Current Medicinal Chemistry - Online First

The molecular mechanisms and causes of primary sclerosis cholangitis (PSC) post-liver transplantation are still unclear. PSC is a progressive cholestatic hepatobiliary disease that happens in about 25% of patients post-liver transplantation and requires re-transplantation. Nicotinamide adenine dinucleotide phosphate oxidase (NADPH oxidase or Nox) is a family of transmembrane proteins whose main function is produci Read More

In most advanced cancers, standard medical treatments are generally employed. With the emergence of Antibody-Drug Conjugates (ADCs), more optimal therapeutic methods have become available for treating tumors. ADC is composed of a monoclonal antibody that targets a specific antigen and a cytotoxic payload, which conjugates via the synthetic linkers. Therefore, ADC combines the accurate targeting of monoclonal anti Read More

The melanoma incidence has been increasing over the past three decades, with a disproportionately high fraction of in situ tumors. The diagnosis of melanoma at its earliest stages can be challenging. The detectability of tumor melanocytes in the dermis is of key importance for distinguishing in situ from invasive melanomas. In this review, a total of 475 melanomas diagnosed as in situ tumors by hematoxylin and eosin staining Read More

Introduction This work provides preclinical in vitro studies of an innovative antimicrobial agent named pyridosept, belonging to the quaternary bis-ammonium salts and synthesized on the base of pyridoxine. Since the wide spread of pathogens with tolerance to both antibiotics and antiseptics challenges the development of new antimicrobials providing high efficiency against fungi and microorganisms with multiple resistance. Read More

Background Myocardial infarction (MI) is a common critical syndrome in the late development of cardiovascular diseases (CVDs), and traditional Chinese Medicine (TCM) treatment has become an essential branch in this field. Objective This study aimed to use bibliometric methods to examine the research trajectory of TCM treatment of MI from 2007 to 2024 from a multidimensional perspective and analyse its characteristics, Read More

Aims We aimed to develop Ferroptosis-Related Gene (FRG) signatures to predict overall survival (OS) along with disease-free survival (DFS) in individuals with colorectal cancer (CRC). Background Prediction of CRC prognosis is challenging. Ferroptosis constitutes a newly reported kind of cell death, and its association with CRC prognosis remains unexplored. Objective This research endeavored to establish a prognostic risk sig Read More

Recently, increasing attention has been directed toward nutraceuticals, natural substances extracted from plants, fruits, or cereals. These compounds are well-known for their antibacterial, anti-inflammatory, antioxidant, and antitumor properties, with the latter being the primary focus of this review. The use of nutraceuticals, both as standalone treatments and in combination with standard chemotherapy, has been exte Read More

Cyclin-dependent kinases that are responsible for cell cycle control, have been studied for over 30 years as therapeutic targets for the treatment of cancer and inflammation. In the past twenty years, their activities in various viral infections have been investigated in the search of novel therapeutic strategies in the treatment of viral infections. The interest in evaluating the antiviral activity of cyclin-dependent kinase inhib Read More

Introduction G-quadruplexes (G4s) are non-classical high-level structures that are formed by DNA/RNA sequences and have been a promising target for developing antitumor drugs. However, it is still a challenge to find a ligand that binds to a particular G4 with selectivity. Telomeric multimeric G4s are more accessible for screening for specific ligands due to their higher-order structure compared with telomeric mono Read More

Introduction/Objectives Escherichia coli strains are known to cause various gastrointestinal disorders, with Shiga toxin 2, a potent cytotoxin, being a key virulence factor contributing to disease severity. Targeting Shiga toxin 2 presents a promising approach for therapeutic intervention in controlling E. coli O157 infections. This study aims to explore natural and synthetic inhibitors as potential therapeutic agents against Shig Read More

Background Calix[n]arenes have attracted great attention due to their biocompatibility and superior stability. When the necessary functional groups are attached to these compounds, they may have the potential to target tumor tissues. Benzimidazoles are among the anticancer drugs discovered in recent years. Aim The aim of this study was to design and synthesise a series of calix[4]arenes-benzimidazoles. For comparison purpo Read More

