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https://www.readbyqxmd.com/read/29792714/docking-screens-for-dual-inhibitors-of-disparate-drug-targets-for-parkinson-s-disease
#1
Mariama Jaiteh, Alexey Zeifman, Marcus Saarinen, Per Svenningsson, José M Brea, Maria Isabel Loza, Jens Carlsson
Modulation of multiple biological targets with a single drug can lead to synergistic therapeutic effects and has been demonstrated to be essential for efficient treatment of CNS disorders. However, rational design of compounds that interact with several targets is very challenging. Here, we demonstrate that structure-based virtual screening can guide the discovery of multi-target ligands of unrelated proteins relevant for Parkinson's disease. A library with 5.4 million molecules was docked to crystal structures of the A2A adenosine receptor (A2AAR) and monoamine oxidase B (MAO-B)...
May 24, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29788780/isoform-selectivity-of-harmine-conjugated-1-2-3-triazoles-against-human-monoamine-oxidase
#2
Saqlain Haider, Manal Alhusban, Narayan D Chaurasiya, Babu L Tekwani, Amar G Chittiboyina, Ikhlas A Khan
AIM: There is little information available on the monoamine oxidase isoform selectivity of N-alkyl harmine analogs, which exhibit a myriad of activities including monoamine oxidase isoform A (MAO-A), tyrosine-phosphorylation-regulated kinase (DYRK1A) and cytotoxicity to several select cancer cell lines. RESULTS: Compounds 3e and 4c exhibited an IC50 of 0.83 ± 0.03 and 0.43 ± 0.002 μM against MAO-A and an IC50 of 0.26 ± 0.04 and 0.36 ± 0.001 μM against MAO-B, respectively...
May 23, 2018: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29769405/%C3%AE-synuclein-stimulation-of-monoamine-oxidase-b-and-legumain-protease-mediates-the-pathology-of-parkinson-s-disease
#3
Seong Su Kang, Eun Hee Ahn, Zhentao Zhang, Xia Liu, Fredric P Manfredsson, Ivette M Sandoval, Susov Dhakal, P Michael Iuvone, Xuebing Cao, Keqiang Ye
Dopaminergic neurodegeneration in Parkinson's disease (PD) is associated with abnormal dopamine metabolism by MAO-B (monoamine oxidase-B) and intracellular α-Synuclein (α-Syn) aggregates, called the Lewy body. However, the molecular relationship between α-Syn and MAO-B remains unclear. Here, we show that α-Syn directly binds to MAO-B and stimulates its enzymatic activity, which triggers AEP (asparagine endopeptidase; legumain) activation and subsequent α-Syn cleavage at N103, leading to dopaminergic neurodegeneration...
May 16, 2018: EMBO Journal
https://www.readbyqxmd.com/read/29760163/%C3%A2-safinamide-for-parkinson-s-disease
#4
(no author information available yet)
▼ Safinamide (Xadago - Zambon S.p.A) is a monoamine-oxidase B (MAO-B) inhibitor licensed as add-on therapy for people with idiopathic Parkinson's disease who are experiencing motor fluctuations with levodopa.1 Currently there is no cure for Parkinson's disease and drugs are used to reduce motor symptoms and improve daily activities.2,3 Here, we review the evidence for this MAO-B inhibitor.
May 2018: Drug and Therapeutics Bulletin
https://www.readbyqxmd.com/read/29758567/synthesis-and-in-vitro-evaluation-of-2-heteroarylidene-1-tetralone-derivatives-as-monoamine-oxidase-inhibitors
#5
Klaudia T Amakali, Lesetja J Legoabe, Anél Petzer, Jacobus P Petzer
The present study investigates the human monoamine oxidase (MAO) inhibition properties of a series of twelve 2-heteroarylidene-1-tetralone derivatives. Also included are related cyclohexylmethylidene, cyclopentylmethylidene and benzylidene substituted 1-tetralones. These compounds are related to the 2-benzylidene-1-indanone class of compounds which has previously been shown to inhibit the MAOs, with specificity for the MAO-B isoform. The target compounds were synthesised by the Claisen-Schmidt condensation between 7-methoxy-1-tetralone or 1-tetralone, and various aldehydes, under acid (hydrochloric acid) or base (potassium hydroxide) catalysis...
