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Method for Testing Drugs Belonging to Substrates and Inhibitors of the Transporter Protein BCRP on CACO-2 Cells.
Dokl Biochem Biophys
January 2025
Ryazan State Medical University, Ryazan, Russian Federation.
Introduction: Breast cancer resistance protein (BCRP) is an efflux membrane transporter that controls the pharmacokinetics of a large number of drugs. Its activity may change when taking some endo- and exogenous substances, thus making it a link in drug interactions.
Aim: The aim of the study was to develop a methodology for testing drugs for belonging to BCRP substrates and inhibitors in vitro.
Study of the Pharmacological Activity Spectrum of the New Original NT-3 Mimetic Dipeptide GTS-302.
Dokl Biochem Biophys
January 2025
Center for Strategic Planning and Management of Biomedical Health Risks, Federal Medical and Biological Agency, Moscow, Russia.
Unlabelled: The association of the pathogenesis of neurodegenerative diseases, depression, anxiety, and cognitive disorders with neurotrophin-3 deficiency determines the prospect of creating drugs with a similar mechanism of action. Since the use of full-length NT-3 is limited by unsatisfactory pharmacokinetic properties, the creation of low-molecular mimetics of neurotrophin-3 that are active when administered systemically is relevant. The Federal Research Center for Innovator and Emerging Biomedical and Pharmaceutical Technologies has created a dimeric dipeptide mimetic of the 4th loop of NT-3, hexamethylenediamide bis-(N-γ-oxybutyryl-L-glutamyl-L-asparagine) with the laboratory code GTS-302, which activates TrkC and TrkB receptors.
View Article and Find Full Text PDFComparing haploidentical transplantation with post-transplantation cyclophosphamide and umbilical cord blood transplantation using targeted busulfan in children and adolescents with hematologic malignancies.
Blood Res
January 2025
Department of Pediatrics, Seoul National University College of Medicine, Seoul National University Cancer Research Institute, Seoul, Republic of Korea.
Purpose: This study compared the outcomes of haploidentical-related donor (HRD) and umbilical cord blood (UCB) hematopoietic stem cell transplantation (HSCT) in pediatric patients with hematologic malignancies.
Methods: Data on patients who underwent HRD HSCT with post-transplant cyclophosphamide (n = 41) and UCB HSCT (n = 24) after targeted busulfan-based myeloablative conditioning with intensive pharmacokinetic monitoring between 2009 and 2018 were retrospectively analyzed.
Results: The median follow-up durations in the HRD and UCB groups were 7.
Discovery of selective ROCK2 inhibitors with free radical scavenging ability for the treatment of gouty arthritis.
Mol Divers
January 2025
Key Laboratory of Structure-Based Drugs Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang, PR China.
ROCK inhibitors can inhibit IL-1β and NLRP3, and their therapeutic potential for osteoarthritis and rheumatoid arthritis has been confirmed, but their impact on gouty arthritis has not been reported yet. By hybridization the structure of Edaravone, a series of ROCK inhibitors with pyrazolone scaffold were designed and synthesized. RM-04 has acceptable selective ROCK2 inhibitory activity with an IC of 4.
View Article and Find Full Text PDFA physiologically based pharmacokinetic (PBPK) model describing the kinetics of a commercial mixture α-, β-, and γ-hexabromocyclododecane exposure in mice.
Arch Toxicol
January 2025
Scientist Emeritus, National Institute of Environmental Health Sciences, Research Triangle Park, NC, USA.
Hexabromocyclododecane (HBCD) is a brominated flame retardant, that is added, but not chemically bonded, to consumer products. HBCD is sold as a commercial-grade HBCD mixture containing three major stereoisomers: alpha (α), beta (β), and gamma (γ), with relative amounts of 12% for α-HBCD, 6% for β-HBCD, and 82% for γ-HBCD. HBCDs are widely measured in the environment and in biological matrices.
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