Protein arginine methyltransferases (PRMTs) play important roles in transcription, splicing, DNA damage repair, RNA biology, and cellular metabolism. Thus, PRMTs have been attractive targets for various diseases. In this study, we reported the design and synthesis of a potent pan-inhibitor for PRMTs that tethers a thioadenosine and various substituted guanidino groups through a propyl linker. Compound II757 exhibits a half-maximal inhibition concentration (IC50) value of 5 to 555 nM for eight tested PRMTs, with the highest inhibition for PRMT4 (IC50 = 5 nM). The kinetic study demonstrated that II757 competitively binds at the SAM binding site of PRMT1. Notably, II757 is selective for PRMTs over a panel of other methyltransferases, which can serve as a general probe for PRMTs and a lead for further optimization to increase the selectivity for individual PRMT.
Summary First: The importance of the study and the need for it: The society is composed of an integrated unit of groups and institutions that seek to achieve a specific goal within a system of salary, and the family remains the most influential institutions on the individual and the unity of society, with the roles and responsibilities of the individual and society, and through the continuation and strength of other social organizations derive their ability On the other hand, any break-up in the institution of the family is reflected negatively on the cohesion of society and its interdependence, and the causes of this disintegration vary from society to another, but family problems remain the main factor in obtaining it. Second: Study Ob
... Show MoreRice is a major staple food for more than two thirds of the world population. Pathogenesis-related proteins-10 (PR10) have a range of 154 to 163 amino acid with molecular weight ~ 17 kDa. They are acidic and generally intracellular and cytosolic proteins accumulate in plants in response to biotic and abiotic stresses. In the present study, a PR10 gene and its corresponding protein were characterized in O. sativa, O. barthii, O. glaberrima, O. glumipatula, O. meridionalis, O. nivara, O. rufipogon and O. punctata. The results revealed a narrow range of variation at both DNA and protein levels in all examined species except O. glumipatula. The latter showed a relatively
... Show MoreMolar conductance (Λ) of ionizable side chains amino acids, lysine (Lys) and arginine (Arg) with dehydroascorbic acid (DHA) in water and in NaCl solutions was measured at temperatures range 298 K to 313 K. The limited molar conductance (Λo) and the constant of the ions association (KA) are calculated using the Shedlovsky techniques. The dynamic radius of the concerned ion (R) is calculated by used Stokes–Einstein relation. The heat of association, the Gibbs free energy, the change of entropy and activation energy (ΔHo/ kJ mol-1, ΔGo/ kJ mol-1, ΔSo/J K-1 mol-1, and ΔES/ kJ mol-1) respectively), also calculated. The data show increases the molar conductance with increas
... Show MoreSARS-CoV-2 stands for severe acute respiratory syndrome coronavirus 2 which is the causative agent of spreading coronavirus disease 2019 that is known as COVID-19 pandemic, the disease leads to severe acute respiratory illness. Matrix metalloproteinases- 9 (MMP-9) plays several important physiological functions. This enzyme could also be implicated in the "cytokine storm" in some way, which may represent one of the possible scianrios during coronavirus infection, in addition to its role in the mechanism of lung fibrosis on molecular basis.. The tissue inhibitors of metalloproteinase (TIMPs) are well characterized for controlling the activity of MMPs in extracellular matrix remodeling. They also considered as signaling molecules anal
... Show MoreBackground: Inhibitor development and HCV are considered the most serious complications of hemophilia treatment. Many factors may increase the risk of complications which include: type of hemophilia, age of the patient, age of onset, duration of the disease, & number of replacement per month. Patients and methods: A descriptive study included 200 patients less than 20 years of age admitted to the Hemophilia Center in Children Welfare Teaching Hospital , medical city in Baghdad , their data ( ag , sex , disease onset and duration , severity of hemophilia ) were collected over 8 months period from 1st January to 31st August 2006. Mixing tests and serology tests for HCV and HBV were performed for all patien
... Show MoreAbstract The results of the effect of the type of feed showed a significant increase (P≤0.01) for palm fronds DM during the incubation period of 7, 14, 21 days, a high Mnp superiority in its incubation 14 days, and a significant superiority of Laccase in its incubation 21 days, while the effect of the enzyme concentration on DM was higher Significant at a concentration of 10% of the enzyme, and the interaction between the type of feed and the enzyme together showed a highly significant increase in the treated palm fronds Laccase and Lip in the incubation period of 7 days, and the treated palm fronds Mnp during incubation 14 days. %, 15% for the interaction between the type of coarse feed and the concentration of the enzyme
... Show MoreThe Covid-19 virus disease has been shown to affect numerous organs and systems including the liver. The study aimed to compare lipid profiles and liver enzyme levels in individuals who had recovered from Covid-19 infection. To achieve the study objectives, liver Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT), Alkaline phosphatase (ALP), Random Blood Sugar (RBS) and Lipid profile which include cholesterol, High-Density Lipoprotein (HDL), Triglycerides (T.G), Low-Density Lipoprotein (LDL), and Very low-density Lipoprotein (VLDL) were determined.
One hundred twenty serum samples were obtained, of which fifty samples were utilized as the control healthy persons (not affected by COVID) and seventy samples came f
... Show MoreThe aim of this research to show the role of some enzymes in pathological mechanism of rheumatoid arthritis (RA) disease. Sixty patients with RA and matched number of apparently healthy volunteers were included in the study. Spectrophotometric methods were used to determine Peroxy nitrite (ONOO), Nitric oxide (NO), Nitric oxide synthase activity (NOS) cycloxygenase-2 activity (COX-2), glutathione peroxidase (GPX) activity and superoxide dismutase (SOD) activity in serum of both groups. Colorimetric assay kits were used to determine Iron. Rheumatoid factor (RF) was determined using Imuno-Latex kit. ONOO, NO levels, and NOS activity were significantly higher in the patients compared to the control group. Conversely, Iron level, SOD
... Show MoreCholinesterases are among the most efficient enzymes known. They are divided into two groups: acetylcholinesterase (AChE) involved in the hydrolysis of the neurotransimitter acetylcholine, and butyrylcholinesterase (BChE) of unknown function. Several crystal structures of the former have shown that the active site is located at the bottom of a deep and narrow gorge. Human BChE has attracted attention because it can hydrolyze toxic esters and nerve agents. Here we analyze the complexes of cholinesterase with soman by describing the 3D geometry of the complex, the active site, the changes happened through the inhibition and provide a description for the mechanism of inhibition. Soman undergoes degradation in the active site of the AChE and B
... Show MoreBackground: Smoking is considering a major risk factor for development and progression of periodontal disease. Investigations regarding the association between smoking and periodontal disease have consistently demonstrated negative periodontal effects and greater probabilities of established periodontal disease among smokers in comparison with non smokers. The purpose of this study was to evaluate the effects of smoking on periodontal health status and on the salivary levels of alkaline phosphatase (ALP), lactate dehydrogenase (LDH) and creatine kinase (CK), and to correlate the clinical parameters of periodontal health with the biochemical findings in smokers and non-smokers. Materials and methods: Unstimulated saliva sample was collected
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