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1

KANIA, BOGDAN FELIKS, URSZULA BRACHA, GRZEGORZ LONC, and TOMASZ WOJNAR. "Significance of metabotropic glutamate receptor antagonists in experimental neuropathic pain in animals." Medycyna Weterynaryjna 76, no. 10 (2020): 6460–2020. http://dx.doi.org/10.21521/mw.6460.

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Neuropathic pain is a serious therapeutic problem. Current therapy is often ineffective, and the available drugs have serious side effects. For these reasons, the search for alternative therapeutic solutions is underway. Recent research on metabotropic receptors for glutamic acid (mGluR) gives great hope for the development of a new type of drug in the treatment of neuropathic pain. Particularly promising are antagonists of mGluR group I receptors. There are many studies demonstrating the efficacy of non-competitive mGlu1 and mGlu5 receptor antagonists in animal models of neuropathic pain. The
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Takeuchi, Koji, and Kenji Nagahama. "Animal Model of Acid-Reflux Esophagitis: Pathogenic Roles of Acid/Pepsin, Prostaglandins, and Amino Acids." BioMed Research International 2014 (2014): 1–10. http://dx.doi.org/10.1155/2014/532594.

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Esophagitis was induced in rats within 3 h by ligating both the pylorus and transitional region between the forestomach and glandular portion under ether anesthesia. This esophageal injury was prevented by the administration of acid suppressants and antipepsin drug and aggravated by exogenous pepsin. Damage was also aggravated by pretreatment with indomethacin and the selective COX-1 but not COX-2 inhibitor, whereas PGE2showed a biphasic effect depending on the dose; a protection at low doses, and an aggravation at high doses, with both being mediated by EP1 receptors. Various amino acids also
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Aldughaim, Mohammed S., Fatimah Alsaffar, and Michael D. Barker. "Coupling of a Novel TIMP3 Peptide to Carboxypeptidase G2 for Pro-Drug Activation at the Tumour Site." Molecules 26, no. 3 (2021): 625. http://dx.doi.org/10.3390/molecules26030625.

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Broad-spectrum cytotoxic drugs have been used in cancer therapy for decades. However, their lack of specificity to cancer cells often results in serious side-effects, limiting efficacy. For this reason, antibodies have been used to attempt to specifically target cytotoxic drugs to tumours. One such approach is antibody-directed enzyme prodrug therapy (ADEPT) which uses a tumour-directed monoclonal antibody, coupled to an enzyme, to convert a systemically administered non-toxic prodrug into a toxic one only at the tumour site. Among the main drawbacks of ADEPT is the immunogenicity of the antib
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Conti, Paola, Marco De Amici, Giovanni Grazioso, et al. "Synthesis, Binding Affinity at Glutamic Acid Receptors, Neuroprotective Effects, and Molecular Modeling Investigation of Novel Dihydroisoxazole Amino Acids†." Journal of Medicinal Chemistry 48, no. 20 (2005): 6315–25. http://dx.doi.org/10.1021/jm0504499.

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5

Hirabara, Sandro Massao, Renata Gorjao, Adriana Cristina Levada-Pires, et al. "Host cell glutamine metabolism as a potential antiviral target." Clinical Science 135, no. 2 (2021): 305–25. http://dx.doi.org/10.1042/cs20201042.

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Abstract A virus minimally contains a nucleic acid genome packaged by a protein coat. The genome and capsid together are known as the nucleocapsid, which has an envelope containing a lipid bilayer (mainly phospholipids) originating from host cell membranes. The viral envelope has transmembrane proteins that are usually glycoproteins. The proteins in the envelope bind to host cell receptors, promoting membrane fusion and viral entry into the cell. Virus-infected host cells exhibit marked increases in glutamine utilization and metabolism. Glutamine metabolism generates ATP and precursors for the
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Pozdniakova, N. V., N. V. Gorokhovets, N. V. Gukasova, A. V. Bereznikova, and E. S. Severin. "New Protein Vector ApE1 for Targeted Delivery of Anticancer Drugs." Journal of Biomedicine and Biotechnology 2012 (2012): 1–5. http://dx.doi.org/10.1155/2012/469756.

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A new chimeric geneApE1encoding the receptor-binding domain of the humanalpha-fetoprotein fused to a sequence of 22 glutamic acid residues was constructed. A new bacterial producer strainE. coliSHExT7 ApE1 was selected for ApE1 production in a soluble state. A simplified method was developed to purify ApE1 from bacterial biomass. It was shown that the new vector protein selectively interacts with AFP receptors on the tumor cell surface and can be efficiently accumulated in tumor cells. In addition, ApE1 was shown to be stable in storage and during its chemical modification. An increased number
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Pangalos, M. N., A. L. Malizia, P. T. Francis, et al. "Effect of Psychotropic Drugs on Excitatory Amino Acids in Patients Undergoing Psychosurgery for Depression." British Journal of Psychiatry 160, no. 5 (1992): 638–42. http://dx.doi.org/10.1192/bjp.160.5.638.

