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, w

Despite the G protein-coupled receptors (GPCRs) being the largest family of signalling proteins at the surface of cells, their potential to be targeted in cancer therapy is still under-utilised. This review highlights the contribution of these receptors to the process of oncogenesis and points to some likely challenges that might be encountered in targeting them. GPCR-signalling pathways are often complex and can be tissue-specific. Cancer cells hijack these communication networks to their proliferative advantage. The role of selected GPCRs in the different hallmarks of cancer is examined to highlight the complexity of targeting these receptors for therapeutic benefit. Our

The study aims to reveal the degree of application of the alternative evaluation strategy in social studies in public education in the Kingdom of Saudi Arabia. It also aims to identify the opinions of experts on how to implement this. The study adopted the mixed methodology, which represented in the descriptive-analytical method, and qualitative methods through the grounded theory. The study used two tools namely: a questionnaire for assessments of social studies teachers and semi-structured interview questions. The results of the study showed a medium degree of appreciation for the application of alternative evaluation strategies by social studies teachers in general education with an average of (2.28). The results also showed that ther

There is a continuous and massive need for newer cephalosporins that should have resistance against β-lactamases and can be used orally. An approach of using cephalexin, as a well-studied and potent antibacterial compound is considered to prepare new designed derivatives.  These derivatives include the incorporation of amino acid moiety linked through an amide bond with the α-amino group of cephalexin. Certain aliphatic amino acids were used, such as glycine, alanine, valine and proline. The chemical structures of these derivatives were confirmed by IR spectroscopy and elemental analyses. All the synthesized compounds were subjected for preliminary evaluation of antimicrobial activity using well diffusion method, against certa

This research focuses on improvement of the corrosion behaviour of commercial pure titanium (Ti) grade II when exposed to Hank’s solution through different surface treatments. The disc shape of titanium samples were constructed to be divided according to their surface treatment. The first experimental group the Ti sample was exposed to computer numerical control (CNC) fiber laser machine. Whereas, the other experimental group the Ti sample was only coated with Polyetherketon keton (PEKK) by using carbon dioxide (CO2) laser technique while the last experimental group the Ti sample was treated with CNC fiber laser followed by PEKK coating by using CO2 laser technique. All were compared with the untreated control group. The electrochemical a

Background: Abdominoplasty is one of the commonest surgical procedures that performed for those patients who had skin laxity, strive and muscle rectur diastasis. Combined using of liposuction and abdominoplasty it can give better result than traditional abdominoplasty with fear complications. Patient and Method: A total number of 25 female patients with age ranging between 27-55 years were underwent lipoabdominoplasty. With extensive liposuction of abdominal wall and selective undermining together with muscle plication. All of our patients had body mass index more than 30. Patients satisfaction and complication were documented postoperatively. Result: All of our patients had no Major complications and the postoperative period passed unevent