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Article ; Online: Role of voltage-dependent calcium channels on the striatal in vivo dopamine release induced by the organophosphorus pesticide glyphosate.

Costas-Ferreira, Carmen / Silva, Ana Carolina de Jesus / Hage-Melim, Lorane Izabel da Silva / Faro, Lilian R Ferreira

Environmental toxicology and pharmacology

2023 Volume 104, Page(s) 104285

Abstract: In the present study, we investigated the role of voltage-sensitive calcium channels (VSCCs) on the striatal dopamine release induced by the pesticide glyphosate (GLY) using selective VSCC inhibitors. The dopamine levels were measured by in vivo cerebral ...

Abstract	In the present study, we investigated the role of voltage-sensitive calcium channels (VSCCs) on the striatal dopamine release induced by the pesticide glyphosate (GLY) using selective VSCC inhibitors. The dopamine levels were measured by in vivo cerebral microdialysis coupled to HPLC-ED. Nicardipine (L-type VSCC antagonist) or ω-conotoxin MVIIC (non-selective P/Q-type antagonist) had no effect on dopamine release induced by 5 mM GLY. In contrast, flunarizine (T-type antagonist) or ω-conotoxin GVIA (neuronal N-type antagonist) significantly reduced GLY-stimulated dopamine release. These results suggest that GLY-induced dopamine release depends on extracellular calcium and its influx through the T- and N-type VSCCs. These findings were corroborated by molecular docking, which allowed us to establish a correlation between the effect of GLY on blocked VSCC with the observed dopamine release. We propose new molecular targets of GLY in the dorsal striatum, which could have important implications for the assessment of pesticide risks in non-target organisms.
MeSH term(s)	Calcium Channels ; Dopamine ; Calcium Channel Blockers/pharmacology ; Organophosphorus Compounds/toxicity ; Pesticides ; Molecular Docking Simulation ; Calcium/metabolism
Chemical Substances	Calcium Channels ; Dopamine (VTD58H1Z2X) ; Calcium Channel Blockers ; Organophosphorus Compounds ; Pesticides ; Calcium (SY7Q814VUP)
Language	English
Publishing date	2023-09-30
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1318302-3
ISSN	1872-7077 ; 1382-6689
ISSN (online)	1872-7077
ISSN	1382-6689
DOI	10.1016/j.etap.2023.104285
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Zs.A 4490: Show issues

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Article ; Online: In silico and in vitro analysis of the mechanisms of action of nitroxoline against some medically important opportunistic fungi.

de Chaves, Magda Antunes / da Costa, Bárbara Souza / de Souza, Jade André / Batista, Mateus Alves / de Andrade, Saulo Fernandes / Hage-Melim, Lorane Izabel da Silva / Abegg, Maxwell / Lopes, Marcela Silva / Fuentefria, Alexandre Meneghello

Journal de mycologie medicale

2023 Volume 33, Issue 3, Page(s) 101411

Abstract: The increasing resistance to antifungal agents associated with toxicity and interactions turns therapeutic management of fungal infections difficult. This scenario emphasizes the importance of drug repositioning, such as nitroxoline - a urinary ... ...

