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http://dx.doi.org/10.1016/j.tplants.2025.08.006 | DOI Listing |
J Med Chem
September 2025
Encoded Technologies, Molecular Modalities Discovery, GSK, Cambridge, Massachusetts 02140, United States.
DNA-encoded libraries (DELs) are used throughout small-molecule drug discovery to identify new lead compounds for protein targets. DEL hits are traditionally evaluated via off-DNA resynthesis and subsequent biological testing. This approach can be time- and resource-intensive, limiting the number of putative hits selected for follow-up.
View Article and Find Full Text PDFPhytopathology
September 2025
Guizhou University, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Huaxi District, Guiyang, Guizhou Province of China, Guiyang, China, 550025;
Osthole exhibits strong inhibitory activity against phytopathogenic fungi; however, its antifungal mechanism remains unclear. This study assessed osthole's inhibitory effects on several phytopathogenic fungi, revealing a half-maximal effective concentration of 70.03 μg/ml against the hyphal growth of .
View Article and Find Full Text PDFArch Pharm (Weinheim)
September 2025
College of Chemistry, Pingyuan Laboratory (Zhengzhou University), Zhengzhou University, Zhengzhou, China.
The SARS-CoV-2 pandemic has spurred global efforts to develop therapeutic approaches. The main protease (Mpro) of SARS-CoV-2 is crucial for viral replication and a key target for therapeutic development. In this study, 22 thiosemicarbazone derivatives were synthesized.
View Article and Find Full Text PDFPhytomedicine
August 2025
Department of Pharmaceutical Biology, Institute of Pharmaceutical and Biomedical Sciences Johannes Gutenberg University, Staudinger Weg 5, 55128 Mainz, Germany. Electronic address:
Background: Non-small-cell lung cancer NSCLC is the major diagnosed type of lung cancers in the USA and Europe. It is generally related to poor prognosis and low rates of survival. Oleandrin is a cardiac glycoside occurring naturally in Nerium oleander (Apocynaceae).
View Article and Find Full Text PDFJ Biol Chem
September 2025
Department of Biochemistry, Stanford University School of Medicine, Stanford, CA, United States; Aligning Science Across Parkinson's (ASAP) Collaborative Research Network, San Francisco, CA, United States. Electronic address:
PPM1H phosphatase reverses Parkinson's disease-associated, Leucine Rich Repeat Kinase 2-mediated, Rab GTPase phosphorylation. We showed previously that PPM1H relies on an N-terminal amphipathic helix for Golgi membrane localization and this helix enables PPM1H to associate with liposomes in vitro; binding to highly curved liposomes activates PPM1H's phosphatase activity. We show here that PPM1H also contains an allosteric binding site for its non-phosphorylated reaction products, Rab8A and Rab10.
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