May 14, 2018: Drug Research
https://www.readbyqxmd.com/read/29748850/from-aggression-to-autism-new-perspectives-on-the-behavioral-sequelae-of-monoamine-oxidase-deficiency
#6
REVIEW
Marco Bortolato, Gabriele Floris, Jean C Shih
The two monoamine oxidase (MAO) enzymes, A and B, catalyze the metabolism of monoamine neurotransmitters, such as serotonin, norepinephrine, and dopamine. The phenotypic outcomes of MAO congenital deficiency have been studied in humans and animal models, to explore the role of these enzymes in behavioral regulation. The clinical condition caused by MAOA deficiency, Brunner syndrome, was first described as a disorder characterized by overt antisocial and aggressive conduct. Building on this discovery, subsequent studies were focused on the characterization of the role of MAOA in the neurobiology of antisocial conduct...
May 10, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29747278/-the-associations-between-comorbidity-and-exacerbation-risk-in-patients-with-chronic-obstructive-pulmonary-disease
#7
Y L Huang, B Mao, J Mim, G H Li, Y Q Zheng, L H Wu, S J Wang, B Qu, J J Fu
Objective: To study the association between comorbidity and acute exacerbation risk in patients with chronic obstructive pulmonary disease (COPD). Methods: This was a prospective cohort study with 64 stable COPD patients included. There were 64 males and 18 females with an average age of (68±9) years. Clinical characteristics, the number and type of comorbidities were recorded, and Charlson comorbidity index (CCI) was calculated. The patients were interviewed by phone calls every 3 months since baseline in which the number of acute exacerbations was recorded until 12 months...
May 12, 2018: Chinese Journal of Tuberculosis and Respiratory Diseases
https://www.readbyqxmd.com/read/29714148/synthesis-and-evaluation-of-2-benzylidene-1-tetralone-derivatives-for-monoamine-oxidase-inhibitory-activity
#8
Klaudia T Amakali, Lesetja Jan Legoabe, Anel Petzer, Jacobus P Petzer
Chalcone has been identified as a promising lead for the design of monoamine oxidase (MAO) inhibitors. This study attempted to discover potent and selective chalcone-derived MAO inhibitors by synthesising a series consisting of various cyclic chalcone derivatives. The cyclic chalcones were selected based on the possibility that their restricted structures would confer a higher degree of MAO isoform selectivity, and included the following chemical classes: 1-indanone, 1-tetralone, 1-benzosuberone, chromone, thiochromone, 4-chromanone and 4-thiochromanone...
May 1, 2018: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29713806/an-inducible-mao-b-mouse-model-of-parkinson-s-disease-a-tool-towards-better-understanding-basic-disease-mechanisms-and-developing-novel-therapeutics
#9
REVIEW
Manish Chamoli, Shankar J Chinta, Julie K Andersen
Several studies have suggested that increases in astrocytic monoamine oxidase B (MAO-B) levels in conjunction with Parkinson's disease (PD) may contribute to subsequent neuropathology associated with the disorder. MAO-B inhibitors are currently widely used as symptomatic therapeutics for PD and, although somewhat controversial, these drugs may also exhibit disease-modifying properties. To obtain a better understanding of the potential role of MAO-B in disease neuropathology, we created an inducible astrocyte-specific transgenic MAO-B mouse model...
April 30, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29697034/nitrocatechol-derivatives-of-chalcone-as-inhibitors-of-monoamine-oxidase-and-catechol-o-methyltransferase
#10
Idalet Engelbrecht, Jacobus P Petzer, Anel Petzer
The efficacy of L-dopa in the treatment of Parkinson's disease depends on its metabolic conversion to dopamine in the brain, however extensive peripheral metabolism of L-dopa diminishes its availability for uptake into the brain. L-Dopa is extensively decarboxylated in the gastrointestinal tract and peripheral tissues by aromatic L-amino acid decarboxylase (AADC), and AADC inhibitors are thus frequently combined with L-dopa therapy. When AADC is inhibited, 3-O-methylation catalysed by catechol-O-methyltransferase (COMT) becomes a dominant metabolic pathway for L-dopa, and COMT inhibitors may thus also be used as adjuncts to L-dopa in Parkinson's disease...
April 26, 2018: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/29671581/novel-mao-b-hit-inhibitors-using-multidimensional-molecular-modeling-approaches-and-application-of-binary-qsar-models-for-prediction-of-their-therapeutic-activity-and-toxic-effects
#11
Yusuf Serhat Is, Serdar Durdagi, Busecan Aksoydan, Mine Yurtsever
Monoamine oxidase (MAO) enzymes MAO-A and MAO-B play a critical role in the metabolism of monoamine neurotransmitters. Hence, MAO inhibitors are very important for the treatment of several neurodegenerative diseases such as Parkinson's disease (PD), Alzheimer's disease (AD), and amyotrophic lateral sclerosis (ALS). In this study, 256750 molecules from Otava Green Chemical Collection were virtually screened for their binding activities as MAO-B inhibitors. Two hit molecules were identified after applying different filters such as high docking scores and selectivity to MAO-B, desired pharmacokinetic profile predictions with binary QSAR models...
