98%
921
2 minutes
20
Organoids, 3D cellular models derived from stem cells, have revolutionized drug testing by providing human-relevant systems for modeling diseases and testing drug efficacy. Unlike traditional 2D cell cultures or animal models, organoids closely resemble the complex architecture and function of human tissues, offering more accurate predictions of drug responses. Researchers are increasingly utilizing these models in oncology, neurology, liver toxicity, and personalized medicine. Recent advances in gene editing (e.g., CRISPR-Cas9), multi-omics technologies, and organoid-on-chip systems have further enhanced the capabilities of organoids in drug discovery. CRISPR-Cas9 allows for precise modeling of genetic disorders, while multi-omics approaches integrate transcriptomics, proteomics, and metabolomics to provide deeper insights into drug metabolism and toxicity. Organoid-on-chip platforms combine organoid culture with microfluidic systems, enabling the simulation of organ interactions and real-time drug testing. AI and machine learning models now enhance these platforms by predicting drug responses and optimizing high-throughput screening. Despite these advancements, challenges such as scalability, reproducibility, and the incomplete recapitulation of complex organ functions remain. Organoids hold the promise of significantly reducing reliance on animal models, improving the accuracy of drug testing, and paving the way for personalized treatments. This review outlines the latest innovations in organoid-based drug discovery, highlighting their potential to transform modern pharmacology and precision medicine, while acknowledging the ongoing efforts to address existing limitations.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1002/ddr.70121 | DOI Listing |
J Org Chem
September 2025
Pharmaron Drug Discovery Services Europe, Pharmaron UK Ltd., West Hill Innovation Park, Hertford Road, Hoddesdon EN11 9FH, United Kingdom.
Sulfur(VI) fluoride exchange (SuFEx) compounds are gaining increasing attention due to their various applications. We present the Diels-Alder reaction of ethenesulfonyl fluoride and analogues to rapidly access cyclic and bicyclic SuFEx derivatives in moderate to good yields. These derivatives have been shown to be useful intermediates in a variety of synthetic transformations to expand the toolkit for the preparation of cyclic aliphatic sulfonyl fluorides.
View Article and Find Full Text PDFOrg Lett
September 2025
United Graduate School of Drug Discovery and Medical Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
A direct azidomethylation reaction at the sulfur atoms of thiols with -azidomethyldisulfonimides is presented, providing a facile and efficient approach for the synthesis of azidomethylated compounds with broad substrate scope and mild reaction conditions. Under optimized conditions using -azidomethyl-bis(4-trifluoromethylbenzene)sulfonimide as the azidomethyl source, various aliphatic and aromatic thiols furnish the corresponding -azidomethyl compounds in moderate to high yields. The reaction proceeds selectively at the mercapto group, even in substrates bearing polar functional groups.
View Article and Find Full Text PDFMicrob Drug Resist
September 2025
Drug Discovery Research, Wockhardt Research Centre, Wockhardt Ltd., Chhatrapati Sambhajinagar, India.
Cefepime (FEP), a fourth-generation cephalosporin combined with tazobactam (TAZ), a β-lactamase inhibitor, is being developed by Wockhardt as a pharmacodynamically optimized fixed dose combination (FEP-2 g + TAZ-2 g) for the treatment of multidrug-resistant Gram-negative infections. To undertake an exposure-response analysis for establishing pharmacokinetic (PK)/pharmacodynamic (PD) targets, it is crucial to characterize the PK profile of compounds in surrogate compartments, such as plasma and lung, in clinically relevant animal infection models used to evaluate efficacy. In the current study, PKs of FEP and TAZ were assessed in plasma and in epithelial lining fluid (ELF) of neutropenic noninfected, lung-infected, and thigh-infected mice.
View Article and Find Full Text PDFChembiochem
September 2025
School of Biological and Chemical Sciences, Ryan Institute, University of Galway, University Road, Galway, H91 TK33, Ireland.
Activated B-cell diffuse large B-cell lymphoma (ABC-DLBCL) is an aggressive cancer with poor response to standard chemotherapy. In search of new therapeutic leads, a library of 435 fractions prepared from the Irish marine biorepository was screened against 2 ABC-DLBCL cell lines (TMD8 and OCI-Ly10) and a non-cancerous control cell line (CB33). Active fractions are prioritized based on potency and selectivity.
View Article and Find Full Text PDFOpen Res Eur
September 2025
Veterinary and Animal Sciences, University of Copenhagen, Frederiksberg, 1870, Denmark.
Background: Innovative antibiotic discovery strategies are urgently needed to successfully combat infections caused by multi-drug-resistant bacteria.
Methods: We employed a direct screening approach to identify compounds with antimicrobial and antimicrobial helper-drug activity against Gram-positive and Gram-negative bacteria. We used this platform in two different strains of methicillin-resistant (MRSA) and aminoglycoside-resistant strains of to screen for antimicrobials compounds, which potentiate the activity of aminoglycoside antibiotics.