Lipids play a variety of roles in living systems. They are a source of extremely high energy and a part of almost all signaling and biological processes. Despite the liver being the hub of lipid metabolism, lipid metabolism occurs across the human body. Any perturbation in the lipid metabolism or lipid storage systems can lead to diseases or disorders that can hamper the normal functioning of the human body. Lipids Read More

With the escalation of viral infections in recent decades, including the COVID-19 pandemic, viral infectious diseases have increasingly become a global concern, attracting significant attention. Among many viral epidemics, the dengue virus, an RNA virus from the Flaviviridae family, has been reported by the WHO as one of the most prevalent mosquito-borne diseases, infecting roughly 400 million people yearly and spreading Read More

Introduction Arjunolic acid, a well-known natural product with various medicinal properties, was isolated from the heartwood of Terminalia arjuna. Various amides of arjunolic acid were synthesized using different aryl and cyclic amines, characterized, and evaluated for their anti-cancer activities at the National Cancer Institute (NCI). Method All the derivatives were active against all the cell lines of NCI compared to the parent mol Read More

Exercise-induced muscle damage (EIMD) is a common occurrence among athletes and individuals engaged in physical fitness activities. Muscle strains result from excessive or repetitive muscle tension, leading to tissue damage, inflammation, and pain. These strains can range from mild discomfort to severe damage, resulting in pain, inflammation, and reduced functionality. Effective management of muscle damage is cr Read More

Introduction Copine-3 (CPNE3) is a conservative calcium-dependent phospholipid-binding protein belonging to the copines protein family. CPNE3 has been implicated in the development and progression of several diseases, including cancer. Method Herein, we investigated the molecular mechanisms through which CPNE3 regulates the migration of lung adenocarcinoma (LUAD) cells in vitro. Western blotting and immunohi Read More

Introduction Melanoma is one of the most dangerous and common types of cancer in humans. In order to minimize the toxicity and side effects of melanoma treatment, it is important to identify drug candidates that have strong anti-cancer activity and fewer side effects. Lobaric acid is a small molecule that has been found to have significant anti-cancer effects on various types of cancer cells. Methods The study aimed to invest Read More

Background This study investigates the potential effects of elemene injection on pancreatic cancer using network pharmacology and experimental validation. Methods GEO database were used to acquire genes which are differentially expressed between pancreatic cancer tissue and normal tissue. The vigorous energetic ingredients were identified in research and the object genes were obtained from BATMAN-TCM. The key t Read More

Background Metabolic Syndrome (MS) is a cluster of conditions that significantly increase the risk of infertility in women. Granulosa cells are crucial for ovarian folliculogenesis and fertility. Understanding molecular alterations in these cells can provide insights into MS-associated infertility. Objective This study aimed to investigate Differentially Expressed Genes (DEGs) and Proteins (DEPs) in granulosa cells from female patie Read More

Targeted therapy for colorectal cancer (CRC) appears to have great potential with lipid nanoparticles (LNPs). The advances in LNP-based techniques, such as liposomes, exosomes, micelles, solid lipid nanoparticles (SLNs), nano-cubosomes, and plant-derived LNPs (PDLNPs), are explored in detail in this thorough review. Every platform provides distinct advantages: liposomes enable precise drug release and impro Read More

Prostaglandin E2 (PGE2) plays a crucial role in inflammation. Non-steroidal anti-inflammatory medications are commonly utilized to alleviate pain and address inflammation by blocking the production of PGE2 and cyclooxygenase (COX). However, selective inhibition of COX can easily lead to a series of risks for cardiovascular diseases. Hence, it is imperative to discover safer and more efficient targets for reducing inflammation. Read More

Cancer is one of the most devastating illnesses in the world, impacting millions of individuals every year. Despite various therapies, the final effect is unsatisfactory. Chemotherapy currently dominates as the primary option of treatment. However, its severe adverse effects, limited efficacy, and resistance to drugs undermine its potential. Growing evidence suggests that ginsenoside Rg3, a natural compound obtained from the gi Read More

Introduction The effectiveness of pharmaceutical treatment methods is vital in cancer treatment. In this context, various targeted drug delivery systems are being developed to minimize or eliminate existing deficiencies and harms. This study aimed to model the interaction of MEN-based drug-targeting systems with cancer cells and determine the properties of interacting MENs. Methods Magnetoelectric Nanostructures (M Read More