Letters in Drug Design & Discovery - Volume 21, Issue 5, 2024

Background: Genetic studies support a key role for RORγ and RORα in the differentiation of proinflammatory Th17 cells, and a growing body of evidence suggests a pathogenic role for Th17 in several autoimmune diseases, including MS, rheumatoid arthritis, inflammatory bowel disease, type I diabetes, and psoriasis. RORγ antagonists have been shown to suppress Th17 differentiation and delay the onset of disease in an Read More

Anticancer drug development is complex and multi-factorial, demanding robust drug evaluative architecture in experimental and preclinical studies. To increase the number of drug licensing, biochemical, pharmacological, technical and economic changes (balance and integration) in evaluative systems should be focused in labs throughout the world. Despite great progress, treatment breakthroughs and drug industry Read More

Cancers remain the leading cause of death worldwide, despite significant advances in their diagnosis and treatment. The inadequacy and ineffectiveness of standard treatments (chemotherapy, radiotherapy, and surgery), their severe side effects, and the resistance of tumor cells to chemotherapeutics have forced researchers to investigate alternative therapeutic strategies. Magnetic nanoparticles (MNPs) have been Read More

Background: Nowadays, infectious diseases caused by bacteria are one of the major risks for the human population worldwide. Antimicrobial resistance determined the necessity to develop both, new drugs and therapeutic approaches as alternatives to antibiotics and novel methods to detect bacteria. Aptamers have revealed their potential in combating antimicrobial infections. Aptamers are small singlestranded DNA o Read More

Introduction: The Epidermal growth factor receptor is a transmembrane glycoprotein that belongs to the ErbB family of tyrosine kinase receptors, which includes four EGFR members ErbB1 (HER1/ErbB1), ErbB2 (HER2/neu), ErbB3 (HER3), and ErbB4 (HER4). Methods: Amplification of EGFR corresponds to tyrosine kinase autophosphorylation that activates a downstream signalling pathway involved in regulating tumorigenesi Read More

Background: It has been shown that drugs used parenterally cause errors in immunosuppressant concentrations measured by LC-MS / MS method. It is yet unknown whether this measurement error is due to drug-drug interaction or analytical interference. Objective: The aim of this study is to investigate the possible interaction and inhibition concentrations of broad-spectrum antibiotics (ertapenem, meropenem, imipenem) wit Read More

Background: Silymarin is a flavonoid utilised in liver dysfunction for years; new studies have emphasised its potential utility as a therapy for nanoparticulate targeting in many other disorders. In order to establish the product quality of such compounds, researchers have been trying to develop a robust method of analysis, but the methods developed till now are too expensive and time-consuming. Here we proposed qua Read More

Background: Asthma is a common chronic respiratory disorder characterized by inflammation and remodeling of the airways. Aims: This study aimed to identify the inhibitory effects of Huatan Tongluo decoction (HTTLD) on airway inflammation and associated remodeling mechanisms. Methods: Mice were immunized with ovalbumin (OVA) for 8 weeks to generate chronic asthma mouse models (CAS), which were rando Read More

Background: Cancer is a serious concern in developing countries. Due to various worldwide impacts, it has surpassed coronary disorders becoming the leading cause of mortality. In cancer progression, the involvement of RORs (retinoic acid receptor-related orphan receptors) has gained attention in the search for versatile agents. Thiazole has the potential to be used as a scaffold in the development of anticancer drugs. Read More

Background: The deficiency of vitamin D is a global concern affecting individuals of all age groups. Insufficient exposure to sunlight and disease conditions can lead to cholecalciferol (vitamin D3) deficiency. Objective: Cholecalciferol is a lipophilic crystalline molecule, and it is highly susceptible to degradation under environmental conditions, including light, temperature, and oxygen, and its degradation rate is high in the low pH r Read More

Background: In this article, a series of novel oxazolidinone derivatives containing dithiocarbamate moieties have been designed and synthesized. Materials and Methods: Their antibacterial activities were measured against Staphylococcus aureus, vancomycin-resistant Enterococcus faecium (VREF), linezolid-resistant Enterococcus faecalis (LREF) and Streptococcus agalactiae (GBS) by minimal inhibitory concentration (MIC) as Read More

Introduction: Marine microbes are known to produce novel bioactive compounds. In this work, the bacterium Actinoalloteichus cyanogriseus, AU-RM-4, isolated from marine soil sediment, capable of producing high amounts of black extracellular melanin pigment when grown on anaerobic actinomycetes agar is reported. The maximum melanin production was approximately 2.5 mg/mL. Methods: The melanin pigment was r Read More

Background: Glioblastoma is one of the most aggressive types of tumors, which occurs in the central nervous system, and has a high fatality rate. Among the cellular changes observed in glioblastoma is the overexpression of certain anti-apoptotic proteins, such as Bcl-xL. Recently, the alkaloid sanguinarine (SAN) was identified as a potent inhibitor of this class of proteins. Objective: In this work, the antitumor activity of ten aryl-i Read More

Background: Multiple myeloma (MM) is a hematological malignancy of plasma cells that produce a monoclonal immunoglobulin protein. Despite significant advances in the treatment of MM, currently available therapies are associated with toxicity and resistance. As a result, there is an increasing demand for novel, effective therapeutics. Inhibition of histone deacetylases (HDACs) is emerging as a potential method for tr Read More

Background: Polo-like kinase 1 (PLK1) is an important target for anti-cancer drugs. A series of novel 2,4-diarylaminopyrimidine derivatives (DAPDs) as PLK1 inhibitors (PLKIs) with remarkable activities have been reported recently. Methods: A systemically computational study was performed on these DAPDs, including threedimensional quantitative structure-activity relationship (3D-QSAR) modeling, molecular docking, and molec Read More