Four isomeric dehydroepiandrosterone- and pregnenolone-based N-alkynylaminosteroids were synthesized and tested in vitro for inhibition of heterologously expressed CYP17A1. The highest inhibitory activity was observed when the optimal number of side chain atoms was met. The conjugate based on pregnenolone containing an N-propynyl moiety was found to interefere with enzymatic activity most effectively and consistently in the micromolar range.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.18097/PBMC20196504324 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Synthesis and Characterization of Antibacterial Poly{2-[(methacryloyloxy)ethyl]trimethylammonium Chloride}/Chitosan Semi-Interpenetrating Networks for Papain Release.
Macromol Biosci
January 2025
Universidade Estadual de Campinas (UNICAMP), School of Chemical Engineering (FEQ), Albert Einstein Avenue, 500, Campinas, São Paulo, 13083-852, Brazil.
Annually, thousands of individuals suffer from skin injuries resulting from trauma, surgeries, or diabetes. Inadequate wound treatment can delay healing and increase the risk of severe infections. In this context, a promising synthetic polymer with potent antimicrobial properties, Poly{2-[(methacryloyloxy)ethyl]trimethylammonium chloride} (PMETAC), is synthesized and crosslinked with N,N'-Methylenebis(acrylamide) (BIS) in the presence of Chitosan (CH), a natural, biocompatible polysaccharide that promotes cell regeneration and provides additional beneficial properties.
View Article and Find Full Text PDFRefinement of a Published Gene-Physical Activity Interaction Impacting HDL-Cholesterol: Role of Sex and Lipoprotein Subfractions.
Genet Epidemiol
January 2025
Clinical and Translational Epidemiology Unit, Massachusetts General Hospital, Boston, Massachusetts, USA.
Large-scale gene-environment interaction (GxE) discovery efforts often involve analytical compromises for the sake of data harmonization and statistical power. Refinement of exposures, covariates, outcomes, and population subsets may be helpful to establish often-elusive replication and evaluate potential clinical utility. Here, we used additional datasets, an expanded set of statistical models, and interrogation of lipoprotein metabolism via nuclear magnetic resonance (NMR)-based lipoprotein subfractions to refine a previously discovered GxE modifying the relationship between physical activity (PA) and HDL-cholesterol (HDL-C).
View Article and Find Full Text PDFUsing system dynamics modeling approach to strengthen health systems to combat cancer: a systematic literature review.
J Med Econ
January 2025
UNESCO-TWAS, The World Academy of Sciences, Trieste, Italy.
Aim: Dynamic cancer control is a current health system priority, yet methods for achieving it are lacking. This study aims to review the application of system dynamics modeling (SDM) on cancer control and evaluate the research quality.
Methods: Articles were searched in PubMed, Web of Science, and Scopus from the inception of the study to November 15th, 2023.
Technological advances in clinical individualized medication for cancer therapy: from genes to whole organism.
Per Med
January 2025
Department of Clinical Pharmacy, Zhejiang Provincial Key Laboratory for Drug Evaluation and Clinical Research, The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, China.
Efforts have been made to leverage technology to accurately identify tumor characteristics and predict how each cancer patient may respond to medications. This involves collecting data from various sources such as genomic data, histological information, functional drug profiling, and drug metabolism using techniques like polymerase chain reaction, sanger sequencing, next-generation sequencing, fluorescence in situ hybridization, immunohistochemistry staining, patient-derived tumor xenograft models, patient-derived organoid models, and therapeutic drug monitoring. The utilization of diverse detection technologies in clinical practice has made "individualized treatment" possible, but the desired level of accuracy has not been fully attained yet.
View Article and Find Full Text PDFAcetylshikonin Derived From Arnebia euchroma (Royle) Johnst Kills Multidrug-Resistant Gram-Positive Pathogens In Vitro and In Vivo.
Phytother Res
January 2025
College of Veterinary Medicine, Yangzhou University, Yangzhou, China.
The rising prevalence of multidrug-resistant (MDR) Gram-positive bacteria threatens the effectiveness of current antibiotic therapies. However, the development of new antibiotics has stagnated in recent years, highlighted the critical need for the discovery of innovative antimicrobial agents. This study aims to evaluate the antibacterial activity of naphthoquinones derived from Arnebia euchroma (Royle) Johnst (ADNs) and elucidate their underlying mechanisms.
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!