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Samples of ventricular CSF were taken from 52 consecutive patients admitted for psychosurgery for intractable depression. Concentrations of asparagine, aspartate, glutamine, glutamic acid, and serine were determined. Glutamate and aspartate concentrations, implicated in excitotoxic brain damage, were not affected by various types of psychotropic drug treatment. Serine, a modulator of glutamate responses, was significantly elevated in samples from subjects receiving antidepressants. These subjects responded poorly to the operation. Psychotropic drugs are unlikely to be neurotoxic. Nevertheless,
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Aizawa, Sayaka, Takafumi Sakai та Ichiro Sakata. "Glutamine and glutamic acid enhance thyroid-stimulating hormone β subunit mRNA expression in the rat pars tuberalis". Journal of Endocrinology 212, № 3 (2012): 383–94. http://dx.doi.org/10.1530/joe-11-0388.

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Thyroid-stimulating hormone (TSH)-producing cells of the pars tuberalis (PT) display distinct characteristics that differ from those of the pars distalis (PD). The mRNA expression ofTSHβandαGSUin PT has a circadian rhythm and is inhibited by melatonin via melatonin receptor type 1; however, the detailed regulatory mechanism forTSHβexpression in the PT remains unclear. To identify the factors that affect PT, a microarray analysis was performed on laser-captured PT tissue to screen for genes coding for receptors that are abundantly expressed in the PT. In the PT, we found high expression of theK
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9

Meadus, WJ, R. MacInnis, and ME Dugan. "Prolonged dietary treatment with conjugated linoleic acid stimulates porcine muscle peroxisome proliferator activated receptor gamma and glutamine-fructose aminotransferase gene expression in vivo." Journal of Molecular Endocrinology 28, no. 2 (2002): 79–86. http://dx.doi.org/10.1677/jme.0.0280079.

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Peroxisome proliferator activated receptors (PPARs) represent a family of DNA binding proteins that are activated by a variety of dietary and endogenous fatty acids. The PPAR proteins are expressed throughout the body and are the target of a variety of lipidaemic and insulin sensitizing drugs. Conjugated linoleic acid (CLA) is a collective name for octadecadienoic acid isomers with conjugated double bonds, which can also act as ligands for some of the PPAR family. To gain better understanding of the long-term effects of PPAR activation, CLA was fed at 11 g/kg of feed for 45 days to castrated m
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10

Szpręgiel, Izabela, Danuta Wrońska, Michał Kmiecik, Sylwia Pałka, and Bogdan F. Kania. "Glutamic Acid Decarboxylase Concentration Changes in Response to Stress and Altered Availability of Glutamic Acid in Rabbit (Oryctolagus cuniculus) Brain Limbic Structures." Animals 11, no. 2 (2021): 455. http://dx.doi.org/10.3390/ani11020455.

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Glutamic acid decarboxylase (GAD) is an enzyme that catalyses the formation of γ-aminobutyric acid (GABA), the most important inhibitory neurotransmitter, from glutamic acid (Glu), which is considered the most important excitatory transmitter in the central and peripheral nervous systems. GAD is a key enzyme that provides a balance between Glu and GABA concentration. Hence, it can be assumed that if the GAD executes the synthesis of GABA from Glu, it is important in the stress response, and thus also in triggering the emotional states of the body that accompany stress. The aim of the study was
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11

Matosiuk, Dariusz. "Potential Future of New Glutamate Agonists and Antagonists Development." Anti-Cancer Agents in Medicinal Chemistry 18, no. 4 (2018): 506–20. http://dx.doi.org/10.2174/1871520618666180404125041.

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Receptors of glutamic acid are known for over 30 years for their action and for about 20 years for their structure. Presence of at least three classes of ionotropic receptors was confirmed at the beginning of 80’. Recognition of the sequence and first cloning were done at the beginning of 90’. In 1994 ligand binding site was recognized at the junction of two subunits S1-S2 in the ligand-binding domain. Since then, many subtypes of ionotropic and metabotropic glutamate receptors were recognized, together with their localization and functions. In the meantime numerous orthosteric ligands, both a
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Debonnel, Guy, Michel Weiss, and Claude de Montigny. "Reduced neuroexcitatory effect of domoic acid following mossy fiber denervation of the rat dorsal hippocampus: further evidence that toxicity of domoic acid involves kainate receptor activation." Canadian Journal of Physiology and Pharmacology 67, no. 8 (1989): 904–8. http://dx.doi.org/10.1139/y89-142.

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Domoic acid, an excitatory amino acid structurally related to kainic acid, has been shown to be responsible for the severe intoxication presented, in 1987, by more than one hundred and fifty people having eaten mussels grown in Prince Edward Island (Canada). Unitary extracellular recordings were obtained from pyramidal neurons of the CA3 region of the rat dorsal hippocampus. The excitatory effects of microiontophoretic applications of domoic acid and of the agonists of the two other subtypes of glutamatergic receptors, quisqualate and N-methyl-D-aspartate, were compared on intact and colchicin
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13

Hu, Xiao-Long, Ya-Jun Niu, Mi Chen та ін. "Preventive Effects of Total Flavonoid C-Glycosides from Abrus mollis on Nonalcoholic Fatty Liver Disease through Activating the PPARα Signaling Pathway". Planta Medica 85, № 08 (2019): 678–88. http://dx.doi.org/10.1055/a-0895-5838.

