Multidrug resistance (MDR) in leukemia is commonly associated with the expression of a transmembrane protein, P-glycoprotein (P-gp). In this study, two monoclonal antibodies (mAbs) specific for the extracellular domain of P-gp were generated. By employing the generated mAbs, a two-color lysed whole blood flow cytometric method for surface P-gp and an efficient sandwich ELISA for soluble P-gp determinations were established. By using the established methods, surface and soluble P-gp were detected in several leukemia patients. The presence of soluble P-gp could be used to identify the P-gp surface expression patients. Detection of soluble P-gp reported provides a new basis that may lead to a better understanding of the MDR mechanism in leukemia.
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http://dx.doi.org/10.1007/s12185-010-0668-8 | DOI Listing |
Clin Pharmacol Ther
January 2025
Sydney Pharmacy School, Faculty of Medicine and Health, University of Sydney, Sydney, New South Wales, Australia.
Green tea (Camellia sinensis) is a commonly consumed beverage or dietary supplement. As a natural product with a myriad of proposed health benefits, patients are likely to consume green tea while taking their medications unaware of its potential to interact with drugs and influence drug efficacy and safety. Catechins are the abundant polyphenolic compounds in green tea (e.
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December 2024
Department of Pharmacy, Birla Institute of Technology and Science Pilani, BITS-Pilani Hyderabad Campus, Jawahar Nagar, Kapra Mandal, Medchal District, Telangana, 500078, India.
Acalabrutinib (ACP) is a first-line treatment for chronic lymphocytic leukemia but suffers from poor and variable oral bioavailability due to its pH-dependent solubility, CYP3A4 metabolism, and P-gp efflux. Thus, the objective of this study was to improve the solubility and dissolution behaviour, in turn enhancing bioavailability, by formulating solid lipid nanoparticles (SLNs). ACP loaded SLNs (ACP-SLNs) were prepared via solvent-free hot emulsification followed by a double sonication process.
View Article and Find Full Text PDFEur J Med Chem
February 2025
School of Pharmacy, Fudan University, Shanghai, 201203, China; School of Chemistry and Chemical Engineering, Henan Normal University, Xinxiang, 453007, China. Electronic address:
J Biomol Struct Dyn
November 2024
Department of Zoology, Mizoram University, Aizawl, Mizoram, India.
Antimicrobial peptides (AMPs) are gaining popularity as potential substitutes for conventional antibiotics and bio-preservatives in response to an increase in antimicrobial resistance cases. However, their poor pharmacokinetic profiles limit their applicability. This study using ADMETlab, OECD QSAR toolbox, and VEGA HUB virtual environments profiled 82 peptide sequences of seven bee antimicrobial peptides (BAMPs: abaecin, apamin, apisimin, apidaecin, defensin, hymenoptaecin, and melittin) using 81 descriptors combining physicochemical, medicinal chemistry, ADMET, and toxicophore criteria.
View Article and Find Full Text PDFBioorg Med Chem
October 2023
Department of Medicinal Chemistry, University of Florida, Gainesville, FL 32610, United States; Center for Natural Products, Drug Discovery and Development (CNPD3), University of Florida, Gainesville, FL 32610, United States. Electronic address:
Microtubules, consisting of α/β-tubulin heterodimers, are prime targets for anticancer drug discovery. Gatorbulin-1 (GB1, 1a) is a recently described marine natural product that targets tubulin at a new, seventh pharmacological site at the tubulin intradimer interface. Using our previously developed robust route towards GB1 (1a), we synthesized simplified, first-generation gatorbulins, GB2-7 (1b-1g) of this highly modified cyclodepsipeptide (GB1) that does not contain any proteinogenic amino acid.
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