Abstract	The increasing resistance to antifungal agents associated with toxicity and interactions turns therapeutic management of fungal infections difficult. This scenario emphasizes the importance of drug repositioning, such as nitroxoline - a urinary antibacterial agent that has shown potential antifungal activity. The aims of this study were to discover the possible therapeutic targets of nitroxoline using an in silico approach, and to determine the in vitro antifungal activity of the drug against the fungal cell wall and cytoplasmic membrane. We explored the biological activity of nitroxoline using PASS, SwissTargetPrediction and Cortellis Drug Discovery Intelligence web tools. After confirmation, the molecule was designed and optimized in HyperChem software. GOLD 2020.1 software was used to predict the interactions between the drug and the target proteins. In vitro investigation evaluated the effect of nitroxoline on the fungal cell wall through sorbitol protection assay. Ergosterol binding assay was carried out to assess the effect of the drug on the cytoplasmic membrane. In silico investigation revealed biological activity with alkane 1-monooxygenase and methionine aminopeptidase enzymes, showing nine and five interactions in the molecular docking, respectively. In vitro results exhibited no effect on the fungal cell wall or cytoplasmic membrane. Finally, nitroxoline has potential as an antifungal agent due to the interaction with alkane 1-monooxygenase and methionine aminopeptidase enzymes, which are not the main human therapeutic targets. These results have potentially revealed a new biological target for the treatment of fungal infections. We also consider that further studies are required to confirm the biological activity of nitroxoline on fungal cells, mainly the confirmation of the alkB gene.
MeSH term(s)	Humans ; Antifungal Agents/pharmacology ; Molecular Docking Simulation ; Cytochrome P-450 CYP4A ; Aminopeptidases ; Methionine ; Fungi
Chemical Substances	nitroxoline (A8M33244M6) ; Antifungal Agents ; Cytochrome P-450 CYP4A (EC 1.14.15.3) ; Aminopeptidases (EC 3.4.11.-) ; Methionine (AE28F7PNPL)
Language	English
Publishing date	2023-06-30
Publishing country	France
Document type	Journal Article
ZDB-ID	1067006-3
ISSN	1773-0449 ; 1156-5233
ISSN (online)	1773-0449
ISSN	1156-5233
DOI	10.1016/j.mycmed.2023.101411
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Zs.A 3148: Show issues

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Article ; Online: Design of Multitarget Natural Products Analogs with Potential Anti-Alzheimer's Activity.

de Souza, Franciane Nunes / de Lima, Henrique Barros / de Souza, Lucilene Rocha / Oliveira, Gabrieli Santos / de Paula da Silva, Carlos Henrique Tomich / Pereira, Arlindo César Matias / da Silva Hage-Melim, Lorane Izabel

Current computer-aided drug design

2022 Volume 18, Issue 2, Page(s) 120–149

Abstract: Background: Alzheimer's disease (AD) is a neurodegenerative condition and the most common type of dementia among the elderly. The enzymes acetylcholinesterase (AChE) and nitric oxide synthase (NOS) have a pivotal role in the pathophysiology of this ... ...

Abstract	Background: Alzheimer's disease (AD) is a neurodegenerative condition and the most common type of dementia among the elderly. The enzymes acetylcholinesterase (AChE) and nitric oxide synthase (NOS) have a pivotal role in the pathophysiology of this disease. Objective: This study aimed to select medicinal plant-derived molecules with reported inhibition of AChE and design optimized molecules that could inhibit not only AChE, but also NOS, potentially increasing its efficacy against AD. Methods: 24 compounds were selected from the literature based on their known AChE inhibitory activity. Then, we performed molecular orbital calculations, maps of electrostatic potential, molecular docking study, identification of the pharmacophoric pattern, evaluation of pharmacokinetic and toxicological properties of these molecules. Next, ten analogs were generated for each molecule to optimize their effect where the best molecules of natural products had failed. Results: The most relevant correlation was between HOMO and GAP in the correlation matrix of the molecules' descriptors. The pharmacophoric group's derivation found the following pharmacophoric features: two hydrogen bond acceptors and one aromatic ring. The studied molecules interacted with the active site of AChE through hydrophobic and hydrogen bonds and with NOS through hydrogen interactions only but in a meaningful manner. In the pharmacokinetic and toxicological prediction, the compounds showed satisfactory results. Conclusion: The design of natural products analogs demonstrated good affinities with the pharmacological targets AChE and NOS, with satisfactory pharmacokinetics and toxicology profiles. Thus, the results could identify promising molecules for treating Alzheimer's disease.
MeSH term(s)	Acetylcholinesterase ; Aged ; Alzheimer Disease/drug therapy ; Biological Products/chemistry ; Biological Products/pharmacology ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Humans ; Molecular Docking Simulation
Chemical Substances	Biological Products ; Cholinesterase Inhibitors ; Acetylcholinesterase (EC 3.1.1.7)
Language	English
Publishing date	2022-04-11
Publishing country	United Arab Emirates
Document type	Journal Article
ISSN	1875-6697
ISSN (online)	1875-6697
DOI	10.2174/1573409918666220328141605
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Article ; Online: Identification of known drugs as potential SARS-CoV-2 Mpro inhibitors using ligand- and structure-based virtual screening.

