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.
Fire is one of the most critical risks devastating to human life and property. Therefore, humans make different efforts to deal with fire hazards. Many techniques have been developed to assess fire safety risks. One of these methods is to predict the outbreak of a fire in buildings, and although it is hard to predict when a fire will start, it is critical to do so to safeguard human life and property. This research deals with evaluating the safety risks of the existing building in the city of Samawah/Iraq and determining the appropriateness of these buildings in terms of safety from fire hazards. Twelve parameters are certified based on the National Fire Protection Association (NFPA20
Amorphization of drug has been considered as an attractive approach in improving drug solubility and bioavailability. Unlike their crystalline counterparts, amorphous materials lack the long-range order of molecular packing and present the highest energy state of a solid material. Co-amorphous systems (CAM) are an innovative formulation technique by where the amorphous drugs are stabilized via powerful intermolecular interactions by means of a low molecular co-former.
This review highlights the different approaches in the preparation of co-amorphous drug delivery system, the proper selection of the co-formers. In addition, the recent advances in characterization, Industrial scale and formulation will be discussed.
Fetal growth restriction is a significant contributor to fetal morbidity and mortality. In addition, there are heightened maternal risks associated with surgical operations and their accompanying dangers. Monitoring fetal development is a crucial objective of prenatal care and effective methods for early diagnosis of Fetal growth restriction, allowing prompt management and timely intervention to improve the outcomes. Screening for Fetal growth restriction can be achieved via many modalities; it can be medical, biochemical, or radiological. Some recommended combining more than one for better outcomes. Currently, there is inconsistency about the best method of Fetal growth restriction screening. In this review, a comprehensive
... Show MoreThe past several years have seen an increase in awareness of the pervasiveness of medications as pollutants in the aquatic environment. The main reason for concern regarding the release of pharmaceuticals into the environment is the possibility that biological agents may become opposing to them. The development of precise and reliable analytical techniques for pharmaceutical determination in a range of samples is necessary for their safe use in the pharmaceutical industry and medical treatments. This review offers a summary of chromatographic techniques for identifying and quantifying the examination of pharmaceuticals in a range of environmental samples. Both the general public and the scientific community are currently very intere
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Bivariate time series modeling and forecasting have become a promising field of applied studies in recent times. For this purpose, the Linear Autoregressive Moving Average with exogenous variable ARMAX model is the most widely used technique over the past few years in modeling and forecasting this type of data. The most important assumptions of this model are linearity and homogenous for random error variance of the appropriate model. In practice, these two assumptions are often violated, so the Generalized Autoregressive Conditional Heteroscedasticity (ARCH) and (GARCH) with exogenous varia
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