Current Medicinal Chemistry - Volume 26, Issue 10, 2019

Background: The molecular genetic technologies revolutionized the diagnostics of many disorders. Thanks to the new molecular techniques and the rapid improvement of the information technologies the number of mendelien inherited disorders has increased rapidly in the last five years. The omics era brought radical changes in the understanding of complex disorders and the underlying pathomechanisms. However, in most c Read More

Background: We report a comprehensive overview of current Chronic Obstructive Lung Disease (COPD) therapies and discuss the development of possible new pharmacological approaches based on “new” knowledge. Specifically, sensitivity/resistance to corticosteroids is evaluated with a special focus on the role of gene mutations in drug response. Objective: Critically review the opportunities and the challenges occurring i Read More

Background: We report a comprehensive overview of current COPD therapies from a real-world experience. Objective: Critically review the opportunities and the challenges occurring in the real-world treatment of COPD. Methods: This is a review that also report results from COPD patients treated with standardized therapy including pulmonary rehabilitation (Real World Data – RWD). Conclusion: Comprehensive asse Read More

The P-glycoprotein is an efflux transporter that expels substances out of the cells and has an important impact on the pharmacokinetic and pharmacodynamic properties of drugs. The study of the interactions between ligands and the P-glycoprotein has implications in the design of Central Nervous System drugs and their transport across the blood-brain barrier. Moreover, since the P-glycoprotein is overexpressed in Read More

Background: Antimicrobial resistance is found in all microorganisms and has become one of the biggest threats to global health. New antimicrobials with different action mechanisms are effective weapons to fight against antibiotic-resistance. Objective: This review aims to find potential drugs which can be further developed into clinic practice and provide clues for developing more effective antimicrobials. Methods: DNA replica Read More

Ascribe to the unique two-dimensional planar nanostructure with exceptional physical and chemical properties, black phosphorous (BP) as the emerging inorganic twodimensional nanomaterial with high biocompatibility and degradability has been becoming one of the most promising materials of great potentials in biomedicine. The exfoliated BP sheets possess ultra-high surface area available for valid bio-conjugation Read More

Janus kinases (JAKs) are a family of non-receptor tyrosine kinases, composed by four members, JAK1, JAK2, JAK3 and TYK2. JAKs are involved in different inflammatory and autoimmune diseases, as well as in malignancies, through the activation of the JAK/STAT signalling pathway. Furthermore, the V617F mutation in JAK2 was identified in patients affected by myeloproliferative neoplasms. This knowledge prompted Read More

Background: The application of traditional Chinese medicine (TCM) in the treatment of fatigue has long been practiced in clinical and showed significant effects. Objective: This article summarizes the work done on the natural products from TCM that are reported to have effects of treating fatigue, in the past two decades. Method: Research status, sources, models, efficacy and mechanisms of active ingredients and their mo Read More

Gossypol, a natural product extracted from the seed, roots, and stem of cotton, was initially used as a male contraceptive but was subsequently investigated as a novel antitumor agent. This review depicts the current status of gossypol and its derivatives as novel antitumor agents as well as presents their preparation and characteristics, especially of some gossypol Schiff bases, through quantitative and structural analysis. Th Read More

Identifying and understanding the biological events that occur following ultraviolet (UV) exposure are mandatory to elucidate the biological and clinical consequences of sun exposure, and to provide efficient and adequate photoprotection strategies. The main UVinduced biological features (markers related to sunburn, cancer, photoaging immunosuppression, pigmentation), characterized in human skin in vivo, could be repr Read More

Background: Type-2 diabetes mellitus accounts for 80-90% of diabetic patients. So far, the treatment of diabetes mainly aims at elevating insulin level and lowering glucose level in the peripheral blood and mitigating insulin resistance. Physiologically, insulin secretion from pancreatic β cells is delicately regulated. Thus, how insulin-related therapies could titrate blood glucose appropriately and avoid the occurrence of hypoglyce Read More

Background: Cannabinoid Receptor 1 (CB1) is a membrane protein prevalent in the central nervous system, whose crystallographic structure has recently been solved. Studies will be needed to investigate CB1 complexes with its ligands and its role in the development of new drugs. Objective: Our goal here is to review the studies on CB1, starting with general aspects and focusing on the recent structural studies, with emphasis Read More