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Abstract Abrus pulchellus subsp. mollis (Hance) Verdc. (Leguminosae) is a well-known edible plant usually added to soups and beverages. In this study, vicenin-2 (1), isoschaftoside (2), schaftoside (3), and their enrichment fraction, total flavonoid C-glycosides, derived from the extracts of A. mollis, were firstly found to prevent nonalcoholic fatty liver disease both in vitro and in vivo. In the in vitro study, total flavonoid C-glycosides decreased the lipid accumulation in oleic acid-treated HepG2 cells. The mechanisms of total flavonoid C-glycosides are involved in the regulation of perox
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Saha, Abhijit, Koushik Sarker, Avijit Ghosh, Suvasish Mishra, and Subrata Sen. "RATIONAL DESIGN, SYNTHESIS AND IN VITRO EVALUATION OF N-(4-ETHOXYPHENYLSULFONYL)-L-GLUTAMIC ACID ANALOGUES AS ANTIANGIOGENIC AND ANTICANCER AGENTS ON MULTIPLE MYELOMA." INDIAN DRUGS 57, no. 12 (2021): 26–35. http://dx.doi.org/10.53879/id.57.12.12807.

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We report the rational design, synthesis and evaluation of the anticancer and antiangiogenic activity of the N-(4-ethoxyphenylsulfonyl)-L-glutamic acid analogs on multiple myeloma. From the series, compound 2c, 2f, and 2h exhibit cytotoxic action on human multiple myeloma cell line RPMI8226 with IC50 (μM) value 2.72, 2.24, and 1.81, respectively. These compounds possess the antiangiogenic property and are selectively cytotoxic to cancer cells, as observed from the in vitro study of Human Umbilical Vein Endothelial Cell (HUVEC) and African green monkey kidney epithelial cell (VERO), respectivel
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15

Kojima, Honami, Saeri Ikegami, Shiho Nakamura та ін. "Preparation and Evaluation of Poly-γ-Glutamic Acid Hydrogel Mixtures with Basic Drugs or Acidic Drugs: Effect on Ease of Swallowing and Taste Masking". Pharmacology & Pharmacy 10, № 10 (2019): 427–44. http://dx.doi.org/10.4236/pp.2019.1010035.

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16

Wolfert, Margreet A., Abhijit Roychowdhury, and Geert-Jan Boons. "Modification of the Structure of Peptidoglycan Is a Strategy To Avoid Detection by Nucleotide-Binding Oligomerization Domain Protein 1." Infection and Immunity 75, no. 2 (2006): 706–13. http://dx.doi.org/10.1128/iai.01597-06.

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ABSTRACT Nucleotide-binding oligomerization domain (NOD) protein 1 (NOD1) and NOD2 are pathogen recognition receptors that sense breakdown products of peptidoglycan (PGN) (muropeptides). It is shown that a number of these muropeptides can induce tumor necrosis factor alpha (TNF-α) gene expression without significant TNF-α translation. This translation block is lifted when the muropeptides are coincubated with lipopolysaccharide (LPS), thereby accounting for an apparently synergistic effect of the muropeptides with LPS on TNF-α protein production. The compounds that induced synergistic effects
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17

Jang, Jeyoun, Minhui Cho, Jeong-Hoon Chun та ін. "The Poly-γ-d-Glutamic Acid Capsule of Bacillus anthracis Enhances Lethal Toxin Activity". Infection and Immunity 79, № 9 (2011): 3846–54. http://dx.doi.org/10.1128/iai.01145-10.

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ABSTRACTThe poly-γ-d-glutamic acid (PGA) capsule is one of the major virulence factors ofBacillus anthracis, which causes a highly lethal infectious disease. The PGA capsule disguisesB. anthracisfrom immune surveillance and allows its unimpeded growth in the host. The PGA capsule recently was reported to be associated with lethal toxin (LT) in the blood of experimentally infected animals (M. H. Cho, et al., Infect. Immun. 78:387-392, 2010). The effect of PGA, either alone or in combination with LT, on macrophages, which play an important role in the progression of anthrax disease, has not been
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18

Drewe, J. A., R. Miles, and D. L. Kunze. "Excitatory amino acid receptors of guinea pig medial nucleus tractus solitarius neurons." American Journal of Physiology-Heart and Circulatory Physiology 259, no. 5 (1990): H1389—H1395. http://dx.doi.org/10.1152/ajpheart.1990.259.5.h1389.

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Neurons isolated from the medial subnuclei of nucleus tractus solitarius in adult guinea pigs were studied for responses to the excitatory amino acid glutamate and its analogues using the whole cell tight-seal voltage clamp technique. In 80% of the cells studied (n = 60) 100 microM glutamate produced inward currents at negative voltages. To further characterize the glutamate response, the agonists for three glutamate receptor subtypes, N-methyl-D-aspartate (NMDA), kainate, and quisqualate, were examined for their effects on membrane conductance. NMDA (25-250 microM) activated currents in 85% o
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19

Von Bergen, Nicholas H., Alberto Subieta, and Timothy J. Brennan. "Effect of Intrathecal Non-NMDA EAA Receptor Antagonist LY293558 in Rats." Anesthesiology 97, no. 1 (2002): 177–82. http://dx.doi.org/10.1097/00000542-200207000-00025.

