Search Results - "Kan, Jason W. Y"
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A New Class of Safe, Potent, and Specific P‑gp Modulator: Flavonoid Dimer FD18 Reverses P‑gp-Mediated Multidrug Resistance in Human Breast Xenograft in Vivo
Published in Molecular pharmaceutics (05-10-2015)“…Flavonoid dimer FD18 is a new class of dimeric P-gp modulator that can reverse cancer drug resistance. FD18 is a potent (EC50 = 148 nM for paclitaxel), safe…”
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Discovery of a Flavonoid FM04 as a Potent Inhibitor to Reverse P-Glycoprotein-Mediated Drug Resistance in Xenografts and Improve Oral Bioavailability of Paclitaxel
Published in International journal of molecular sciences (04-12-2022)“…Biotransformation of flavonoid dimer FD18 resulted in an active metabolite FM04. It was more druggable because of its improved physicochemical properties. FM04…”
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Characterization of a Potent, Selective, and Safe Inhibitor, Ac15(Az8)2, in Reversing Multidrug Resistance Mediated by Breast Cancer Resistance Protein (BCRP/ABCG2)
Published in International journal of molecular sciences (31-10-2022)“…Overexpression of breast cancer resistance transporter (BCRP/ABCG2) in cancers has been explained for the failure of chemotherapy in clinic. Inhibition of the…”
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Amine Linked Flavonoid Dimers as Modulators for P-Glycoprotein-Based Multidrug Resistance: Structure–Activity Relationship and Mechanism of Modulation
Published in Journal of medicinal chemistry (08-03-2012)“…Here we report a great improvement in reversal potency of cancer drug resistance when flavonoid dimers possess a functionally substituted aminopolyethylene…”
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Identification of Binding Sites in the Nucleotide-Binding Domain of P‑Glycoprotein for a Potent and Nontoxic Modulator, the Amine-Containing Monomeric Flavonoid FM04
Published in Journal of medicinal chemistry (11-05-2023)“…We have previously discovered an amine-containing flavonoid monomer FM04 as a potent P-glycoprotein (P-gp) inhibitor (EC50 = 83 nM). Here, a series of…”
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Boosting the efficacy of anti-MRSA β-lactam antibiotics via an easily accessible, non-cytotoxic and orally bioavailable FtsZ inhibitor
Published in European journal of medicinal chemistry (01-02-2019)“…The rapid emergence of methicillin-resistant Staphylococcus aureus (MRSA) strains has undermined the therapeutic efficacy of existing β-lactam antibiotics…”
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