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1. Prenatal expression of D-aspartate oxidase causes early cerebral D-aspartate depletion and influences brain morphology and cognitive functions at adulthood

Author:
De Rosa, Arianna; Mastrostefano, Francesca; Di Maio, Anna; Nuzzo, Tommaso; Saitoh, Yasuaki; Katane, Masumi; Isidori, Andrea M.; Caputo, Viviana; Marotta, Pina; Falco, Geppino; De Stefano, Maria Egle; Homma, Hiroshi; Usiello, Alessandro; Errico, Francesco
Source:
Amino acids 2020 v.52 no.4 pp. 597-617
ISSN:
0939-4451
Subject:
D-aspartate oxidase; adulthood; agonists; amino acids; animal models; cognition; interneurons; memory; metabolism; mice; neurodevelopment; prefrontal cortex; receptors
Abstract:
... The free D-amino acid, D-aspartate, is abundant in the embryonic brain but significantly decreases after birth. Besides its intracellular occurrence, D-aspartate is also present at extracellular level and acts as an endogenous agonist for NMDA and mGlu5 receptors. These findings suggest that D-aspartate is a candidate signaling molecule involved in neural development, influencing brain morphology ...
DOI:
10.1007/s00726-020-02839-y

2. Central, but not systemic, thermoregulatory effects of leptin are impaired in rats with obesity: interactions with GABAB agonist and antagonist

Author:
Hristov, Milen; Landzhov, Boycho; Nikolov, Rumen; Yakimova, Krassimira
Source:
Amino acids 2019 v.51 no.7 pp. 1055-1063
ISSN:
0939-4451
Subject:
agonists; animal disease models; antagonists; appetite; body temperature; energy expenditure; food intake; heat production; immunohistochemistry; leptin; neurons; obesity; obesity-related diseases; pathogenesis; preoptic area; rats; transactivators; weight loss
Abstract:
... Leptin is an adipokine that regulates body weight by decreasing appetite and increasing energy expenditure. Besides the effects on food intake, leptin can regulate energy expenditure at least in part by modulating thermogenesis. Many of the effects of leptin are attributable to action in the central nervous system, particularly in the hypothalamus. Common forms of obesity are associated with incre ...
DOI:
10.1007/s00726-019-02746-x

3. Functionality of an absolutely conserved glycine residue in the chimeric relaxin family peptide R3/I5

Author:
Wang, Jia-Hui; Shao, Xiao-Xia; Hu, Meng-Jun; Liu, Ya-Li; Xu, Zeng-Guang; Guo, Zhan-Yun
Source:
Amino acids 2019 v.51 no.4 pp. 619-626
ISSN:
0939-4451
Subject:
agonists; cysteine; insulin; mutagenesis; peptides; receptors; relaxin
Abstract:
... The insulin superfamily is a group of homologous proteins that are further divided into the insulin family and relaxin family according to their distinct receptors. All insulin superfamily members contain three absolutely conserved disulfide linkages and a nonchiral Gly residue immediately following the first B-chain cysteine. The functionality of this conserved Gly residue in the insulin family h ...
DOI:
10.1007/s00726-018-02694-y

4. Novel Fubinaca/Rimonabant hybrids as endocannabinoid system modulators

Author:
Stefanucci, Azzurra; Macedonio, Giorgia; Dvorácskó, Szabolcs; Tömböly, Csaba; Mollica, Adriano
Source:
Amino acids 2018 v.50 no.11 pp. 1595-1605
ISSN:
0939-4451
Subject:
agonists; amino acids; analgesics; anti-obesity agents; bioactive properties; cannabinoid receptors; cannabinoids; carboxylic acids; hydrophobicity; radionuclides; sulfur
Abstract:
... The discovery of novel modulators of the cannabinoid system is a current topic in medicinal chemistry. In this paper, we report nine novel carboxamides designed as hybrids of Fubinaca family compounds and Rimonabant. These hybrids were obtained by linking the 1-benzyl-2,5-dichloroindazole-3-carboxylic acid to different amino acids bearing a hydrophobic side chain and three different C-terminus. Th ...
DOI:
10.1007/s00726-018-2636-1

