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Tranylcypromine

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https://www.readbyqxmd.com/read/27893888/potential-neuroprotective-effects-of-an-lsd1-inhibitor-in-retinal-ganglion-cells-via-p38-mapk-activity
#1
Takayuki Tsutsumi, Keiichiro Iwao, Hideki Hayashi, Tomoko Kirihara, Takahiro Kawaji, Toshihiro Inoue, Shinjiro Hino, Mitsuyoshi Nakao, Hidenobu Tanihara
Purpose: The epigenetic mechanisms associated with ocular neurodegenerative diseases remain unclear. The present study aimed to determine the role of lysine-specific demethylase 1 (LSD1), which represses transcription by removing the methyl group from methylated lysine 4 of histone H3, in retinal ganglion cell (RGC) survival, and to investigate the details of the neuroprotective mechanism of tranylcypromine, a major LSD1 inhibitor. Methods: The authors evaluated whether tranylcypromine contributes to neuronal survival following stress-induced damage using primary cultured rat RGCs and in vivo N-methyl-D-aspartate (NMDA)-induced excitotoxicity...
November 1, 2016: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/27885768/gram-scale-synthesis-of-chiral-cyclopropane-containing-drugs-and-drug-precursors-with-engineered-myoglobin-catalysts-featuring-complementary-stereoselectivity
#2
Priyanka Bajaj, Gopeekrishnan Sreenilayam, Vikas Tyagi, Rudi Fasan
Engineered hemoproteins have recently emerged as promising systems for promoting asymmetric cyclopropanations, but variants featuring predictable, complementary stereoselectivity in these reactions have remained elusive. In this study, a rationally driven strategy was implemented and applied to engineer myoglobin variants capable of providing access to 1-carboxy-2-aryl-cyclopropanes with high trans-(1R,2R) selectivity and catalytic activity. The stereoselectivity of these cyclopropanation biocatalysts complements that of trans-(1S,2S)-selective variants developed here and previously...
November 25, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27715253/an-overview-of-analytical-methods-for-the-determinationof-monoamine-oxidase-inhibitors-in-pharmaceutical-formulations-and-biological-fluids
#3
Cafer Saka
Monoamine oxidase inhibitors (MAOIs) were the first type of antidepressant developed. MAOIs elevate the levels of norepinephrine, serotonin, and dopamine by inhibiting an enzyme called monoamine oxidase. They are also used in the treatment of Parkinson's disease, tuberculosis, and several other disorders. Therefore, it is very important to develop efficient analytical methods for monitoring and management. There are two isoforms of monoamine oxidase, MAO-A and MAO-B. In this article, analyses of MAOIs in pharmaceutical formulations and biological fluids were reviewed from 2000 to the present, including all types of chromatographic, spectrophotometric, electrophoretic, and voltammetric techniques, focusing on isoniazid, tranylcypromine, moclobemide, rasagiline, and selegiline...
October 7, 2016: Critical Reviews in Analytical Chemistry
https://www.readbyqxmd.com/read/27479862/lsd1-biologic-roles-and-therapeutic-targeting
#4
Alba Maiques-Diaz, Tim Cp Somervaille
LSD1 (KDM1A; BHC110; AOF2) was the first protein reported to exhibit histone demethylase activity and has since been shown to have multiple essential roles in mammalian biology. Given its enzymatic activity and its high-level expression in many human malignancies, a significant recent focus has been the development of pharmacologic inhibitors. Here we summarize structural and biochemical knowledge of this important epigenetic regulator, with a particular emphasis on the functional and preclinical studies in oncology that have provided justification for the evaluation of tranylcypromine derivative LSD1 inhibitors in early phase clinical trials...
August 2016: Epigenomics
https://www.readbyqxmd.com/read/27457692/evaluation-of-herb-drug-interaction-of-a-polyherbal-ayurvedic-formulation-through-high-throughput-cytochrome-p450-enzyme-inhibition-assay
#5
Subrata Pandit, Satyajyoti Kanjilal, Anshumali Awasthi, Anika Chaudhary, Dipankar Banerjee, B N Bhatt, Avinash Narwaria, Rahul Singh, Kakoli Dutta, Manu Jaggi, Anu T Singh, Neena Sharma, Chandra Kant Katiyar
ETHNOPHARMACOLOGICAL RELEVANCE: Arishtas are Ayurvedic formulation made with decoction of herbs. Arjunarishta formulation is being used in Ayurveda for cardio-protective activity. Ashwagandharishta formulation possesses antioxidant, anti-atherosclerotic and anti-stress properties. Ridayarishta, a novel empirical formulation was prepared using combination of selected ingredients from these two formulations to support healthy heart functions and to reduce stress. AIM OF THE STUDY: Aim of the Study was to investigate herb-drug interaction (HDI) of Ridayarishta formulation through human hepatic cytochrome P450 (CYP450) enzyme inhibition assay...
