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.
Background: Recent research indicates that persistent inflammatory responses may contribute to the rise of diabetic nephropathy (DN) and diabetic cardiovascular disease (DCVD) in type 2 diabetes mellitus patients (DM2). Numerous molecules associated with inflammation and angiogenesis have been implicated in the development and progression of DN and DCVD, respectively. Methods: The subjects were separated into five groups: healthy controls (n= 25), type 2 diabetes mellitus patients (n= 30), type 2 diabetes mellitus patients with nephropathy DN (n= 30), and type 2 diabetes mellitus patients with cardiovascular disease DCVD (n= 30). The blood levels of irisin, IL-8, HbA1C, urea, and creatinine were determined. Results: In current study there w
... Show MoreMultiple sclerosis (MS) is a neurodegenerative disorder with various clinical types. Glial fibrillary acidic protein (GFAP) is significantly elevated in the cerebrospinal fluid (CSF) of MS patients compared with that of healthy controls. The aim of this study is to evaluate serum levels of GFAP in relation to disease activity in relapsing-remitting MS patients and to compare them with those of healthy controls. Method: This study involved 58 MS patients of relapsing-remitting MS (RRMS) type, 22 in an active stage of the disease and 36 in remission, and 50 healthy individuals as age- and sex-matched controls. Blood samples were taken from the patients at the MS Clinic of the Baghdad Teaching Hospital, and the serum levels of GFAP were determ
... Show MoreEndothelin-1 (ET-1) is a potent vasoconstrictor hormone that has been identified as an important factor
responsible for the development of cardiovascular dysfunctions. ET-1 exerts its vasoconstrictor activity
through two pharmacologically distinct receptors, ETA and ETB that are found in vascular smooth muscle
cells (VSMCs) and the vasodilator activity through an ETB receptor located on endothelial cells. This study
aimed to show the impact of 1µM L-arginine (LA), 100µM tetrahydrobiopterin (BH4), and their combined
effect on ET-1 activity in both lead-treated and lead-untreated rat aortic rings. This means, investigating how
endothelial dysfunction reverses the role of nitric oxide precursor and cofa
Abstract Background: Timely diagnosis of periodontal disease is crucial for restoring healthy periodontal tissue and improving patients’ prognosis. There is a growing interest in using salivary biomarkers as a noninvasive screening tool for periodontal disease. This study aimed to investigate the diagnostic efficacy of two salivary biomarkers, lactate dehydrogenase (LDH) and total protein, for periodontal disease by assessing their sensitivity in relation to clinical periodontal parameters. Furthermore, the study aimed to explore the impact of systemic disease, age, and sex on the accuracy of these biomarkers in the diagnosis of periodontal health. Materials and methods: A total of 145 participants were categorized into three groups based
... Show MoreDiabetes mellitus can be defined as a metabolic disorder disease .Complication of diabetes are due to diabetic nephropathy .This study was done in vitro to study the effect of different concentrations of erlotinib inhibitor ( tyrosine kinase inhibitor) on electrolyte levels (MgâºÂ²,CaâºÂ²,Naâº) in sera of Iraqi patients with newly diagnosis type2 diabetes and diabetic nephropathy in addition to find the best percentage inhibition for utilizing different concentrations from erlotinib (6.97x10â»â·, 9.30x10â»â· ,1.16x10â»â¶,1.39x10â»â¶ ,1.62x10â»âµ )molar on electrolyte levels . This study was conducted in The National Diabetes Ce
... Show MoreThe present study was designed in the aquaculture and fish nutrition research aquarium in the College of Veterinary Medicine/Baghdad University from a period 1/3 to 1/6/2013 to investigate the toxicity of the herbicide glyphosate aqua on Barbus sharpeyi fish. Fish fingerlings were used with average weight between 10 – 15 gm to measure the (LC50), and 200 fingerlings were used to know the acute and chronic toxic effect for the herbicide. The fingerlings were randomly distributed as 10 fish for each aquarium. Fish were divided into four treatments and control group (without addition of herbicide). The first processing with a concentration of 0.415 mg/L for a duration of exposure 90 days, the second processing group with a concentration 0.
... Show MoreA pot culture experiment was conducted at the greenhouse of soil and water resources department in College of Agriculture, University of Baghdad in Abo-Ghraib at season 2009-2010 to investigate the effects of using foliar application of some macro and micronutrients in induce antioxidant enzymes in wheat grown under salt stress . Doar85 planted under three levels of salt stress, and three combinations of foliar application were used from nutrients (K+ Ca) at 3000 and 1500 mg.L-1 respectively, and (Fe + Zn + Mn) at 30, 20, and 10 mg.L-1 respectively , and ( K+ Ca) + (Fe+ Zn + Mn). The results showed that increasing levels of sodium chloride in the irrigation of water significantly increased at p<0.05 level SOD and POD activity
... Show MoreThe main objectives of this pepper are to introduce new classes. We have attempted to obtain coefficient estimates, radius of convexity, Distortion and Growth theorem and other related results for the classes