Conformational analysis of potent competitive inhibitors of aromatase, androst-4-enes 5, as well as 2,4-diene steroids 3, 4, and 6 was carried out, using theoretical calculations, to determine the stereochemistry of their aromatase-catalyzed oxygenation. In the steroids examined, both the 19-alcohols and the 19-aldehydes favor the above- A ring conformation among the possible three in each. The results suggest that the 3-deoxy steroid 5a as well as the 2,4-diene steroids 4a and 6a would be oxygenated at C-19 by aromatase through the same stereomechanism as that involved in the androstenedione aromatization.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1248/bpb.18.782 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Conformational dynamics of the membrane protein of MERS-CoV in comparison with SARS-CoV-2 in ERGIC complex.
J Biomol Struct Dyn
January 2025
College of Applied Medical Sciences, lmam Abdulrahman Bin Faisal University (lAU), Dammam, Saudi Arabia.
The present study explores the conformational dynamics of the membrane protein of Middle East Respiratory Syndrome Coronavirus (MERS-CoV) within the Endoplasmic Reticulum-Golgi Intermediate Compartment (ERGIC) complex using an all-atomistic molecular dynamics simulation approach. Significant structural changes were observed in the N-terminal, C-terminal, transmembrane, and beta-sheet sandwich domains of the MERS-CoV membrane protein. This study also highlights the structural similarities between the MERS-CoV and the SARS-CoV-2 membrane proteins, particularly in how both exhibit a distinct kink in the transmembrane helix caused by aromatic residue-lipid interactions.
View Article and Find Full Text PDFInhibitory mechanisms of galloylated forms of theaflavins on α-glucosidase.
Int J Biol Macromol
January 2025
School of Biological and Chemical Engineering, NingboTech University, Ningbo 315100, China. Electronic address:
Theaflavins, oxidation product of tea polyphenols, have demonstrated significant inhibitory effects on α-glucosidase, which is beneficial in alleviating hyperglycemia. This study found that the inhibition of four monomers of theaflavins on α-glucosidase was related to the presence of the galloyl moiety (GM), with IC values ranging from TFDG (0.26 mg/mL) < TF3'G (0.
View Article and Find Full Text PDFEffects of in vitro simulated digestion on the hypoglycaemic capacity of wheat bran-soluble dietary fibre.
Biochem Biophys Res Commun
December 2024
College of Food Science and Engineering, Nanjing University of Finance and Economics, Nanjing, 210023, China. Electronic address:
Wheat bran-soluble dietary fibre (WB-SDF) is known for its hypoglycaemic properties and its potential to control postprandial blood glucose levels in individuals with hyperglycaemia. However, the digestive process may alter its glucose-lowering potential. This study investigated the effects of in vitro simulated digestion on the hypoglycaemic efficacy of WB-SDF.
View Article and Find Full Text PDFXanthine Nucleosides with Pyrazolo[3,4-]pyrimidine Skeleton: Functionalization with Halogen Atoms, Clickable Side Chains, Pyrene, and iEDDA Cycloadducts, and Impact of Ionic Forms on Photophysical Properties.
J Org Chem
January 2025
Laboratory of Bioorganic Chemistry and Chemical Biology, Center for Nanotechnology, Heisenbergstrasse 11, 48149 Münster, Germany.
Xanthine nucleosides play a significant role in the expansion of the four-letter genetic code. Herein, 7-functionalized 8-aza-7-deazaxanthine ribo- and 2'-deoxyribonucleosides are described. 2-Amino-6-alkoxy nucleosides were converted to halogenated 8-aza-7-deazaxanthine nucleosides by deamination followed by hydroxy/alkoxy substitution.
View Article and Find Full Text PDFSingle-Step Genome-Wide Association Study of Factors for Evaluated and Linearly Scored Traits in Swedish Warmblood Horses.
J Anim Breed Genet
January 2025
Department of Animal Biosciences, Swedish University of Agricultural Sciences, Uppsala, Sweden.
Swedish Warmblood horses (SWB) are bred for show jumping and/or dressage with young horse test scores as indicator traits. This study aimed to investigate possible candidate genes and regions of importance for evaluated and linearly scored young horse test traits. A single-step genome-wide association study (ssGWAS) was done using the BLUPF90 suite of programs for factors scores from factor analysis of traits assessed at young horse tests together with height at withers.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!