July 25, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27405777/forced-chromatin-looping-raises-fetal-hemoglobin-in-adult-sickle-cells-to-higher-levels-than-pharmacologic-inducers
#6
Laura Breda, Irene Motta, Silvia Lourenco, Chiara Gemmo, Wulan Deng, Jeremy W Rupon, Osheiza Y Abdulmalik, Deepa Manwani, Gerd A Blobel, Stefano Rivella
Overcoming the silencing of the fetal γ-globin gene has been a long-standing goal in the treatment of sickle cell disease (SCD). The major transcriptional enhancer of the β-globin locus, called the locus control region (LCR), dynamically interacts with the developmental stage-appropriate β-type globin genes via chromatin looping, a process requiring the protein Ldb1. In adult erythroid cells, the LCR can be redirected from the adult β- to the fetal γ-globin promoter by tethering Ldb1 to the human γ-globin promoter with custom-designed zinc finger (ZF) proteins (ZF-Ldb1), leading to reactivation of γ-globin gene expression...
August 25, 2016: Blood
https://www.readbyqxmd.com/read/27256596/rebalancing-gene-haploinsufficiency-in-vivo-by-targeting-chromatin
#7
Filomena Gabriella Fulcoli, Monica Franzese, Xiangyang Liu, Zhen Zhang, Claudia Angelini, Antonio Baldini
Congenital heart disease (CHD) affects eight out of 1,000 live births and is a major social and health-care burden. A common genetic cause of CHD is the 22q11.2 deletion, which is the basis of the homonymous deletion syndrome (22q11.2DS), also known as DiGeorge syndrome. Most of its clinical spectrum is caused by haploinsufficiency of Tbx1, a gene encoding a T-box transcription factor. Here we show that Tbx1 positively regulates monomethylation of histone 3 lysine 4 (H3K4me1) through interaction with and recruitment of histone methyltransferases...
2016: Nature Communications
https://www.readbyqxmd.com/read/27105957/significant-inhibitory-impact-of-dibenzyl-trisulfide-and-extracts-of-petiveria-alliacea-on-the-activities-of-major-drug-metabolizing-enzymes-in-vitro-an-assessment-of-the-potential-for-medicinal-plant-drug-interactions
#8
J Murray, D Picking, A Lamm, J McKenzie, S Hartley, C Watson, L Williams, H Lowe, R Delgoda
Dibenzyl trisulfide (DTS) is the major active ingredient expressed in Petiveria alliacea L., a shrub widely used for a range of conditions, such as, arthritis, asthma and cancer. Given its use alone and concomitantly with prescription medicines, we undertook to investigate its impact on the activities of important drug metabolizing enzymes, the cytochromes P450 (CYP), a key family of enzymes involved in many adverse drug reactions. DTS and seven standardized extracts from the plant were assessed for their impact on the activities of CYPs 1A2, 2C19, 2C9, 2D6 and 3A4 on a fluorometric assay...
June 2016: Fitoterapia
https://www.readbyqxmd.com/read/27063220/an-improved-substrate-cocktail-for-assessing-direct-inhibition-and-time-dependent-inhibition-of-multiple-cytochrome-p450s
#9
Zhong-Hua Chen, Su-Xing Zhang, Na Long, Li-Shan Lin, Tao Chen, Fei-Peng Zhang, Xue-Qin Lv, Pei-Zhen Ye, Ning Li, Ke-Zhi Zhang
AIM: The substrate cocktail is frequently used to evaluate cytochrome P450 (CYP) enzyme-mediated drug interactions and potential interactions among the probe substrates. Here, we re-optimized the substrate cocktail method to increase the reliability and accuracy of screening for candidate compounds and expanded the method from a direct CYP inhibition assay to a time-dependent inhibition (TDI) assay. METHODS: In the reaction mixtures containing human liver microsome (0...
May 2016: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/27062244/tranylcypromine-a-lysine-specific-demethylase-1-lsd1-inhibitor-suppresses-lesion-growth-and-improves-generalized-hyperalgesia-in-mouse-with-induced-endometriosis
#10
Qunyan Sun, Ding Ding, Xishi Liu, Sun-Wei Guo
BACKGROUND: Growing evidence indicates that endometriosis is an epigenetic disease. Encouragingly, histone deacetylases (HDACs) and DNA methyltransferases have been shown to be promising targets by numerous in vitro studies. However, only a few studies have shown promising effects of HDAC inhibition in preclinical studies in endometriosis. While lysine-specific demethylase 1 (LSD1) is recently found to be aberrantly expressed in endometriosis, and that the treatment of endometriotic stromal cells with tranylcypromine (TC), an LSD1 inhibitor, significantly reduced cellular proliferation, cell cycle progression, and invasiveness, the in vivo effect of TC treatment is currently lacking...