5. Development of a novel ligand binding assay for relaxin family peptide receptor 3 and 4 using NanoLuc complementation

Author:
Hu, Meng-Jun; Shao, Xiao-Xia; Li, Hao-Zheng; Nie, Wei-Han; Wang, Jia-Hui; Liu, Ya-Li; Xu, Zeng-Guang; Guo, Zhan-Yun
Source:
Amino acids 2018 v.50 no.8 pp. 1111-1119
ISSN:
0939-4451
Subject:
G-protein coupled receptors; agonists; automation; bioluminescence; humans; ligands; peptide receptors; peptides; plasma membrane; relaxin; sortase A; washing
Abstract:
... Relaxin family peptides perform a variety of biological functions by binding and activating relaxin family peptide receptor 1–4 (RXFP1–4), four A-class G protein-coupled receptors. In the present work, we developed a novel ligand binding assay for RXFP3 and RXFP4 based on NanoLuc complementation technology (NanoBiT). A synthetic ligation version of the low-affinity small complementation tag (SmBiT ...
DOI:
10.1007/s00726-018-2588-5

6. A novel BRET-based binding assay for interaction studies of relaxin family peptide receptor 3 with its ligands

Author:
Wang, Jia-Hui; Shao, Xiao-Xia; Hu, Meng-Jun; Wei, Dian; Liu, Ya-Li; Xu, Zeng-Guang; Guo, Zhan-Yun
Source:
Amino acids 2017 v.49 no.5 pp. 895-903
ISSN:
0939-4451
Subject:
Escherichia coli; G-protein coupled receptors; agonists; binding capacity; bioluminescence; chimerism; cysteine; dissociation; energy transfer; fluorescent proteins; food intake; humans; ligands; peptide receptors; relaxin; stress response
Abstract:
... Relaxin family peptide receptor 3 (RXFP3) is an A-class G protein-coupled receptor that is implicated in the regulation of food intake and stress response upon activation by its cognate agonist relaxin-3. To study its interaction with various ligands, we developed a novel bioluminescence resonance energy transfer (BRET)-based binding assay using the brightest NanoLuc as an energy donor and a newly ...
DOI:
10.1007/s00726-017-2387-4

7. D-Aspartate drinking solution alleviates pain and cognitive impairment in neuropathic mice

Author:
Palazzo, Enza; Luongo, Livio; Guida, Francesca; Marabese, Ida; Romano, Rosaria; Iannotta, Monica; Rossi, Francesca; D’Aniello, Antimo; Stella, Luigi; Marmo, Federica; Usiello, Alessandro; de Bartolomeis, Andrea; Maione, Sabatino; de Novellis, Vito
Source:
Amino acids 2016 v.48 no.7 pp. 1553-1567
ISSN:
0939-4451
Subject:
agonists; antidepressants; anxiety; ataxia (disorder); brain; cognition; cortex; drinking; glutamic acid; humans; mice; models; nerve tissue; pain; receptors; surgery
Abstract:
... D-Aspartate (D-Asp) is a free D-amino acid detected in multiple brain regions and putative precursor of endogenous N-methyl-D-aspartate (NMDA) acting as agonist at NMDA receptors. In this study, we investigated whether D-Asp (20 mM) in drinking solution for 1 month affects pain responses and pain-related emotional, and cognitive behaviour in a model of neuropathic pain induced by the spared nerve ...
DOI:
10.1007/s00726-016-2205-4

8. 6-(4-Amino-2-butyl-imidazoquinolyl)-norleucine: Toll-like receptor 7 and 8 agonist amino acid for self-adjuvanting peptide vaccine

Author:
Fujita, Yoshio; Hirai, Kazuyuki; Nishida, Keigo; Taguchi, Hiroaki
Source:
Amino acids 2016 v.48 no.5 pp. 1319-1329
ISSN:
0939-4451
Subject:
Influenza A virus; Toll-like receptor 7; Toll-like receptor 8; agonists; amino acids; antibodies; antigens; ligands; mice; peptides; pharmacology; subunit vaccines; vaccine adjuvants
Abstract:
... Generally, small peptides by themselves are weak to induce antibody responses. Toll-like receptor (TLR) ligands are attractive candidates of vaccine adjuvants to improve their antigenicity. The covalent conjugation of TLR ligands with antigens to produce self-adjuvanting peptide vaccine is a promising approach. Based on the structure of TLR7/8 ligands, a series of synthetic amino acids 6-imidazoqu ...
DOI:
10.1007/s00726-016-2190-7

