Evolution, structure, and drug-metabolizing activity of mammalian prenylcysteine oxidases. [PDF]
Prenylcysteine oxidases (PCYOXs) metabolize prenylated cysteines produced by protein degradation. They utilize oxygen as co-substrate to produce free cysteine, an aldehyde, and hydrogen peroxide through the unusual oxidation of a thioether bond.
Barone M+4 more
europepmc +3 more sources
An extended substrate spectrum of the proton organic cation antiporter and relation to other cation transporters [PDF]
Abstract Most central nervous system (CNS) active drugs are organic cations, which need carrier proteins for efficient transfer through the blood–brain barrier (BBB). A genetically still unidentified proton organic cation (H+/OC) antiporter is found in several tissues, including endothelial cells of the BBB.
Cauzar Ali Khan+3 more
wiley +2 more sources
A combination of repurposed drugs reduces the proliferation and viability of glioblastoma cells [PDF]
Background: Glioblastoma multiforme (GBM) is a malignant primary brain tumour with high rates of recurrence. The tumour is characterized by high molecular diversity.
Sachkova, Aleksandra
core +1 more source
Gene regulation and epigenotype in Friedreich's ataxia [PDF]
Friedreich??????s ataxia (FRDA) is known to be provoked by an abnormal GAA-repeat expansion located in the first intron of the FXN gene. As a result of the GAA expansion, patients exhibit low levels of FXN mRNA, leading to FRDA.
Rothe, Nadine, Rothe, Nadine
core +2 more sources
Monoamine oxidase-A modulates apoptotic cell death induced by staurosporine in human neuroblastoma cells [PDF]
Monoamine oxidases (MAOs) are mitochondrial enzymes which control the levels of neurotransmitters in the brain and dietary amines in peripheral tissues via oxidative deamination. MAO has also been implicated in cell signalling. In this study, we describe
Billett E. E.+7 more
core +1 more source
Polymyxins and quinazolines are LSD1/KDM1A inhibitors with unusual structural features [PDF]
Because of its involvement in the progression of several malignant tumors, the histone lysine-specific demethylase 1 (LSD1) has become a prominent drug target in modern medicinal chemistry research.
Ciossani, Giuseppe+11 more
core +2 more sources
Epigenetic Mechanisms Regulate Stem Cell Expressed Genes Pou5f1 and Gfra1 in a Male Germ Cell Line [PDF]
Male fertility is declining and an underlying cause may be due to environment-epigenetic interactions in developing sperm, yet nothing is known of how the epigenome controls gene expression in sperm development.
A Buageaw+94 more
core +7 more sources
Discrimination Between Drug Abuse and Medical Therapy : Case report of a tranylcypromine overdose-related fatality [PDF]
Tranylcypromine is an effective antidepressant from the class of monoamine oxidase inhibitors and is structurally related to amphetamine. However, reports differ regarding the potential metabolism of tranylcypromine to amphetamine and methamphetamine ...
Akhgari, Maryam+3 more
core +3 more sources
Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A) [PDF]
We report a series of tranylcypromine analogues containing a fluorine in the cyclopropyl ring. A number of compounds with additional m- or p- substitution of the aryl ring were micromolar inhibitors of the LSD1 enzyme.
Al-Jamal, Wafa T.+10 more
core +2 more sources
Anti-diabetic effect of a monoamine oxidase inhibitor (tranylcypromine) in rats with poorly-controlled blood glucose levels: A potential and novel therapeutic option for diabetes [PDF]
Purpose: To determine the anti-diabetic effect of a monoamine oxidase inhibitor (tranylcypromine) in sulphonyl urea-refractory rats with poorly-controlled blood glucose levels.Methods: Alloxan-induced diabetic Wistar rats were assigned to two groups (30 ...
Dong, Zhichun+3 more
core +2 more sources