Federico, Leonardo Bruno / Silva, Guilherme Martins / da Silva Hage-Melim, Lorane Izabel / Gomes, Suzane Quintana / Barcelos, Mariana Pegrucci / Galindo Francischini, Isaque Antônio / Tomich de Paula da Silva, Carlos Henrique

Future medicinal chemistry

2021 Volume 13, Issue 16, Page(s) 1353–1366

Abstract: Background: ...

Abstract	Background:
MeSH term(s)	Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; COVID-19/drug therapy ; Databases, Chemical ; Drug Evaluation, Preclinical ; Humans ; Ligands ; Molecular Docking Simulation ; Molecular Structure ; Protease Inhibitors/chemistry ; Protease Inhibitors/pharmacology ; Protein Binding ; SARS-CoV-2/drug effects ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/pharmacology ; Structure-Activity Relationship ; Viral Proteases/metabolism
Chemical Substances	Antiviral Agents ; Ligands ; Protease Inhibitors ; Small Molecule Libraries ; Viral Proteases (EC 3.4.-)
Language	English
Publishing date	2021-06-25
Publishing country	England
Document type	Journal Article
ISSN	1756-8927
ISSN (online)	1756-8927
DOI	10.4155/fmc-2021-0025
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Article: Chromatographic profile, in silico and in vivo study of the pharmacokinetic and toxicological properties of major constituent present in kefir, the kefiran.

Barros, Susy Érika de Lima / de Lima, Henrique Barros / Gonçalves, Leandra Karoline Alves / Correia, Lenir Cabral / Brito, Maiara de Fátima de Brito / Barcelos, Mariana Pegrucci / Silva, Guilherme Martins / da Silva, Carlos Henrique Tomich de Paula / da Costa, Rafael Garrett / Cruz, Rodrigo Alves Soares / Carvalho, José Carlos Tavares / da Silva Hage-Melim, Lorane Izabel

Toxicology research

2022 Volume 11, Issue 3, Page(s) 520–528

Abstract: Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to ... ...

Abstract	Kefiran is a polysaccharide present in kefir grains that have been widely explored due to its potential health benefits. The objective of this work was to characterize and quantify the components present in the ethanolic extract of milk kefir grains; to study its pharmacokinetic and toxicological properties in silico and evaluate the acute toxicity of the kefiran in zebrafish. The prediction of pharmacokinetic properties was performed by QikProp software. In silico toxicity assessment was performed using the DEREK (deductive estimate of risk from existing knowledge) software. In the chromatographic, kefiran was identified as the major component. Results showed that the kefiran had low human oral absorption and intestinal absorption its due poor solubility profile; low logP value, indicating its lipophilicity and the low MDCK and Caco-2 cells permability, and unable to cross the blood-brain barrier. Kefiran did not present any structural warning for in silico toxicity. In zebrafish, the dose of 2,000 mg/kg of kefiran produced nonsignificant alterations in the analyzed organs. It can be said then that kefiran has an acceptable degree of safety for use in the development of drugs or functional foods. Further research such as in vivo testing to confirm its pharmacological potential is currently underway.
Language	English
Publishing date	2022-05-31
Publishing country	England
Document type	Journal Article
ZDB-ID	2684701-2
ISSN	2045-4538 ; 2045-452X
ISSN (online)	2045-4538
ISSN	2045-452X
DOI	10.1093/toxres/tfac032
Database	MEDical Literature Analysis and Retrieval System OnLINE

2021 Volume 22, Issue 2, Page(s) 139–150

Abstract: Background: Alzheimer's disease is a progressive neurodegenerative process with multifactorial characteristics. This disease follows the natural aging process, affecting mainly people over 65 years. Pharmacotherapeutic treatment currently combats ... ...