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Background Excitatory amino acid receptors are important for both sensory and motor function in the spinal cord. We studied the effects of intrathecal LY293558, a competitive non-N-methyl-D-aspartate excitatory amino acid receptor antagonist, on motor and sensory function in rats to determine whether drugs blocking these receptors could potentially be used as alternative agents to local anesthetics for spinal anesthesia. Methods Rats were tested before and 15-240 min after intrathecal injection of 5 nmol (in 10 microl) LY293558. Sensory function was tested at the hind paw using withdrawal resp
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20

Kim, Choi, Choi, Park, and Ryu. "Hyaluronic Acid-Coated Nanomedicine for Targeted Cancer Therapy." Pharmaceutics 11, no. 7 (2019): 301. http://dx.doi.org/10.3390/pharmaceutics11070301.

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Hyaluronic acid (HA) has been widely investigated in cancer therapy due to its excellent characteristics. HA, which is a linear anionic polymer, has biocompatibility, biodegradability, non-immunogenicity, non-inflammatory, and non-toxicity properties. Various HA nanomedicines (i.e., micelles, nanogels, and nanoparticles) can be prepared easily using assembly and modification of its functional groups such as carboxy, hydroxy and N-acetyl groups. Nanometer-sized HA nanomedicines can selectively deliver drugs or other molecules into tumor sites via their enhanced permeability and retention (EPR)
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Fried, David E., Ralph E. Watson, Simon C. Robson та Brian D. Gulbransen. "Ammonia modifies enteric neuromuscular transmission through glial γ-aminobutyric acid signaling". American Journal of Physiology-Gastrointestinal and Liver Physiology 313, № 6 (2017): G570—G580. http://dx.doi.org/10.1152/ajpgi.00154.2017.

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Impaired gut motility may contribute, at least in part, to the development of systemic hyperammonemia and systemic neurological disorders in inherited metabolic disorders, or in severe liver and renal disease. It is not known whether enteric neurotransmission regulates intestinal luminal and hence systemic ammonia levels by induced changes in motility. Here, we propose and test the hypothesis that ammonia acts through specific enteric circuits to influence gut motility. We tested our hypothesis by recording the effects of ammonia on neuromuscular transmission in tissue samples from mice, pigs,
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Bhardwaj, Ankit, Atma Ram Sharma, and Sarla Sharma. "Cefixime induce non convulsive status epileptics: a neurotoxic effect." International Journal of Basic & Clinical Pharmacology 8, no. 10 (2019): 2341. http://dx.doi.org/10.18203/2319-2003.ijbcp20194284.

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Nonconvulsive status epileptics comprises a group of syndromes that display a great diversity regarding response to anticonvulsants ranging from virtually self-limiting variants to entirely refractory forms cephalosporins are thought to provoke seizure through inhibitory effects on gamma-aminobutyric acid (GABA) transmission and GABA receptors. Interference with GABA transmission result in pre-disposition towards excitatory neurotransmission, which can leads to seizures. Antibiotics can alter the serum concentration of anti-epileptic, resulting in seizures and anti-epileptic drugs toxicity.
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Dill, Veronika, Aline Zimmer, Martin Beer, and Michael Eschbaumer. "Targeted Modification of the Foot-And-Mouth Disease Virus Genome for Quick Cell Culture Adaptation." Vaccines 8, no. 4 (2020): 583. http://dx.doi.org/10.3390/vaccines8040583.

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Foot-and-mouth disease virus (FMDV) causes the highly contagious foot-and-mouth disease, which is characterized by the appearance of vesicles in and around the mouth and feet of cloven-hoofed animals. BHK-21 cells are the cell line of choice for the propagation of FMDV for vaccine production worldwide but vary in their susceptibility for different FMDV strains. Previous studies showed that the FMDV resistance of a certain BHK cell line can be overcome by using a closely related but permissive cell line for the pre-adaptation of the virus, but the adapted strains were found to harbor several ca
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Dhar, Priyanka, and Paushali Roy. "Molecular Docking Unmasks Potent Phytoligands against SARS CoV 2 Spike Glycoprotein, Main Protease, Papain like Protease and RNA dependent RNA Polymerase." Defence Life Science Journal 5, no. 4 (2020): 255–67. http://dx.doi.org/10.14429/dlsj.5.15999.

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The recent coronavirus disease 2019 (COVID-19) pandemic caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has offered a unique challenge for human survival. However, there is no available known prophylaxis, therapeutic intervention, and vaccine candidate against SARS-CoV-2 to date. We aimed towards identifying novel phytoligands from widely available botanical resources which could serve as potential inhibitors against SARS-CoV-2. Based on literature review, database search, ADMET, and drug-likeness, 55 phytoligands and 8 synthetic repurposing drugs were screened and teste
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FRAGOSO, GABRIELA, and ANA MARÍA LÓPEZ-COLOMÉ. "Excitatory amino acid-induced inositol phosphate formation in cultured retinal pigment epithelium." Visual Neuroscience 16, no. 2 (1999): 263–69. http://dx.doi.org/10.1017/s0952523899162072.

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Excitatory amino acid (EAA)-induced production of inositolphosphates (IPs) was studied in primary cultures of chick retinal pigment epithelium (RPE) following in vitro incorporation of [3H] myo-inositol. Glutamic acid (L-glu) significantly increased [3H]-IPs accumulation (215%). L-glu agonists stimulated [3H]IPs accumulation in the following order of efficiency: N-methyl-D-aspartate (NMDA) ≥ L-glu > quisqualate ≥ kainate > (1S,3R)-1-aminocyclopentane-1,3-dicarboxylic acid (ACPD). Stimulation was dependent on external Ca2+. The NMDA-induced response was blocked by (+)-5-methyl-10,11-dihyd
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Chalisova, N. I., V. K. Kozlov, A. B. Mulik, E. P. Zatsepin, and T. A. Kostrova. "Protective influence of coded amino acids on the development of liver tissue culture in the presence of cytostatic." Toxicological Review, no. 2 (May 15, 2020): 48–53. http://dx.doi.org/10.36946/0869-7922-2020-2-47-52.

