The design and synthesis of biotin chain-terminated inhibitors (BTI) showing high affinity for matrix metalloproteinases (MMPs) on one side and high affinity for avidin through the biotinylated tag on the other are reported. The affinity of the designed BTI toward five different MMPs has been evaluated and the simultaneous formation of a highly stable ternary system Avidin-BTI-MMP clearly assessed. This system will permit the development of new approaches to detect, quantify, or collect MMPs in biological samples, with potential applications in vivo.
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http://dx.doi.org/10.1021/bc8003827 | DOI Listing |
Bioorg Chem
January 2025
Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Suez Canal University, Ismailia, Egypt. Electronic address:
EGFR inhibitors are a class of targeted therapies utilized in the management of certain tumor kinds such as NSCLC and breast cancer. Series of 1,2,3-triazole-Schiff's base hybrids were designed, synthesized, and estimated for their antitumor effect toward breast cancer cells, MCF-7 and MDA-MB-231. The safety and selectivity of the new compounds were tested using normal cell (WI-38).
View Article and Find Full Text PDFOrg Lett
January 2025
Shanghai Frontiers Science Center of Optogenetic Techniques for Cell Metabolism, Shanghai Key Laboratory of New Drug Design, and School of Pharmacy, East China University of Science and Technology, Shanghai 200237, P. R. China.
The efficient construction of chiral aryl-containing organosilicon frameworks via catalytic enantioselective three-component silylarylation of alkenes remains a great challenge. Herein, a photoredox/nickel dual-catalytic asymmetric protocol has been disclosed by using a chiral biimidazoline (BiIM) as the ligand, silylboranes as the silyl radical precursors, aryl bromides as the coupling partners, and morpholine as the promoter. Remarkably, the reaction features mild and green conditions, high reaction efficiency, and excellent enantioselectivity, enabling the facile synthesis of valuable chiral tropic acid and sila-isoflavanone structures.
View Article and Find Full Text PDFHum Reprod
January 2025
The International Peace Maternity and Child Health Hospital, School of Medicine, Shanghai Jiao Tong University, Shanghai, China.
Study Question: Is elevated plasma molybdenum level associated with increased risk for idiopathic premature ovarian insufficiency (POI)?
Summary Answer: Elevated plasma molybdenum level is associated with an increased risk of idiopathic POI through vascular endothelial injury and inhibition of granulosa cell proliferation.
What Is Known Already: Excessive molybdenum exposure has been associated with ovarian oxidative stress in animals but its role in the development of POI remains unknown.
Study Design, Size, Duration: Case-control study of 30 women with idiopathic POI and 31 controls enrolled from August 2018 to May 2019.
Diabetes Care
January 2025
Division of Endocrinology, Diabetes & Metabolism, Department of Medicine, Johns Hopkins School of Medicine, Baltimore, MD.
Objective: To assess the extent to which the concomitant presence of subclinical myocardial injury or stress and diabetes affects the risk of heart failure (HF) subtypes.
Research Design And Methods: The Jackson Heart Study included Black adults, categorized based on diabetes status, high-sensitivity cardiac troponin I (hs-cTnI), and brain natriuretic peptide (BNP) levels. Subclinical myocardial injury was defined as hs-cTnI ≥4 ng/L in women and ≥6 ng/L in men, and subclinical myocardial stress as BNP ≥35 pg/mL.
Diabetes
January 2025
Adelaide Medical School and Centre of Research Excellence (CRE) in Translating Nutritional Science to Good Health, The University of Adelaide, Adelaide, Australia.
Individuals with type 2 diabetes are at high risk of postprandial falls in blood pressure (BP) (i.e., a reduction in systolic BP of ≥20mmHg, termed postprandial hypotension (PPH)), which increases the risk of falls and mortality.
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