores de Melanocortina/metabolismo
Tomografia Computadorizada de Emissão de Fóton Único
Tomografia Computadorizada por Raios X
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Antineoplastic Agents); 0 (Folate Receptors, GPI-Anchored); 0 (Indium Radioisotopes); 0 (Receptors, Melanocortin); 9002-79-3 (Melanocyte-Stimulating Hormones); EC 2.7.10.1 (Receptor, Epidermal Growth Factor)
[Em] Mês de entrada:1703
[Cu] Atualização por classe:170817
[Lr] Data última revisão:
170817
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:170201
[St] Status:MEDLINE
[do] DOI:10.2147/IJN.S125359


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[PMID]:27568547
[Au] Autor:Kühnen P; Handke D; Waterland RA; Hennig BJ; Silver M; Fulford AJ; Dominguez-Salas P; Moore SE; Prentice AM; Spranger J; Hinney A; Hebebrand J; Heppner FL; Walzer L; Grötzinger C; Gromoll J; Wiegand S; Grüters A; Krude H
[Ad] Endereço:Institute for Experimental Pediatric Endocrinology, Charité Universitätsmedizin Berlin, 13353 Berlin, Germany. Electronic address: peter.kuehnen@charite.de.
[Ti] Título:Interindividual Variation in DNA Methylation at a Putative POMC Metastable Epiallele Is Associated with Obesity.
[So] Source:Cell Metab;24(3):502-509, 2016 Sep 13.
[Is] ISSN:1932-7420
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:The estimated heritability of human BMI is close to 75%, but identified genetic variants explain only a small fraction of interindividual body-weight variation. Inherited epigenetic variants identified in mouse models named "metastable epialleles" could in principle explain this "missing heritability." We provide evidence that methylation in a variably methylated region (VMR) in the pro-opiomelanocortin gene (POMC), particularly in postmortem human laser-microdissected melanocyte-stimulating hormone (MSH)-positive neurons, is strongly associated with individual BMI. Using cohorts from different ethnic backgrounds, including a Gambian cohort, we found evidence suggesting that methylation of the POMC VMR is established in the early embryo and that offspring methylation correlates with the paternal somatic methylation pattern. Furthermore, it is associated with levels of maternal one-carbon metabolites at conception and stable during postnatal life. Together, these data suggest that the POMC VMR may be a human metastable epiallele that influences body-weight regulation.
[Mh] Termos MeSH primário: Alelos
Metilação de DNA/genética
Obesidade/genética
Pró-Opiomelanocortina/genética
[Mh] Termos MeSH secundário: Adulto
Biomarcadores/sangue
Peso Corporal
Carbono/metabolismo
Estudos de Coortes
Ilhas de CpG/genética
Feminino
Variação Genética
Seres Humanos
Leucócitos Mononucleares/metabolismo
Masculino
Hormônios Estimuladores de Melanócitos/metabolismo
Meia-Idade
Obesidade/sangue
Gravidez
Análise de Sequência de DNA
[Pt] Tipo de publicação:JOURNAL ARTICLE
[Nm] Nome de substância:
0 (Biomarkers); 66796-54-1 (Pro-Opiomelanocortin); 7440-44-0 (Carbon); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1706
[Cu] Atualização por classe:171024
[Lr] Data última revisão:
171024
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160830
[St] Status:MEDLINE


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[PMID]:27561155
[Au] Autor:Cai M; Hruby VJ
[Ad] Endereço:Department of Chemistry & Biochemistry, University of Arizona, 1306 E University Blvd, Tucson, AZ, 85721.
[Ti] Título:Design of cyclized selective melanotropins.
[So] Source:Biopolymers;106(6):876-883, 2016 Nov.
[Is] ISSN:1097-0282
[Cp] País de publicação:United States
[La] Idioma:eng
[Ab] Resumo:This article describes the development of cyclic peptides for G-protein coupled receptors to enable structure-function knowledge and the design of novel therapeutics. One important property of cyclic peptides is that they tend to be resistant to the digestion, enabling them to survive in the human digestive tract. This trait makes them very important as drug leads or as scaffolds which, in theory, can be engineered to incorporate a peptide domain of medicinal value. This is especially important for delivery of peptides that would be destroyed without such implementation. The melanocortin system is the focus of this article, and includes melanotropin ligands and melanocortin receptors. We examine two strategies to constrain the melanotropin peptide backbone. The first is based on global constraint of peptides by cyclization using various kinds of linkers. In the second approach we describe the use of a natural cyclized template, the cyclotide, to graft the melanotropin phamacophore, -His-Phe-Arg-Trp-, to obtain selective drug leads. In these examples the conserved melanocyte stimulating hormone pharmacophore is examined and the modified peptides were synthesized by solid phase methodology. Biological studies confirmed the production of selective, potent and in some cases orally available ligands.
[Mh] Termos MeSH primário: Ciclotídeos/química
Ciclotídeos/síntese química
Hormônios Estimuladores de Melanócitos/química
Hormônios Estimuladores de Melanócitos/síntese química
[Mh] Termos MeSH secundário: Animais
Seres Humanos
[Pt] Tipo de publicação:JOURNAL ARTICLE; REVIEW
[Nm] Nome de substância:
0 (Cyclotides); 9002-79-3 (Melanocyte-Stimulating Hormones)
[Em] Mês de entrada:1702
[Cu] Atualização por classe:171101
[Lr] Data última revisão:
171101
[Sb] Subgrupo de revista:IM
[Da] Data de entrada para processamento:160826
[St] Status:MEDLINE
[do] DOI:10.1002/bip.22976



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