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An urgent problem is the search for substances that can provide a protective effect in cases of DNA synthesis and repair disorders that arise as a result of side effects of cytostatic drugs used in the treatment of cancer. The aim of this work was to study the effect of 20 encoded amino acids in the presence of Cyclophosphane on the development of organotypic culture of rat liver tissue. The results obtained indicate that Cyclophosphane; which simulates the action of such cytostatic substances; inhibits cell proliferation in the liver tissue. It was also found that the encoded amino acids: asp
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Ziganshin, A. U., D. V. Bedova, E. A. Zubkov, and M. E. Sitdykova. "P2-receptors of the urinary bladder as potential targets for novel drugs." Kazan medical journal 99, no. 3 (2018): 462–66. http://dx.doi.org/10.17816/kmj2018-462.

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Purinergic P2 receptors, the basic endogenous agonist of which is adenosine triphosphoric acid (ATP), are widely spread in the organs and tissues of human and animals including urogenitary system. Physiologically, in the peripheral nervous system the role of P2 receptors in most cases is not leading, they only complement or modulate the action of main neuromediators (acetylcholine, norepinephrine). But in pathology the role of P2 receptors significantly increases and often takes the lead in the pathogenesis of one or another disease. In particular, it was determined that purinergic component o
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Nguyen, Sy Le Thanh, Keitarou Kimura, Thi Tuyen Do та Thi Ngoc Anh Le. "Isolation, characterization of Bacillus sp. producing heavy metal absorption γ-PGA". Journal of Vietnamese Environment 9, № 1 (2018): 49–54. http://dx.doi.org/10.13141/jve.vol9.no1.pp49-54.

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Poly-gamma-glutamic acid (γPGA), which is a biodegradable, non-immunogenic and unusual anionic amino-acid polymer consist of D- and L-glutamic acid units, was exploited for a wide array of useful applications. Bacillus are well known cellular system important for fermentation to synthesize γPGA, which is used as thickener, drugs carrier, cryoprotectant, humectant, biological adhesive, flocculants, or heavy metal absorbent. This study focused on the isolation of Bacillus spp. that is possible to produce γ-PGA from different soil samples from different places in Vietnam. Study the effect of prec
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Ma, Shu-Rong, Jin-Bo Yu, Jie Fu, et al. "Determination and Application of Nineteen Monoamines in the Gut Microbiota Targeting Phenylalanine, Tryptophan, and Glutamic Acid Metabolic Pathways." Molecules 26, no. 5 (2021): 1377. http://dx.doi.org/10.3390/molecules26051377.

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It has been reported that monoamine neurotransmitters can be produced by gut microbiota, and that several related metabolites of amino acids in these pathways are associated with nervous system (NVS) diseases. Herein, we focused on three pathways, namely, phenylalanine (Phe), tryptophan (Trp), and glutamic acid (Glu), and established an underivatized liquid chromatography–tandem mass spectrometry (LC-MS/MS) method for the quantification of nineteen monoamine neurotransmitters and related metabolites in the gut microbiota. The neurotransmitters and related metabolites included Phe, tyrosine (Ty
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Chaika, Natalia, Matar Mazen, Oleh Koshovyi, et al. "Research in phytochemical composition and hypoglycemic activity screening of the dry extracts from bearberry leaves." ScienceRise: Pharmaceutical Science, no. 3(31) (June 30, 2021): 42–50. http://dx.doi.org/10.15587/2519-4852.2021.235939.

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Diabetes mellitus is a global medical and social issue. In the developed countries of the world, from 5 to 12% of the population are diagnosed with diabetes mellitus and, according to WHO prognosis, the level of this disease may increase to 30-35%. Type 2 diabetes is a disease that progresses over time, but the rational and systematic use of hypoglycemic synthetic drugs and phytopreparations can significantly delay the onset of insulin therapy. A promising source of BAS with a hypoglycemic effect is the raw material of plants of the Heather family, namely, bearberry leaves. However, on the Ukr
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PARADATURSKA, J., and W. TURSKI. "Excitatory amino acid antagonists and memory: Effect of drugs acting at N-methyl-d-aspartate receptors in learning and memory tasks." Neuropharmacology 29, no. 12 (1990): 1111–16. http://dx.doi.org/10.1016/0028-3908(90)90034-o.

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Itzhaki, Ella, Elad Hadad, Neta Moskovits, Salomon M. Stemmer, and Shlomo Margel. "Tumor-Targeted Fluorescent Proteinoid Nanocapsules Encapsulating Synergistic Drugs for Personalized Cancer Therapy." Pharmaceuticals 14, no. 7 (2021): 648. http://dx.doi.org/10.3390/ph14070648.