9. The interaction of central nitrergic and GABAergic systems on food intake in neonatal layer-type chicks

Author:
Mokhtarpouriani, Kasra; Zendehdel, Morteza; Jonaidi, Hossein; Babapour, Vahab; Shayan, Parviz
Source:
Amino acids 2016 v.48 no.5 pp. 1275-1283
ISSN:
0939-4451
Subject:
agonists; antagonists; arginine; chicks; food intake; gamma-aminobutyric acid; nitric oxide; paraventricular hypothalamic nucleus; receptors
Abstract:
... Most physiological behaviors such as food intake are controlled by the hypothalamus and its nuclei. It has been demonstrated that injection of the paraventricular nucleus of the hypothalamus with nitric oxide (NO) donors elicited changes in the concentration of some amino acids, including GABA. Also, central nitrergic and GABAergic systems are known to provide inputs to the paraventricular nucleus ...
DOI:
10.1007/s00726-016-2178-3

10. Application of the novel bioluminescent ligand–receptor binding assay to relaxin-RXFP1 system for interaction studies

Author:
Wu, Qing-Ping; Zhang, Lei; Shao, Xiao-Xia; Wang, Jia-Hui; Gao, Yu; Xu, Zeng-Guang; Liu, Ya-Li; Guo, Zhan-Yun
Source:
Amino acids 2016 v.48 no.4 pp. 1099-1107
ISSN:
0939-4451
Subject:
crosslinking; screening; Komagataella pastoris; humans; antagonists; G-protein coupled receptors; ligands; bioluminescence; peptide hormones; relaxin; agonists; binding capacity; cysteine
Abstract:
... Relaxin is a prototype of the relaxin family peptide hormones and plays important biological functions by binding and activating the G protein-coupled receptor RXFP1. To study their interactions, in the present work, we applied the newly developed bioluminescent ligand–receptor binding assay to the relaxin-RXFP1 system. First, a fully active easily labeled relaxin, in which three Lys residues of h ...
DOI:
10.1007/s00726-015-2146-3

11. Activation of 5-HT2A/C receptor reduces glycine receptor-mediated currents in cultured auditory cortical neurons

Author:
Luo, Bin; Hu, Lingli; Liu, Chunhua; Guo, Yiping; Wang, Haitao
Source:
Amino acids 2016 v.48 no.2 pp. 349-356
ISSN:
0939-4451
Subject:
agonists; antagonists; cerebral cortex; drugs; ion channels; nervous system diseases; neurons; receptors; serotonin
Abstract:
... Glycine receptors (GlyRs) permeable to chloride only mediate tonic inhibition in the cerebral cortex where glycinergic projection is completely absent. The functional modulation of GlyRs was largely studied in subcortical brain regions with glycinergic transmissions, but the function of cortical GlyRs was rarely addressed. Serotonin could broadly modulate many ion channels through activating 5-HT₂ ...
DOI:
10.1007/s00726-015-2086-y

12. The modulation of NMDA receptors and L-arginine/nitric oxide pathway is implicated in the anti-immobility effect of creatine in the tail suspension test

Author:
Cunha, Mauricio P.; Pazini, Francis L.; Ludka, Fabiana K.; Rosa, Julia M.; Oliveira, Ágatha; Budni, Josiane; Ramos-Hryb, Ana B.; Lieberknecht, Vicente; Bettio, Luis E. B.; Martín-de-Saavedra, Maria D.; López, Manuela G.; Tasca, Carla I.; Rodrigues, Ana Lúcia S.
Source:
Amino acids 2015 v.47 no.4 pp. 795-811
ISSN:
0939-4451
Subject:
agonists; antagonists; antidepressants; arginine; creatine; ketamine; mice; nervous system diseases; neuronal nitric oxide synthase; neuroprotective effect; nitric oxide; polyamines; receptors; tail; viability
Abstract:
... The modulation of N-methyl-D-aspartate receptor (NMDAR) and L-arginine/nitric oxide (NO) pathway is a therapeutic strategy for treating depression and neurologic disorders that involves excitotoxicity. Literature data have reported that creatine exhibits antidepressant and neuroprotective effects, but the implication of NMDAR and L-arginine/nitric oxide (NO) pathway in these effects is not establi ...
DOI:
10.1007/s00726-014-1910-0