April 19, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29648817/tight-binding-inhibition-of-human-monoamine-oxidase-b-by-chromone-analogs-a-kinetic-crystallographic-and-biological-analysis
#12
Joana Reis, Nicola Manzella, Fernando Cagide, Jeanne Mialez-Perez, Eugenio Uriarte, Angelo Parini, Fernanda M Borges, Claudia Binda
Monoamine oxidase B (MAO-B) is a validated drug target for Parkinson's disease. Chromone derivatives were identified as novel potent and reversible MAO-B inhibitors and herewith we report on a crystallographic and biochemical analysis to investigate their inhibition mechanism. The crystal structures of human MAO-B in complex with three chromone analogs bearing different substituents on the exocyclic aromatic ring (determined at 1.6-1.8 Å resolution) showed that they all bind in the active site cavity of the protein with the chromone moiety located in front of the FAD cofactor...
April 12, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29578580/mao-b-and-comt-genetic-variations-associated-with-levodopa-treatment-response-in-patients-with-parkinson-s-disease
#13
Tiago Furtado Sampaio, Erinaldo Ubirajara Damasceno Dos Santos, Gessica Dayane Cordeiro de Lima, Rute Salgues Gueiros Dos Anjos, Ronaldo Celerino da Silva, Amdore Guescel C Asano, Nadja Maria Jorge Asano, Sergio Crovella, Paulo Roberto Eleutério de Souza
The most commonly used Parkinson's disease (PD) treatment is the replacement of dopamine by its levodopa precursor (l-dopa). Monoamine oxidase-B (MAO-B) and catechol-o-methyl transferase (COMT) are enzymes involved in the metabolism and regulation of dopamine availability. In our study we investigated the possible relation among selected single-nucleotide polymorphisms (SNPs) in the MAO-B (rs1799836) and COMT (rs4680) genes and the therapeutic response to levodopa (l-dopa). A total of 162 Brazilian patients from the Pro-Parkinson service of Clinics Hospital of Pernambuco diagnosed with sporadic PD and treated with levodopa were enrolled...
March 26, 2018: Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29570223/an-investigation-of-the-monoamine-oxidase-inhibition-properties-of-pyrrolo-3-4-f-indole-5-7-dione-and-indole-5-6-dicarbonitrile-derivatives
#14
Zhanna V Chirkova, Mariya V Kabanova, Sergey I Filimonov, Igor G Abramov, Anél Petzer, Idalet Engelbrecht, Jacobus P Petzer, Kyrill Yu Suponitsky, Alexander V Veselovsky
Hit, Lead & Candidate Discovery In recent studies, we have shown that pyrrolo[3,4-f]indole-5,7-dione and indole-5,6-dicarbonitrile derivatives act as good potency in vitro inhibitors of the monoamine oxidase (MAO) enzymes. To expand on these series and to further derive structure-activity relationships (SARs) for MAO inhibition, in the present study we synthesized additional homologs and related analogs of these chemical classes. Analyzes of the MAO inhibition properties of the synthesized compounds show that among the pyrrolo[3,4-f]indole-5,7-dione derivatives good potency MAO inhibitors exist as exemplified by 10, which possesses IC50 values for the inhibition of MAO-A and MAO-B of 0...
March 23, 2018: Drug Development Research
https://www.readbyqxmd.com/read/29569037/monoamine-oxidase-b-inhibitors-in-the-treatment-of-parkinson-s-disease-clinical-pharmacological-aspects
#15
REVIEW
Peter Riederer, Thomas Müller
This invited narrative review emphasizes the role of MAO-B inhibition in the drug portfolio for dopamine substitution in patients with Parkinson's disease. Neuronal and glial MAO-B inhibition contributes to more stable levels of dopamine and other biogenic amines in the synaptic cleft. Accordingly, symptomatic effects of MAO-B inhibition for a limited amelioration of impaired motor behaviour and wearing-off phenomena in patients with Parkinson's disease are well proven, even when MAO-B inhibitors are only applied together with dopamine agonists...