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Personalized cancer treatment based on specific mutations offers targeted therapy and is preferred over “standard” chemotherapy. Proteinoid polymers produced by thermal step-growth polymerization of amino acids may form nanocapsules (NCs) that encapsulate drugs overcoming miscibility problems and allowing passive targeted delivery with reduced side effects. The arginine-glycine-glutamic acid (RGD) sequence is known for its preferential attraction to αvβ3 integrin, which is highly expressed on neovascular endothelial cells that support tumor growth. Here, tumor-targeted RGD-based proteinoid NCs
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Wang, Dian-Shi, Kirusanthy Kaneshwaran, Gang Lei та ін. "Dexmedetomidine Prevents Excessive γ-Aminobutyric Acid Type A Receptor Function after Anesthesia". Anesthesiology 129, № 3 (2018): 477–89. http://dx.doi.org/10.1097/aln.0000000000002311.

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Abstract What We Already Know about This Topic What This Article Tells Us That Is New Background Postoperative delirium is associated with poor long-term outcomes and increased mortality. General anesthetic drugs may contribute to delirium because they increase cell-surface expression and function of α5 subunit-containing γ-aminobutyric acid type A receptors, an effect that persists long after the drugs have been eliminated. Dexmedetomidine, an α2 adrenergic receptor agonist, prevents delirium in patients and reduces cognitive deficits in animals. Thus, it was postulated that dexmedetomidine p
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Dubé, G. R., and K. C. Marshall. "Activity-Dependent Activation of Presynaptic Metabotropic Glutamate Receptors in Locus Coeruleus." Journal of Neurophysiology 83, no. 3 (2000): 1141–49. http://dx.doi.org/10.1152/jn.2000.83.3.1141.

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Synaptic activation of metabotropic glutamate receptors (mGluRs) in the locus coeruleus (LC) was investigated in adult rat brain slice preparations. Evoked excitatory postsynaptic potentials (EPSPs) resulting from stimulation of LC afferents were measured with current clamp from intracellularly recorded LC neurons. In this preparation, mGluR agonists (±)-1-aminocyclopentane- trans-1,3-dicarboxylic acid ( t-ACPD) and L(+)-2-amino-4-phosphonobutyric acid (L-AP4) activate distinct presynaptic mGluRs, resulting in an inhibition of EPSPs. When two stimuli were applied to afferents at intervals >
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Rodríguez-Silverio, Juan, María Elena Sánchez-Mendoza, Héctor Isaac Rocha-González, et al. "Evaluation of the Antinociceptive, Antiallodynic, Antihyperalgesic and Anti-Inflammatory Effect of Polyalthic Acid." Molecules 26, no. 10 (2021): 2921. http://dx.doi.org/10.3390/molecules26102921.

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Nonsteroidal anti-inflammatory drugs (NSAIDs) are very commonly used, but their adverse effects warrant investigating new therapeutic alternatives. Polyalthic acid, a labdane-type diterpenoid, is known to produce gastroprotection, tracheal smooth muscle relaxation, and antitumoral, antiparasitic and antibacterial activity. This study aimed to evaluate the antinociceptive, antiallodynic, antihyperalgesic and anti-inflammatory effect of polyalthic acid on rats. Moreover, the effectiveness of treating hyperalgesia with a combination of polyalthic acid and naproxen was analyzed, as well as the typ
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Farhat, Hala, and Bruce G. Allen. "Salicylic acid alters endothelin-1 binding in intact adult rat ventricular myocytes." Biochemistry and Cell Biology 82, no. 6 (2004): 728–38. http://dx.doi.org/10.1139/o04-125.

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Endothelin receptors ETAR and ETBR form tight receptor–ligand complexes that complicate our understanding of the physiological, pharmacological, and biochemical properties of these receptors. Although radioligand–binding studies have demonstrated the binding of endothelin-1 (ET-1) to ETAR to be essentially irreversible, ETAR internalize in a ligand-dependent manner, release ET-1, and then recycle to the cell surface. Salicylic acid (SA) reduces ET-1 binding (IC50 = 10 mmol/L) to recombinant ETAR in isolated membranes by promoting dissociation of [125I]ET-1. In the present study, SA (5 mmol SA/
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Chiara, Federica, Subal Bishayee, Carl-Henrik Heldin та Jean-Baptiste Demoulin. "Autoinhibition of the Platelet-derived Growth Factor β-Receptor Tyrosine Kinase by Its C-terminal Tail". Journal of Biological Chemistry 279, № 19 (2004): 19732–38. http://dx.doi.org/10.1074/jbc.m314070200.

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In this report, we investigated the role of the C-terminal tail of the platelet-derived growth factor (PDGF) β-receptor in the control of the receptor kinase activity. Using a panel of PDGF β-receptor mutants with progressive C-terminal truncations, we observed that deletion of the last 46 residues, which contain a proline- and glutamic acid-rich motif, increased the autoactivation velocityin vitroand theVmaxof the phosphotransfer reaction, in the absence of ligand, as compared with wild-type receptors. By contrast, the kinase activity of mutant and wild-type receptors that were pre-activated
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Martínez-Vázquez, Mariano, and Rosa Estrada-Reyes. "Secondary metabolismin in Annonaceae: potencial source of drugs." Revista Brasileira de Fruticultura 36, spe1 (2014): 141–46. http://dx.doi.org/10.1590/s0100-29452014000500017.