13. Modulation of GABA-A receptors of astrocytes and STC-1 cells by taurine structural analogs

Author:
Reyes-Haro, Daniel; Cabrera-Ruíz, Elizabeth; Estrada-Mondragón, Argel; Miledi, Ricardo; Martínez-Torres, Ataúlfo
Source:
Amino acids 2014 v.46 no.11 pp. 2587-2593
ISSN:
0939-4451
Subject:
agonists; astrocytes; chloride channels; chlorides; electrophysiology; gamma-aminobutyric acid; receptors; taurine
Abstract:
... Taurine activates and modulates GABA receptors in vivo as well as those expressed in heterologous systems. This study aimed to determine whether the structural analogs of taurine: homotaurine and hypotaurine, have the ability to activate GABA-A receptors that include GABAρ subunits. The expression of GABA-A receptors containing GABAρ has been reported in the STC-1 cells and astrocytes. In both cel ...
DOI:
10.1007/s00726-014-1813-0

14. Glycine modulates membrane potential, cell volume, and phagocytosis in murine microglia

Author:
Komm, Barbara; Beyreis, Marlena; Kittl, Michael; Jakab, Martin; Ritter, Markus; Kerschbaum, Hubert H.
Source:
Amino acids 2014 v.46 no.8 pp. 1907-1917
ISSN:
0939-4451
Subject:
agonists; amino acid transporters; antagonists; choline; glycine (amino acid); isobutyric acid; membrane potential; mice; neuroglia; phagocytes; phagocytosis; polystyrenes; pseudopodia; reverse transcriptase polymerase chain reaction; scanning electron microscopy; strychnine; taurine
Abstract:
... Phagocytes form engulfment pseudopodia at the contact area with their target particle by a process resembling cell volume (CV) regulatory mechanisms. We evaluated whether the osmoregulatory active neutral amino acid glycine, which contributes to CV regulation via activation of sodium-dependent neutral amino acid transporters (SNATs) improves phagocytosis in isotonic and hypertonic conditions in th ...
DOI:
10.1007/s00726-014-1745-8

15. Acylated and unacylated ghrelin protect MC3T3-E1 cells against tert-butyl hydroperoxide-induced oxidative injury: pharmacological characterization of ghrelin receptor and possible epigenetic involvement

Author:
Dieci, Elisa; Casati, Lavinia; Pagani, Francesca; Celotti, Fabio; Sibilia, Valeria
Source:
Amino acids 2014 v.46 no.7 pp. 1715-1725
ISSN:
0939-4451
Subject:
actin; agonists; antagonists; apoptosis; binding sites; cultured cells; cytoskeleton; cytotoxicity; epigenetics; genes; ghrelin; ghrelin receptors; histones; osteoblasts; osteoporosis; oxidative stress; reactive oxygen species; viability
Abstract:
... Increasing evidence suggests a role for oxidative stress in age-related decrease in osteoblast number and function leading to the development of osteoporosis. This study was undertaken to investigate whether ghrelin, previously reported to stimulate osteoblast proliferation, counteracts tert-butyl hydroperoxide (t-BHP)-induced oxidative damage in MC3T3-E1 osteoblastic cells as well as to character ...
DOI:
10.1007/s00726-014-1734-y

16. A new 68Ga-labeled BBN peptide with a hydrophilic linker for GRPR-targeted tumor imaging

Author:
Pan, Donghui; Xu, Yu Ping; Yang, Rong Hua; Wang, Lizhen; Chen, Fei; Luo, Shineng; Yang, Min; Yan, Yongjun
Source:
Amino acids 2014 v.46 no.6 pp. 1481-1489
ISSN:
0939-4451
Subject:
agonists; amino acids; antagonists; binding capacity; bombesin; excretion; gastrin-releasing peptide; humans; hydrophilicity; image analysis; intestines; liver; liver neoplasms; models; peptide receptors; pharmacokinetics; positron-emission tomography; prostatic neoplasms; radiolabeling
Abstract:
... Bombesin (BBN) is a peptide exhibiting high affinity for the gastrin-releasing peptide receptor (GRPR), which is overexpressed on several types of cancers. Various GRPR antagonists and agonists have been labeled with radiometals for positron emission tomography (PET) imaging of GRPR-positive tumors. However, unfavorable hepatobiliary excretion such as high intestinal activity may prohibit their cl ...
DOI:
10.1007/s00726-014-1718-y

