Microbial biofilms pose a severe threat to global health, as they are associated with deadly chronic infections and antibiotic resistance. To date, very few drugs are in clinical practice that specifically target microbial biofilms. Therefore, there is an urgent need for the development of novel therapeutic options targeting biofilm-related infections. In this review, we discuss nearly seventy-five different molecular scaffolds published over the last decade (2010-2023) which have exhibited their biofilm inhibition potential. For convenience, we have classified these into five different sub-groups based on their origin and design (excluding peptides as they are placed in between small molecules and biologics), namely, heterocycles; inorganic small molecules & metal complexes; small molecules decorated nanoparticles; small molecules derived from natural products (both plant and marine sources); and small molecules designed by in-silico approach. These antibiofilm agents are capable of disrupting microbial biofilms and can offer a promising avenue for future developments in human medicine. A hitherto review of this kind will lay a platform for the researchers to find new molecular entities to curb the serious menace of antimicrobial resistance especially caused by biofilms.
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http://dx.doi.org/10.1016/j.micpath.2024.106543 | DOI Listing |
Mol Divers
December 2024
Small-Molecule Drug Research Center, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai, 201203, People's Republic of China.
Overexpressed AXL kinase is involved in various human malignancies, which incurs tumor progression, poor prognosis, and drug resistance. Suppression of the aberrant AXL axis with genetic tools or small-molecule inhibitors has achieved valid antitumor efficacies in both preclinical studies and clinical antitumor campaigns. Herein we will report the design, synthesis, and structure-activity relationship (SAR) exploration of a series of anilinopyrimidine type II AXL inhibitors.
View Article and Find Full Text PDFACS Nano
December 2024
Faculty of Materials Science, Shenzhen MSU-BIT University, Shenzhen 518100, P. R. China.
Protein hydrolysis targeted chimeras (PROTACs) represent a different therapeutic approach, particularly relevant for overcoming challenges associated with traditional small molecule inhibitors. These challenges include targeting difficult proteins that are often deemed "undruggable" and addressing issues of acquired resistance. PROTACs employ the body's own E3 ubiquitin ligases to induce the degradation of specific proteins of interest (POIs) through the ubiquitin-proteasome pathway.
View Article and Find Full Text PDFBiomacromolecules
December 2024
School of Chemistry, Xi'an Jiaotong University, Xi'an 710049, China.
Persistent oxidative stress following bone defects significantly impedes the repair of bone tissue. Designing an antioxidative hydrogel with a suitable mechanical strength can help alter the local microenvironment and promote bone defect healing. In this work, α-lipoic acid (LA), a natural antioxidant small molecule, was chemically cross-linked with lipoic acid-functionalized poly(ethylene glycol) (PEG, = 6k or 10k) in sodium bicarbonate solution, to prepare LA-PEG hydrogels (LP, = 6k or 10k).
View Article and Find Full Text PDFExpert Opin Ther Pat
December 2024
Key Laboratory of Structure-Based Drugs Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, China.
Introduction: Xanthine oxidase (XO) catalyzes the oxidation of both hypoxanthine and xanthine in the last two steps of the purine metabolic pathway, serving as a rate-limiting enzyme for uric acid production as well as a key target for the treatment of gout and other hyperuricemia-related conditions.
Areas Covered: This paper reviews XO inhibitors in patents from 2021 to the present. We summarize in detail the structural classes and characteristics, in vitro and in vivo biological results, and structure‒activity relationships of synthetic inhibitors, as well as the sources, specific structures, research methods, and biological activities of XO inhibitors from natural products.
BMC Genomics
December 2024
Department of Medicine and Animal Surgery, Veterinary Science, University of Murcia, Murcia, Spain.
Background: Extracellular vesicles (EVs) are essential for cell-to-cell communication because they transport functionally active molecules, including proteins, RNA, and lipids, from secretory cells to nearby or distant target cells. Seminal plasma contains a large number of EVs (sEVs) that are phenotypically heterogeneous. The aim of the present study was to identify the RNA species contained in two subsets of porcine sEVs of different sizes, namely small sEVs (S-sEVs) and large sEVs (L-sEVs).
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