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Several species of Annona (Annonaceae) are used in traditional Mexican medicine by their anti-anxiety, anticonvulsant and tranquilizing properties. It has been reported that the alkaloids isolated from some species of the Annona have affinity to serotonergic 5-HT1A receptors and modulate dopaminergic transmission, which is involved in depressive disorders. In this review it is showed the results of the antidepressant-like effect of an alkaloid extract from the aerial parts of Annona cherimola (TA) in mice. The antidepressant-like effect was evaluated in the forced swimming test. To elucidate a
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Lindsay, Paul J., та W. Reuben Kaufman. "Potentiation of salivary fluid secretion in ixodid ticks: a new receptor system for γ-aminobutyric acid". Canadian Journal of Physiology and Pharmacology 64, № 8 (1986): 1119–26. http://dx.doi.org/10.1139/y86-191.

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γ-Aminobutyric acid (GABA), having minimal intrinsic activity, potentiates dopamine-induced fluid secretion in salivary glands of female ixodid ticks. Because the effect of GABA was similar to that of spiperone, we tested whether these two drugs act at a common recognition site. Potentiation was not augmented when salivary glands were exposed to supramaximal concentrations of spiperone (1 μM) plus GABA (100 μM). (±)-Sulpiride (100 μM), a spiperone antagonist in this system, also blocked GABA-induced potentiation. Picrotoxin (100 μM) and (−)-bicuculline (100 μM), two GABA antagonists, blocked G
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Kwak, Sang Hyun, Gi-Sung Nam, Seong Hoon Bae, and Jinsei Jung. "Effect of Specific Retinoic Acid Receptor Agonists on Noise-Induced Hearing Loss." International Journal of Environmental Research and Public Health 16, no. 18 (2019): 3428. http://dx.doi.org/10.3390/ijerph16183428.

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Noise is one of the most common causes of hearing loss in industrial countries. There are many studies about chemical agents to prevent noise-induced hearing loss (NIHL). However, there is no commercially available drug yet. Retinoic acid is an active metabolite of Vitamin A; it has an anti-apoptic role in NIHL. This study aims to verify the differences among selective agonists of retinoic acid receptors (RARs) in NIHL. All-trans retinoic acid (ATRA), AM80 (selective retinoic acid receptor α agonist), AC261066 (Selective retinoic acid receptor β1 agonist), and CD1530 (Selective retinoic acid λ
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Studneva, Irina M., Oksana М. Veselova, Arthur A. Bahtin, Galina G. Konovalova, Vadim Z. Lankin, and Oleg I. Pisarenko. "The mechanisms of cardiac protection using a synthetic agonist of galanin receptors during chronic administration of doxorubicin." Acta Naturae 12, no. 1 (2020): 89–98. http://dx.doi.org/10.32607/actanaturae.10945.

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The use of the anticancer drug doxorubicin (Dox) is limited by its cardiotoxic effect. The aim of this work was to study the effect of a new synthetic agonist of the galanin receptor GalR1-3 [Ala14, His15]-galanine (215) (G) on the metabolism, antioxidant enzyme activity, and cardiac function in rats with cardiomyopathy (CM) caused by chronic administration of Dox. Coadministration of peptide G and Dox significantly increased the fractional shortening (FS) and ejection fraction (EF) by an average of 30 4% compared with the indices in the Dox group. The reduced severity of cardiac dysfunction u
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Wheatley, Mark, Jack Charlton, Mohammed Jamshad, et al. "GPCR–styrene maleic acid lipid particles (GPCR–SMALPs): their nature and potential." Biochemical Society Transactions 44, no. 2 (2016): 619–23. http://dx.doi.org/10.1042/bst20150284.

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G-protein-coupled receptors (GPCRs) form the largest class of membrane proteins and are an important target for therapeutic drugs. These receptors are highly dynamic proteins sampling a range of conformational states in order to fulfil their complex signalling roles. In order to fully understand GPCR signalling mechanisms it is necessary to extract the receptor protein out of the plasma membrane. Historically this has universally required detergents which inadvertently strip away the annulus of lipid in close association with the receptor and disrupt lateral pressure exerted by the bilayer. De
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BASIVIREDDY, Jayasree, Molly JACOB, and Kunissery A. BALASUBRAMANIAN. "Oral glutamine attenuates indomethacin-induced small intestinal damage." Clinical Science 107, no. 3 (2004): 281–89. http://dx.doi.org/10.1042/cs20030390.

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The use of NSAIDs (non-steroidal anti-inflammatory drugs), although of great therapeutic value clinically, is limited by their tendency to cause mucosal damage in the gastrointestinal tract. In the small intestine, the effects these drugs have been shown to produce include inhibition of cyclo-oxygenase, mitochondrial dysfunction and free radical-induced oxidative changes, all of which contribute to the mucosal damage seen. Glutamine is a fuel preferentially used by enterocytes and is known to contribute to maintaining the integrity of these cells. In the present study, we investigated the effe
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Semina, I. I., and A. Z. Baychurina. "Development of new potential drugs with psychotropic activity among phosphorylacetohydrazides and other phosphorylated carboxylic acids derivatives - priority area of Kazan school of psychopharmacologists." Kazan medical journal 97, no. 1 (2016): 148–55. http://dx.doi.org/10.17750/kmj2016-148.