17. Supraspinal metabotropic glutamate receptor subtype 8: a switch to turn off pain

Author:
Palazzo, Enza; de Novellis, Vito; Rossi, Francesco; Maione, Sabatino
Source:
Amino acids 2014 v.46 no.6 pp. 1441-1448
ISSN:
0939-4451
Subject:
agonists; analgesia; analgesics; central nervous system; glutamic acid; ligands; neurons; pain; receptors; sequence homology
Abstract:
... Glutamate is the main excitatory neurotransmitter in the central nervous system and as such controls the majority of synapses. Glutamatergic neurotransmission is mediated via ionotropic and metabotropic glutamate receptors (iGluRs and mGluRs). Signaling via mGluRs permits to finely tune, rather than turning on/off, the excitatory neurotransmission as the iGluRs do. Eight mGluRs (mGluR1-8) have bee ...
DOI:
10.1007/s00726-014-1703-5

18. Synthesis and analgesic effects of novel β2-tryptophan hexapeptide analogs

Author:
Bocheva, Adriana; Nocheva, Hristina; Pavlov, Nikola; Todorov, Petar; Calmès, Monique; Martinez, Jean; Naydenova, Emilia
Source:
Amino acids 2013 v.45 no.4 pp. 983-988
ISSN:
0939-4451
Subject:
agonists; analgesic effect; analgesics; antagonists; males; mechanism of action; rats; receptors
Abstract:
... Aiming to develop more potent analgesic substances a new series of hexapeptides containing β²-tryptophan analogues was synthesized. The Trp in position 4 and 5, respectively in Ac-Arg-Phe-Met-Trp-Met-Lys-NH₂(opioid receptor antagonist) and Ac-Arg-Tyr-Tyr-Arg-Trp-Lys-NH₂(highly potent and selective NOP-receptor agonist) was substituted by the (S)-2-(1-methyl-1H-indol-3-yl)propionic residue or the ( ...
DOI:
10.1007/s00726-013-1555-4

19. On the segregation of protein ionic residues by charge type

Author:
Parker, Michael S.; Balasubramaniam, Ambikaipakan; Parker, Steven L.
Source:
Amino acids 2012 v.43 no.6 pp. 2231-2247
ISSN:
0939-4451
Subject:
agonists; antagonists; antimicrobial peptides; polynucleotides; polypeptides; protein synthesis; regulatory proteins; transcription (genetics)
Abstract:
... Based on ubiquitous presence of large ionic motifs and clusters in proteins involved in gene transcription and protein synthesis, we analyzed the distribution of ionizable sidechains in a broad selection of proteins with regulatory, metabolic, structural and adhesive functions, in agonist, antagonist, toxin and antimicrobial peptides, and in self-excising inteins and intron-derived proteins and se ...
DOI:
10.1007/s00726-012-1418-4

20. Structural elucidation of Leuprolide and its analogues in solution: insight into their bioactive conformation

Author:
Laimou, Despina K.; Katsara, Maria; Matsoukas, Minos-Timotheos I.; Apostolopoulos, Vasso; Troganis, Anastassios N.; Tselios, Theodore V.
Source:
Amino acids 2010 v.39 no.5 pp. 1147-1160
ISSN:
0939-4451
Subject:
G-protein coupled receptors; agonists; breast neoplasms; deuterium oxide; dimethyl sulfoxide; gonadotropin-releasing hormone; humans; molecular dynamics; nuclear magnetic resonance spectroscopy; solvents
Abstract:
... Leuprolide [dLeu⁶, NHEt¹⁰]GnRH, a potent gonadotropin-releasing hormone (GnRH) agonist, is used in a wide variety of hormone-related diseases like cancer and endometriosis. In this report, the conformational behaviour of Leuprolide and its linear synthetic analogues, namely [Tyr⁵(OMe), dLeu⁶, Aze⁹, NHEt¹⁰]GnRH (1) and [Tyr⁵(OMe), dLeu⁶, NHEt¹⁰]GnRH (2) have been studied in DMSO and H₂O solutions b ...
DOI:
10.1007/s00726-010-0549-8