Macrocyclic peptides, including depsipeptides, are an emerging new modality in drug discovery research. Tetraselide, an antifungal cyclic peptide isolated from a marine-derived filamentous fungus, possesses a unique amphiphilic structural feature consisting of five consecutive β-hydroxy-amino acid residues and fatty acid moieties. Because the structure elucidation of the naturally occurring product left six stereocenters ambiguous, we implemented bioinformatic analyses, chemical degradation studies and chiral pool fragment synthesis to identify two of the undetermined stereocenters. Convergent total synthesis of the four remaining plausible isomers of tetraselide was accomplished liquid-phase peptide synthesis (LPPS) using soluble hydrophobic tag auxiliaries. The key advances involve fragment coupling by the serine/threonine ligation (STL) reaction and head-to-tail macrolactamization of the carrier-supported precursors that enabled systematic elaboration of the amphiphilic cyclic peptides. Ultimately, we determined the absolute structure of this natural product.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11892018 | PMC |
http://dx.doi.org/10.1039/d5sc00566c | DOI Listing |
J Med Internet Res
March 2025
Department of Pharmacology, Faculty of Medicine, University of Helsinki, Helsinki, Finland.
Background: Acceptance and commitment therapy provides a psychobehavioral framework feasible for digital and hybrid weight loss interventions. In face-to-face studies, group-based interventions yield more favorable outcomes than individual interventions, but the effect of the intervention form has not been studied in combination with eHealth.
Objective: This study investigated whether a minimal, 3-session group or individual enhancement could provide additional benefits compared to an eHealth-only intervention when assessing weight, body composition, and laboratory metrics in a sample of occupational health patients with obesity.
Chemistry
March 2025
University of Groningen: Rijksuniversiteit Groningen, Stratingh Institute for Chemistry, Nijenborgh 7, 9747 AG, Groningen, NETHERLANDS, KINGDOM OF THE.
Glycerol dialkyl glycerol tetraethers (GDGTs) are a group of membrane spanning lipids produced by both Archaea and Bacteria. Branched GDGTs (brGDGTs) are a class of these tetraether lipids known to be produced by certain bacteria and are commonly found in terrestrial environments. Due to their environmental ubiquity, high preservation potential, and role in membrane adaptation, brGDGTs form the basis of many widely employed paleoenvironmental proxies.
View Article and Find Full Text PDFMed Oncol
March 2025
Centre for Biotechnology, Siksha O Anusandhan (Deemed to Be University), Bhubaneswar, Odisha, 751003, India.
Prostate cancer has garnered much importance in recent years due to its rising incidence and mortality among men worldwide. The ineffectiveness of existing therapies and adverse events associated with conventional treatment have led patients to turn towards traditional medicine for the management of prostate cancer. Cinnamomum zeylanicum bark essential oil (CZEO) possesses promising anticancer properties, yet the exact mechanism of action of CZEO for the management of prostate cancer remains unclear.
View Article and Find Full Text PDFJ Epidemiol Glob Health
March 2025
Microbiological Type Culture Collection and Gene Bank (MTCC), CSIR Institute of Microbial Technology, Chandigarh, 160036, India.
Introduction: Antimicrobial resistance (AMR) is one of the major global concerns in the current scenario. Mass-gathering events in fast-developing and densely populated areas may contribute to antibiotic resistance. Despite meticulous planning and infrastructure development, the effect of mass gatherings on microbial ecosystems and antibiotic resistance must be investigated.
View Article and Find Full Text PDFFunct Integr Genomics
March 2025
Department of Orthopedics, The First Affiliated Hospital of Chongqing Medical University, Chongqing, 400016, China.
Osteosarcoma is the most common bone tumor and a highly aggressive malignant neoplasm. This study aims to elucidate the role of lactylation-related genes (LRGs) in osteosarcoma, with the goal of improving prognostic accuracy and enhancing the efficacy of immunotherapy. Using public datasets, we integrated differential and correlated genes based on single-cell sequencing AUCell scores and performed enrichment analysis and risk model construction on these genes.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!