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In the present review professors A.I. Razumov and I.V. Zaikonnikova ideas development on the prospects of potential drugs investigation in the class of phosphorylated carboxylic acids are described. The first representative of these compounds, approved for clinical use, became a difenilphosphorylacetic acid hydrazide - the drug phosenazid (diphenizid, phosphabenzide, gidiphen) with a tranquilizing, anti-alcohol, antidepressant and antiepileptic properties. Continuing research, we studied the new series of phosphorylacetohydrazides and found that the 4-dimethylaminophenyl, 2’-chloroethoxyphosph
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45

Boegman, Roland, and Brian Collier. "Symposium Cholinergic Mechanisms: I. Function and Dysfunction of Cholinergic Neurones: II. Neurotoxicity Associated with Altered Cholinergic Function." Canadian Journal of Physiology and Pharmacology 64, no. 3 (1986): 316–17. http://dx.doi.org/10.1139/y86-051.

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The objective of these two symposia was to summarize some of the more recent advances relating to the neurobiology of cholinergic synaptic transmission, with particular emphasis on presynaptic function and dysfunction.For many years productive studies of acetylcholine metabolism were sustained by the physiological importance of this neurotransmitter. More recently research upon cholinergic mechanisms has been stimulated by the association of cholinergic dysfunction with disorders of the nervous system, particularly those related to cognitive dysfunction. The association between central choline
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Piotrovsky, L. B., O. N. Koreschonkov, P. V. Perestenko, and M. A. Dumpis. "THE EFFECT OF N-PHTHALAMOYL-L-GLUTAMIC ACID (PhGA), A NOVEL SELECTIVE NMDA RECEPTORS AGONIST, ON THE BINDING OF 3H-L-GLU WITH THE SYNAPTIC MEMBRANES OF HUMAN HIPPOCAMPUS." Clinical Neuropharmacology 15 (1992): 557B. http://dx.doi.org/10.1097/00002826-199202001-01087.

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Kmiecik, Szymon Wojciech, Mateusz Adam Krzyścik, Beata Filip-Psurska, Joanna Wietrzyk, Janusz Boratyński, and Tomasz Marek Goszczyński. "Methotrexate and epirubicin conjugates as potential antitumor drugs." Postępy Higieny i Medycyny Doświadczalnej 71, no. 1 (2017): 0. http://dx.doi.org/10.5604/01.3001.0010.3842.

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Introduction: The use of hybrid molecules has become one of the most significant approaches in new cytotoxic drug design. This study describes synthesis and characterization of conjugates consisting of two well-known and characterized chemotherapeutic agents: methotrexate (MTX) and epirubicin (EPR). The synthesized conjugates combine two significant anticancer strategies: combinatory therapy and targeted therapy. These two drugs were chosen because they have different mechanisms of action, which can increase the anticancer effect of the obtained conjugates. MTX, which is a folic acid analog, h
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Filippatos, Theodosios D., Angelos Liontos, Eliza C. Christopoulou, and Moses S. Elisaf. "Novel Hypolipidaemic Drugs: Mechanisms of Action and Main Metabolic Effects." Current Vascular Pharmacology 17, no. 4 (2019): 332–40. http://dx.doi.org/10.2174/1570161116666180209112351.

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Over the last 3 decades, hypolipidaemic treatment has significantly reduced both Cardiovascular (CV) risk and events, with statins being the cornerstone of this achievement. Nevertheless, residual CV risk and unmet goals in hypolipidaemic treatment make novel options necessary. Recently marketed monoclonal antibodies against proprotein convertase subtilisin/kexin type 9 (PCSK9) have shown the way towards innovation, while other ways of PCSK9 inhibition like small interfering RNA (Inclisiran) are already being tested. Other effective and well tolerated drugs affect known paths of lipid synthesi
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Zhang, Hongliang, Chunkui Zhou, Limin Wu, Fengming Ni, Jie Zhu, and Tao Jin. "Are Onconeural Antibodies a Clinical Phenomenology in Paraneoplastic Limbic Encephalitis?" Mediators of Inflammation 2013 (2013): 1–9. http://dx.doi.org/10.1155/2013/172986.

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Paraneoplastic neurological syndromes (PNSs) occur in patients with cancer and can cause clinical symptoms and signs of dysfunction of the nervous system that are not due to a local effect of the tumor or its metastases. Most of these clinical syndromes in adults are associated with lung cancer, especially small cell lung cancer (SCLC), lymphoma, and gynecological tumors. The finding of highly specific antibodies directed against onconeural antigens has revolutionized the diagnosis and promoted the understanding of these syndromes and led to the current hypothesis of an autoimmune pathophysiol
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Wielgat, Przemyslaw, Karol Rogowski, Katarzyna Niemirowicz-Laskowska, and Halina Car. "Sialic Acid-Siglec Axis as Molecular Checkpoints Targeting of Immune System: Smart Players in Pathology and Conventional Therapy." International Journal of Molecular Sciences 21, no. 12 (2020): 4361. http://dx.doi.org/10.3390/ijms21124361.

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The sialic acid-based molecular mimicry in pathogens and malignant cells is a regulatory mechanism that leads to cross-reactivity with host antigens resulting in suppression and tolerance in the immune system. The interplay between sialoglycans and immunoregulatory Siglec receptors promotes foreign antigens hiding and immunosurveillance impairment. Therefore, molecular targeting of immune checkpoints, including sialic acid-Siglec axis, is a promising new field of inflammatory disorders and cancer therapy. However, the conventional drugs used in regular management can interfere with glycome mac
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