Abstract	Background: Alzheimer's disease is a progressive neurodegenerative process with multifactorial characteristics. This disease follows the natural aging process, affecting mainly people over 65 years. Pharmacotherapeutic treatment currently combats symptoms related to cognitive function. Several targets have begun to attract the interest of the scientific community to develop new drug candidates which have better pharmacokinetic and lower toxicity parameters. Objective: The present study aims to design new candidates for acetylcholinesterase/β-secretase (AChE/BACE1) multitarget inhibitor drugs. Methods: 17 natural products were selected from the literature with anticholinesterase activity and 1 synthetic molecule with inhibitory activity for BACE1. Subsequently, the molecular docking study was performed, followed by the derivation of the pharmacophoric pattern and prediction of pharmacokinetic and toxicological properties. Finally, the hybrid prototype was designed. Results: All selected molecules showed interactions with their respective target enzymes. Derivation of the pharmacophoric pattern from molecules that interacted with the AChE enzyme resulted in 3 pharmacophoric regions: an aromatic ring, an electron-acceptor region and a hydrophobic region. The molecules showed good pharmacokinetic and toxicological results, showing no warnings of mutagenicity and/or carcinogenicity. After the hybridization process, three hybrid molecules were obtained, which showed inhibitory activity for both targets. Conclusion: It is concluded that research in the field of medicinal chemistry is advancing towards the discovery of new drug candidates that bring a better quality of life to patients with AD.
MeSH term(s)	Acetylcholinesterase ; Amyloid Precursor Protein Secretases/chemistry ; Aspartic Acid Endopeptidases/chemistry ; Humans ; Molecular Docking Simulation ; Quality of Life
Chemical Substances	Acetylcholinesterase (EC 3.1.1.7) ; Amyloid Precursor Protein Secretases (EC 3.4.-) ; Aspartic Acid Endopeptidases (EC 3.4.23.-)
Language	English
Publishing date	2021-10-04
Publishing country	United Arab Emirates
Document type	Journal Article
ZDB-ID	2227560-5
ISSN	1875-6166 ; 1871-5249
ISSN (online)	1875-6166
ISSN	1871-5249
DOI	10.2174/1871524922666220517110606
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Zs.A 5594: Show issues

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Article ; Online: In silico study of the mechanism of action, pharmacokinetic and toxicological properties of some N-methylanthranilates and their analogs.

Izabel da Silva Hage-Melim, Lorane / Curtolo Poiani, João Gabriel / Tomich de Paula da Silva, Carlos Henrique / Boylan, Fábio

Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association

2019 Volume 131, Page(s) 110556

Abstract: The in silico evaluation for the three previously synthesized compounds (Methyl (MMA), propyl (PMA) and isopropyl (IMA) N-methylanthranilate), MMA and IMA originally found in the leaf essential oil of Choisya ternata, provided a very good confirmation ... ...

Abstract	The in silico evaluation for the three previously synthesized compounds (Methyl (MMA), propyl (PMA) and isopropyl (IMA) N-methylanthranilate), MMA and IMA originally found in the leaf essential oil of Choisya ternata, provided a very good confirmation for the in vivo pharmacological results obtained with such compounds for a number of pharmacological targets. This manuscript dealt with their assessment in six pharmacological targets to understanding anti-inflammatory, antinociceptive, anxiolytic, antidepressant and anti-allergic activities using docking molecular as well as their pharmacokinetics and toxicological parameters prediction. The compound IMA seems to be the best one when all the combined parameters are put together. Interestingly this compound presented the best in vivo profile in previous studies by the group. Derivatives of the three original molecules were proposed. Overall the second modification (5-[2-(methoxycarbonyl)anilino]pentanoic acid, 5-[2-(propoxycarbonyl)anilino]pentanoic acid and 5-(2-{[(propan-2-yl)oxy]carbonyl}anilino)pentanoic acid) of all three original molecules was the one that achieved highest score in molecular docking and a better combination of the other parameters. Further research as in the obtaining of such derivatives via synthesis and their in vivo testing to confirm their higher pharmacological potential is currently on the way.
MeSH term(s)	Animals ; Binding Sites ; Humans ; Molecular Docking Simulation ; Protein Binding ; Proteins/chemistry ; Proteins/metabolism ; Rats ; Sheep ; ortho-Aminobenzoates/chemical synthesis ; ortho-Aminobenzoates/metabolism ; ortho-Aminobenzoates/pharmacokinetics ; ortho-Aminobenzoates/toxicity
Chemical Substances	Proteins ; ortho-Aminobenzoates
Language	English
Publishing date	2019-06-07
Publishing country	England
Document type	Journal Article
ZDB-ID	782617-5
ISSN	1873-6351 ; 0278-6915
ISSN (online)	1873-6351
ISSN	0278-6915
DOI	10.1016/j.fct.2019.06.003
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Zs.A 529: Show issues

