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A novel oligobenzamide-based α-helix mimetic was designed and synthesised with either imine or hydrazone functionalities that serve both to pre-organise the side-chain vectors to mimic the i, i + 4 and i + 7 residues of an α-helix, and to allow for the facile creation of dynamic libraries.
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http://dx.doi.org/10.1039/c6cc07787k | DOI Listing |
PLoS One
September 2025
Faculty of Health, Institute of Pharmacology and Toxicology, Centre for Biomedical Education and Research (ZBAF), School of Medicine, Witten/Herdecke University, Witten, Germany.
The emergence of antibiotic resistance continues to pose a significant global challenge. Drug repurposing, wherein existing therapeutics are evaluated for new applications, offers a promising strategy to address this issue. Farnesyltransferase inhibitors (FTIs), initially developed for cancer therapy, have demonstrated antimicrobial activity against several gram-positive bacteria.
View Article and Find Full Text PDFMol Divers
September 2025
Medical Biotechnology Laboratory (MedBiotech), Faculty of Medecine and Pharmacy of Rabat, Mohammed Vth University in Rabat, Rabat, Morocco.
Asthma is a chronic inflammatory disorder of the airways. Standard treatments, such as inhaled corticosteroids like fluticasone, beclomethasone, and budesonide, are effective in managing asthma symptoms by reducing inflammation through immune suppression. However, prolonged corticosteroid therapy can impair vitamin D metabolism, exacerbating vitamin D deficiency, which is essential for immune regulation and anti-inflammatory responses via the vitamin D receptor (VDR).
View Article and Find Full Text PDFJ Mol Biol
September 2025
Microbiology and Molecular Biology Laboratory, Department of Biological Sciences, Indian Institute of Science Education and Research Bhopal. Electronic address:
Emergence of drug resistance in Mycobacterium tuberculosis (Mtb) calls for newer drugs and drug targets. Essential proteins such as DNA polymerase (DNAP) processivity factor, also called sliding clamp (DnaN), are indispensable for bacterial survival, and are excellent drug targets. Here, we constructed a dnaN-conditional knockout in Mycobacterium smegmatis (MsmΔdnaN) and were able to successfully complement it with Mtb DnaN (DnaN).
View Article and Find Full Text PDFiScience
September 2025
Institute of Pharmaceutical and Biomedical Sciences (IPBS), 55128 Mainz, Germany.
DNMT2 (TRDMT1) is a human RNA methyltransferase implicated in various disease processes. However, small-molecule targeting of DNMT2 remains challenging due to poor selectivity and low cellular availability of known -adenosylhomocysteine (SAH)-derived ligands. In this study, a DNA-encoded library (DEL) screen identified five non-SAH-like chemotypes that selectively bind DNMT2, including three peptidomimetics.
View Article and Find Full Text PDFAdv Sci (Weinh)
August 2025
Guangdong Provincial Engineering Research Center of Molecular Imaging, Guangdong-Hong Kong-Macao University Joint Laboratory of Interventional Medicine, the Fifth Affiliated Hospital, Sun Yat-sen University, Zhuhai, Guangdong, 519000, China.
Although cartilage damage is key to the pathogenesis of many musculoskeletal diseases, including osteoarthritis and rheumatoid arthritis (RA), imaging and drug delivery to cartilage remain a demanding challenge. Cartilage is an avascular tissue with a dense matrix constraining the penetration of imaging and targeting agents. Here, a unique class of cationic peptidomimetics featuring peptoid residue Nlys (N-substituted butyl-amino glycine) is reported for cartilage targeting.
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