March 22, 2018: Journal of Neural Transmission
https://www.readbyqxmd.com/read/29561824/nutraceutical-potential-of-phenolics-from-brava-and-mansa-extra-virgin-olive-oils-on-the-inhibition-of-enzymes-associated-to-neurodegenerative-disorders-in-comparison-with-those-of-picual-and-cornicabra
#16
María Figueiredo-González, Patricia Reboredo-Rodríguez, Carmen González-Barreiro, Alegría Carrasco-Pancorbo, Jesús Simal-Gándara, Beatriz Cancho-Grande
The increasing interest in the Mediterranean diet is based on the protective effects against several diseases, including neurodegenerative disorders. Polyphenol-rich functional foods have been proposed to be unique supplementary and nutraceutical treatments for these disorders. Extra-virgin olive oils (EVOOs) obtained from 'Brava' and 'Mansa', varieties recently identified from Galicia (northwestern Spain), were selected for in vitro screening to evaluate their capacity to inhibit key enzymes involved in Alzheimer's disease (AD) (acetylcholinesterase (AChE), butyrylcholinesterase (BuChE) and 5-lipoxygenase (5-LOX)), major depressive disorder (MDD) and Parkinson's disease (PD) (monoamine oxidases: h MAO-A and h MAO-B respectively)...
March 21, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29552556/structure-activity-relationship-analysis-of-3-phenylcoumarin-based-monoamine-oxidase-b-inhibitors
#17
Sanna Rauhamäki, Pekka A Postila, Sanna Niinivehmas, Sami Kortet, Emmi Schildt, Mira Pasanen, Elangovan Manivannan, Mira Ahinko, Pasi Koskimies, Niina Nyberg, Pasi Huuskonen, Elina Multamäki, Markku Pasanen, Risto O Juvonen, Hannu Raunio, Juhani Huuskonen, Olli T Pentikäinen
Monoamine oxidase B (MAO-B) catalyzes deamination of monoamines such as neurotransmitters dopamine and norepinephrine. Accordingly, small-molecule MAO-B inhibitors potentially alleviate the symptoms of dopamine-linked neuropathologies such as depression or Parkinson's disease. Coumarin with a functionalized 3-phenyl ring system is a promising scaffold for building potent MAO-B inhibitors. Here, a vast set of 3-phenylcoumarin derivatives was designed using virtual combinatorial chemistry or rationally de novo and synthesized using microwave chemistry...
2018: Frontiers in Chemistry
https://www.readbyqxmd.com/read/29552078/isolation-and-biological-evaluation-of-prenylated-flavonoids-from-maclura-pomifera
#18
Yerkebulan Orazbekov, Mohamed A Ibrahim, Serjan Mombekov, Radhakrishnan Srivedavyasasri, Ubaidilla Datkhayev, Bauyrzhan Makhatov, Narayan D Chaurasiya, Babu L Tekwani, Samir A Ross
Phytochemical analysis of the ethanolic extract of Maclura pomifera fruits yielded four new compounds ( I - IV ) along with eleven known compounds ( V - XV ). The crude extract exhibited significant activity towards cannabinoid receptors (CB1: 103.4% displacement; CB2: 68.8% displacement) and possibly allosteric interaction with δ and μ opioid receptors (-49.7 and -53.8% displacement, resp.). Compound I was found to be possibly allosteric for κ and μ opioid receptors (-88.4 and -27.2% displacement, resp...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
https://www.readbyqxmd.com/read/29550344/hplc-uv-assays-for-evaluation-of-inhibitors-of-mono-and-diamine-oxidases-using-novel-phenyltetrazolylalkanamine-substrates
#19
Kira Mergemeier, Matthias Lehr
Recently, we have described an HPLC-UV assay for the evaluation of inhibitors of plasma amine oxidase (PAO) using 6-(5-phenyl-2H-tetrazol-2-yl)hexan-1-amine (4) as a new type of substrate. Now we studied, whether this compound or homologues of it can also function as substrate for related amine oxidases, namely diamine oxidase (DAO), monoamine oxidase A (MAO A) and monoamine oxidase B (MAO B). Among these substances, 4 was converted by DAO with the highest rate. The best substrate for MAO A and B was 4-(5-phenyl-2H-tetrazol-2-yl)butan-1-amine (2)...
May 15, 2018: Analytical Biochemistry
https://www.readbyqxmd.com/read/29549278/-18-f-av-1451-in-parkinson-s-disease-with-and-without-dementia-and-in-dementia-with-lewy-bodies
#20
Ruben Smith, Michael Schöll, Elisabet Londos, Tomas Ohlsson, Oskar Hansson
Mixed pathologies of α-synuclein, β-amyloid and tau are relatively common in Parkinson's disease (PD) and Dementia with Lewy Bodies (DLB). We therefore wanted to study the retention patterns of 18 F-AV-1451 in PD, PD-dementia (PDD), and DLB. To do this 44 healthy controls, 11 non-demented patients with PD, 18 patients with PDD, and six patients with DLB underwent MRI and 18 F-AV-1451 PET scanning and cognitive testing. We found that parietal 18 F-AV-1451 retention was increased in patients with DLB compared to controls and PD patients, while 18 F-AV-1451 uptake was reduced in the substantia nigra in PDD...
March 16, 2018: Scientific Reports
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