2016: Reproductive Biology and Endocrinology: RB&E
https://www.readbyqxmd.com/read/26955970/effects-of-monoamine-oxidase-inhibition-on-the-reinforcing-properties-of-low-dose-nicotine
#11
Tracy T Smith, Laura E Rupprecht, Samantha N Cwalina, Matthew J Onimus, Sharon E Murphy, Eric C Donny, Alan F Sved
The Food and Drug Administration (FDA) has the authority to regulate cigarette smoke constituents, and a reduction in nicotine content might benefit public health by reducing the prevalence of smoking. Research suggests that cigarette smoke constituents that inhibit monoamine oxidase (MAO) may increase the reinforcing value of low doses of nicotine. The aim of the present experiments was to further characterize the impact of MAO inhibition on the primary reinforcing and reinforcement enhancing effects of nicotine in rats...
August 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/26917855/maois-does-the-evidence-warrant-their-resurrection
#12
David Menkes, Peter Bosanac, David Castle
OBJECTIVE: The place of monoamine oxidase inhibitors (MAOIs) in psychiatry is reviewed, and the question posed as to whether they are now justifiably disregarded by prescribers. METHOD: Multiple databases (PubMed, Medline, Embase, Cochrane) were interrogated to provide an overview regarding the use, efficacy and toxicity of MAOIs. Data regarding funded use of these agents in New Zealand were obtained from PHARMAC. RESULTS: Evidence supports the use of MAOIs in major depressive disorder, certain anxiety disorders and, to lesser extent, bipolar depression...
August 2016: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/26881714/irreversible-lsd1-inhibitors-application-of-tranylcypromine-and-its-derivatives-in-cancer-treatment
#13
REVIEW
Yi C Zheng, Bin Yu, Guo Z Jiang, Xue J Feng, Peng X He, Xiao Y Chu, Wen Zhao, Hong M Liu
Due to the increasing costs and time consuming for new drug discovery, a large number of pharmaceutical firms have chosen to modify the existing drug molecules for repositioning candidates with new or improved properties, especially those with severe adverse effects, thereby accelerating the drug discovery process. Such strategy has witnessed its success with several examples reported. As the first identified histone lysine specific demethylase, lysine specific demethylase 1 (LSD1) is classified as a member of monoamine oxidase (MAO) superfamily, and specifically removes mono- and dimethylated histone 3 lysine 4 (H3K4) and H3 lysine 9 (H3K9)...
2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/26872725/the-histone-demethylase-lsd1-is-a-novel-oncogene-and-therapeutic-target-in-oral-cancer
#14
Yanling Wang, Yumin Zhu, Qiong Wang, Huijun Hu, Zhongwu Li, Dongmiao Wang, Wei Zhang, Bin Qi, Jinhai Ye, Heming Wu, Hongbing Jiang, Laikui Liu, Jianrong Yang, Jie Cheng
The histone demethylase LSD1 functions as a key pro-oncogene and attractive therapeutic target in human cancer. Here we sought to interrogate the oncogenic roles of LSD1 in OSCC tumorigenesis and therapeutic intervention by integrating chemical-induced OSCC model, genetic and pharmacological loss-of-function approaches. Our data revealed that aberrant LSD1 overexpression in OSCC was significantly associated with tumor aggressiveness and shorter overall survival. Increased abundance of LSD1 was detected along with disease progression in DMBA- or 4NQO-induced OSCC animal models...
April 28, 2016: Cancer Letters
https://www.readbyqxmd.com/read/26748182/the-effects-of-lsd1-inhibition-on-self-renewal-and-differentiation-of-human-induced-pluripotent-stem-cells
#15
Hong-Jie Yan, Shu-Yan Zhou, Yang Li, Hui Zhang, Chun-Yan Deng, Hui Qi, Fu-Rong Li
Human induced pluripotent stem cells (hiPSCs) are capable of unlimited self-renewal and can generate nearly all cells in the body. Changes induced by different LSD1 activities on the regulation of hiPSC self-renewal and differentiation and the mechanism underlying such changes were determined. We used two different LSD1 inhibitors (phenelzine sulfate and tranylcypromine) and RNAi technique to inhibit LSD1 activity, and we obtained hiPSCs showing 71.3%, 53.28%, and 31.33% of the LSD1 activity in normal hiPSCs...
