A novel caspase-3 substrate N-Ac-DEVD-N'-MC-R110, which is a fluorogenic substrate cleavable in a single step, has been prepared. It has a significantly higher enzyme turnover rate and sensitivity for detecting caspase-3 activity both in solution and living cells than existing fluorogenic substrates.
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http://dx.doi.org/10.1016/j.bmcl.2005.02.081 | DOI Listing |
Biol Direct
January 2025
Department of Hematology, The Second Affiliated Hospital, School of Medicine, The Chinese University of Hong Kong, Shenzhen & Longgang District People's Hospital of Shenzhen, Shenzhen, 518172, China.
Background: Multiple myeloma (MM) is a hematological malignancy characterized by uncontrolled proliferation of plasma cells and is currently incurable. Despite advancements in therapeutic strategies, resistance to proteasome inhibitors, particularly bortezomib (BTZ), poses a substantial challenge to disease management. This study aimed to explore the efficacy of boanmycin, a novel antitumor antibiotic, in overcoming resistance to BTZ in MM.
View Article and Find Full Text PDFJ Ethnopharmacol
January 2025
Tianjin Key Laboratory for Modern Drug Delivery & High-Efficiency, School of Pharmaceutical Science and Technology, Faculty of Medicine, Tianjin University, Weijin Road, 300072 Tianjin, China. Electronic address:
Ethnopharmacological Relevance: Originally formulated to mitigate high-altitude sickness, Xinnaoxin capsules (XNX) are composed of three traditional Chinese medicines (Rhodiola rosea L., Lycium barbarum L. and Hippophae rhamnoides) with properties of anti-hypoxia, anti-fatigue, and anti-aging.
View Article and Find Full Text PDFFundam Clin Pharmacol
February 2025
Experimental Oncology and Hemopathies Laboratory, Clinical Analysis Department, Federal University of Santa Catarina, Florianópolis, 88040-900, Brazil.
Background: Chalcones have been described in the literature as promising antineoplastic compounds.
Objectives: Therefore, the objective of this study was to analyze the cytotoxic effect of 23 synthetic chalcones on human acute leukemia (AL) cell lines (Jurkat and K562).
Methods: Cytotoxicity assessment was performed using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) method.
Int J Biol Macromol
December 2024
College of pharmacy, Xinxiang Medical University, 453003 Xinxiang, PR China; Pingyuan Laboratory, Xinxiang, Henan 453007, PR China. Electronic address:
Effective delivery of sufficient doxorubicin (DOX) molecules in tumors is hindered by the complex biological barriers. Herein, a DOX-loaded sodium alginate-based injectable hydrogel (DOX@MHB-conj-SA) was designed by the Michael addition reactions between the sulfydryl in cross-linkers and the double bonds in a derivative of sodium alginate. DOX@MHB-conj-SA was administrated to CT26 tumor-bearing mice via peritumoral injection for locoregional treatment of colorectal cancer by inducing apoptosis and pyroptosis.
View Article and Find Full Text PDFEndocr Relat Cancer
January 2025
C Alvarez, Centro de Investigación en Medicina Molecular y Enfermedades Crónicas (CIMUS), University of Santiago de Compostela (USC), Santiago de Compostela, Spain.
The discovery of RET mutations in Multiple Endocrine Neoplasia 2A (MEN2A) in 1993 ignited a revolution in our understanding of this versatile receptor. Since then, RET's influence has expanded to encompass diverse organs, including the pituitary gland. This review explores the multifaceted role of RET in somatotrophs, focusing on two opposing pathways: proliferation versus differentiation and apoptosis.
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