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Article ; Online: Potential of the Compounds from

Batista, Mateus Alves / de Lima Teixeira Dos Santos, Abrahão Victor Tavares / do Nascimento, Aline Lopes / Moreira, Luiz Fernando / Souza, Indira Ramos Senna / da Silva, Heitor Ribeiro / Pereira, Arlindo César Matias / da Silva Hage-Melim, Lorane Izabel / Carvalho, José Carlos Tavares

Molecules (Basel, Switzerland)

2022 Volume 27, Issue 5

Abstract: Some significant compounds present in annatto are geranylgeraniol and tocotrienols. These compounds have beneficial effects against hyperlipidemia and chronic diseases, where oxidative stress and inflammation are present, but the exact mechanism of ... ...

Abstract	Some significant compounds present in annatto are geranylgeraniol and tocotrienols. These compounds have beneficial effects against hyperlipidemia and chronic diseases, where oxidative stress and inflammation are present, but the exact mechanism of action of such activities is still a subject of research. This study aimed to evaluate possible mechanisms of action that could be underlying the activities of these molecules. For this, in silico approaches such as ligand topology (PASS and SEA servers) and molecular docking with the software GOLD were used. Additionally, we screened some pharmacokinetic and toxicological parameters using the servers PreADMET, SwissADME, and ProTox-II. The results corroborate the antidyslipidemia and anti-inflammatory activities of geranylgeraniol and tocotrienols. Notably, some new mechanisms of action were predicted to be potentially underlying the activities of these compounds, including inhibition of squalene monooxygenase, lanosterol synthase, and phospholipase A
MeSH term(s)	Bixaceae ; Carotenoids ; Diterpenes ; Dyslipidemias ; Molecular Docking Simulation ; Plant Extracts/pharmacology ; Tocotrienols/pharmacology
Chemical Substances	Diterpenes ; Plant Extracts ; Tocotrienols ; Carotenoids (36-88-4) ; annatto (6PQP1V1B6O) ; geranylgeraniol (AIA02AJA3A)
Language	English
Publishing date	2022-02-28
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	1413402-0
ISSN	1420-3049 ; 1431-5165 ; 1420-3049
ISSN (online)	1420-3049
ISSN	1431-5165 ; 1420-3049
DOI	10.3390/molecules27051584
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Article ; Online: Potential beneficial effects of kefir and its postbiotic, kefiran, on child food allergy.

Barros, Susy Érika de Lima / Rocha, Caique Dos Santos / de Moura, Mayara Storel Beserra / Barcelos, Mariana Pegrucci / da Silva, Carlos Henrique Tomich de Paula / Hage-Melim, Lorane Izabel da Silva

Food & function

2021 Volume 12, Issue 9, Page(s) 3770–3786

Abstract: Food allergies are known as the public health problem, affecting people of all age groups, but more commonly in babies and children, with consequences for nutritional status and quality of life. The increase in the consumption of healthy foods has ... ...