January 15, 2016: Experimental Cell Research
https://www.readbyqxmd.com/read/26702542/discovery-of-a-novel-inhibitor-of-histone-lysine-specific-demethylase-1a-kdm1a-lsd1-as-orally-active-antitumor-agent
#16
Paola Vianello, Oronza A Botrugno, Anna Cappa, Roberto Dal Zuffo, Paola Dessanti, Antonello Mai, Biagina Marrocco, Andrea Mattevi, Giuseppe Meroni, Saverio Minucci, Giulia Stazi, Florian Thaler, Paolo Trifiró, Sergio Valente, Manuela Villa, Mario Varasi, Ciro Mercurio
We report the stereoselective synthesis and biological activity of a novel series of tranylcypromine (TCPA) derivatives (14a-k, 15, 16), potent inhibitors of KDM1A. The new compounds strongly inhibit the clonogenic potential of acute leukemia cell lines. In particular three molecules (14d, 14e, and 14g) showing selectivity versus MAO A and remarkably inhibiting colony formation in THP-1 human leukemia cells, were assessed in mouse for their preliminary pharmacokinetic. 14d and 14e were further tested in vivo in a murine acute promyelocytic leukemia model, resulting 14d the most effective...
February 25, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/26599973/cytochrome-p450-inhibition-potential-of-new-psychoactive-substances-of-the-tryptamine-class
#17
Julia Dinger, Campbell Woods, Simon D Brandt, Markus R Meyer, Hans H Maurer
New psychoactive substances (NPS) are not tested for their cytochrome P450 (CYP) inhibition potential before consumption. Therefore, this potential was explored for tryptamine-derived NPS (TDNPS) including alpha-methyl tryptamines (AMTs), dimethyl tryptamines (DMTs), diallyl tryptamines (DALTs), and diisopropyl tryptamines (DiPTs) using test substrates preferred by the Food and Drug Administration in a cocktail assay. All tested TDNPS with the exception of DMT inhibited CYP2D6 activity with IC50 values below 100μM...
January 22, 2016: Toxicology Letters
https://www.readbyqxmd.com/read/26555748/partial-dedifferentiation-of-murine-radial-glia-type-neural-stem-cells-by-brn2-and-c-myc-yields-early-neuroepithelial-progenitors
#18
Raffaela Bung, Philipp Wörsdörfer, Marc Christian Thier, Kathrin Lemke, Martina Gebhardt, Frank Edenhofer
Direct cell conversion developed into an important paradigm for generating cells with enhanced differentiation capability. We combined a transcription-factor-based cell fate conversion strategy with the use of pharmacological compounds to derive early neuroepithelial progenitor cells from developmentally more restricted radial glia-type neural stem cells. By combining the small molecules CHIR99021, Tranylcypromine, SB431542 and valproic acid with viral transduction of the transcription factor c-Myc and the POU domain transcription factor Brn2, we dedifferentiated radial glia-type neural stem cells into an early neuroepithelial progenitor cell state within 6 days...
April 10, 2016: Journal of Molecular Biology
https://www.readbyqxmd.com/read/26521853/novel-tranylcypromine-hydroxylcinnamic-acid-hybrids-as-lysine-specific-demethylase-1-inhibitors-with-potent-antitumor-activity
#19
Yan Han, Chunlei Wu, Haifeng Lv, Na Liu, Huaying Deng
Novel tranylcypromine/hydroxylcinnamic acid hybrids 15a, b, and 19a-l were designed and synthesized by connecting tranylcypromine with hydroxylcinnamic acid, and their biological activities were evaluated. The in vitro assay of their inhibitory activities against lysine-specific demethylase 1 (LSD1) showed that most of the target compounds displayed high potency with IC50 values ranging from submicromolar to single-digit micromolar levels. In particular, compound 19l had robust, selective LSD1 inhibitory activity, which was obviously higher than the inhibitory activity against homologues monoamine oxidase-A (MAO-A) and MAO-B, respectively...
2015: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/26479223/efficacy-of-tranylcypromine-in-bipolar-depression-a-systematic-review
#20
REVIEW
Willemijn T Heijnen, Jürgen De Fruyt, André I Wierdsma, Pascal Sienaert, Tom K Birkenhäger
OBJECTIVE: Currently, there is a paucity of treatment options with limited efficacy for bipolar depression. The monoamine oxidase inhibitor tranylcypromine might be an effective form of treatment. The current systematic review reassesses the efficacy and safety of tranylcypromine in bipolar depression. METHODS: For this systematic review comparing tranylcypromine with placebo or active comparators in bipolar depression, relevant randomized controlled trials were identified from systematic searches of PubMed, EMBASE, and Cochrane library databases...
December 2015: Journal of Clinical Psychopharmacology
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