Abstract	Food allergies are known as the public health problem, affecting people of all age groups, but more commonly in babies and children, with consequences for nutritional status and quality of life. The increase in the consumption of healthy foods has consequently led to an increased demand for functional foods with specific health benefits. Thus, the pharmaceutical industry's interest in natural products has grown every time and is therefore considered as an alternative to synthetic drugs. Kefir has been outstanding for several years as promising in the manufacture of various pharmaceutical products, due to its nutritional and therapeutic properties for the treatment of many diseases. Currently, a wide variety of new functional foods are appearing on the market, representing an important segment. Postbiotics, for example, has stood out for being a product with action similar to probiotics, without offering side effects. The kefiran is the postbiotic from kefir that promotes potential beneficial effects on food allergy from the intestinal microbiome to the immune system. In this context, it is necessary to know the main promoting component of this functional effect. This review compiles the benefits that kefir, and especially its postbiotic, kefiran, can bring to food allergy. In addition, it serve as a subsidy for studies on the development of innovative nutraceutical products, including the use of kefiran as an alternative therapy in food allergy.
MeSH term(s)	Animals ; Child ; Child, Preschool ; Food Hypersensitivity/complications ; Food Hypersensitivity/epidemiology ; Food Hypersensitivity/physiopathology ; Food Hypersensitivity/therapy ; Functional Food ; Gastrointestinal Microbiome ; Humans ; Immune System/physiology ; Infant ; Kefir/analysis ; Kefir/microbiology ; Polysaccharides/administration & dosage ; Polysaccharides/therapeutic use ; Probiotics ; Risk Factors
Chemical Substances	Polysaccharides ; kefir grain polysaccharide (8L821V6V99)
Language	English
Publishing date	2021-05-12
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	2612033-1
ISSN	2042-650X ; 2042-6496
ISSN (online)	2042-650X
ISSN	2042-6496
DOI	10.1039/d0fo03182h
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Article ; Online: Allosteric Modulators of Potential Targets Related to Alzheimer's Disease: a Review.

Silva, Guilherme Martins / Barcelos, Mariana Pegrucci / Poiani, João Gabriel Curtolo / Hage-Melim, Lorane Izabel da Silva / da Silva, Carlos Henrique Tomich de Paula

ChemMedChem

2019 Volume 14, Issue 16, Page(s) 1467–1483

Abstract: Among neurodegenerative disorders, Alzheimer's disease (AD) is the most common type of dementia, and there is an urgent need to discover new and efficacious forms of treatment for it. Pathological patterns of AD include cholinergic dysfunction, increased ...

Abstract	Among neurodegenerative disorders, Alzheimer's disease (AD) is the most common type of dementia, and there is an urgent need to discover new and efficacious forms of treatment for it. Pathological patterns of AD include cholinergic dysfunction, increased β-amyloid (Aβ) peptide concentration, the appearance of neurofibrillary tangles, among others, all of which are strongly associated with specific biological targets. Interactions observed between these targets and potential drug candidates in AD most often occur by competitive mechanisms driven by orthosteric ligands that sometimes result in the production of side effects. In this context, the allosteric mechanism represents a key strategy; this can be regarded as the selective modulation of such targets by allosteric modulators in an advantageous manner, as this may decrease the likelihood of side effects. The purpose of this review is to present an overview of compounds that act as allosteric modulators of the main biological targets related to AD.
MeSH term(s)	Allosteric Regulation/drug effects ; Alzheimer Disease/drug therapy ; Amyloid Precursor Protein Secretases/antagonists & inhibitors ; Animals ; Glycogen Synthase Kinase 3 beta/antagonists & inhibitors ; Humans ; Ligands ; Phosphodiesterase 4 Inhibitors/therapeutic use ; Receptors, Cell Surface/agonists ; Receptors, Cell Surface/antagonists & inhibitors
Chemical Substances	Ligands ; Phosphodiesterase 4 Inhibitors ; Receptors, Cell Surface ; Glycogen Synthase Kinase 3 beta (EC 2.7.11.1) ; Amyloid Precursor Protein Secretases (EC 3.4.-)
Language	English
Publishing date	2019-08-01
Publishing country	Germany
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2218496-X
ISSN	1860-7187 ; 1860-7179
ISSN (online)	1860-7187
ISSN	1860-7179
DOI	10.1002/cmdc.201900299
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