Search Results - "Sim, Hong May"
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Multiple transport-active binding sites are available for a single substrate on human P-glycoprotein (ABCB1)
Published in PloS one (05-12-2013)“…P-glycoprotein (Pgp, ABCB1) is an ATP-Binding Cassette (ABC) transporter that is associated with the development of multidrug resistance in cancer cells. Pgp…”
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Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1
Published in Biochemical pharmacology (01-10-2013)“…The overexpression of the serine/threonine specific Polo-like kinase 1 (Plk1) has been detected in various types of cancer, and thus has fast become an…”
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Saracatinib (AZD0530) is a potent modulator of ABCB1‐mediated multidrug resistance in vitro and in vivo
Published in International journal of cancer (01-01-2013)“…Saracatinib, a highly selective, dual Src/Abl kinase inhibitor, is currently in a Phase II clinical trial for the treatment of ovarian cancer. In our study, we…”
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ARRY-334543 Reverses Multidrug Resistance by Antagonizing the Activity of ATP-Binding Cassette Subfamily G Member 2
Published in Journal of cellular biochemistry (01-08-2014)“…ABSTRACT ARRY‐334543 is a small molecule inhibitor of ErbB1 and ErbB2 tyrosine kinases. We conducted this study to determine whether ARRY‐334543 can enhance…”
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Molecular Basis of the Polyspecificity of P-Glycoprotein (ABCB1): Recent Biochemical and Structural Studies
Published in ABC Transporters and Cancer (2015)“…ABCB1 (P-glycoprotein/P-gp) is an ATP-binding cassette transporter well known for its association with multidrug resistance in cancer cells. Powered by the…”
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Book Chapter Journal Article -
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Overexpression of ATP-binding cassette transporter ABCG2 as a potential mechanism of acquired resistance to vemurafenib in BRAF(V600E) mutant cancer cells
Published in Biochemical pharmacology (01-02-2013)“…Melanoma is the most serious type of skin cancer with a high potential for metastasis and very low survival rates. The discovery of constitutive activation of…”
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A yeast two-hybrid system for the screening and characterization of small-molecule inhibitors of protein-protein interactions identifies a novel putative Mdm2-binding site in p53
Published in BMC biology (09-11-2017)“…Protein-protein interactions (PPIs) are fundamental to the growth and survival of cells and serve as excellent targets to develop inhibitors of biological…”
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Dimethoxyaurones: Potent inhibitors of ABCG2 (breast cancer resistance protein)
Published in European journal of pharmaceutical sciences (15-11-2008)“…A series of 4,6-dimethoxyaurones were synthesized by reacting 4,6-dimethoxybenzofuran-3(2 H)-one with various benzaldehydes in a base-catalyzed aldol reaction…”
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Conserved Walker A Cysteines 431 and 1074 in Human P‑Glycoprotein Are Accessible to Thiol-Specific Agents in the Apo and ADP-Vanadate Trapped Conformations
Published in Biochemistry (Easton) (15-10-2013)“…P-Glycoprotein (P-gp) is an ATP-binding cassette efflux transporter involved in the development of multidrug resistance in cancer cells. Although the mechanism…”
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Aurones as Modulators of ABCG2 and ABCB1: Synthesis and Structure-Activity Relationships
Published in ChemMedChem (04-04-2011)“…The ability of aurones to modulate the efflux activities of ABCG2 and ABCB1 was investigated by quantifying their effects on the accumulation of pheophorbide A…”
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In vitro and in vivo modulation of ABCG2 by functionalized aurones and structurally related analogs
Published in Biochemical pharmacology (01-12-2011)“…Over-expression of ABCG2 is linked to multidrug resistance in cancer chemotherapy. We have previously shown that functionalized aurones effectively reduced the…”
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12
Synthesis and antimicrobial activity of N-benzyl or N-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines
Published in Bioorganic & medicinal chemistry letters (15-09-2011)Get full text
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Abstract 766: Human ABCB1 and ABCG2 confer acquired resistance to Polo-like kinase 1 inhibitors, BI 2536, volasertib and GSK641364
Published in Cancer research (Chicago, Ill.) (01-10-2014)“…Abstract The overexpression of the serine/threonine specific polo-like kinase 1 (Plk1) has been detected in various types of cancer, and thus has fast become…”
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Neratinib reverses ATP-binding cassette B1-mediated chemotherapeutic drug resistance in vitro, in vivo, and ex vivo
Published in Molecular pharmacology (01-07-2012)“…Neratinib, an irreversible inhibitor of epidermal growth factor receptor and human epidermal receptor 2, is in phase III clinical trials for patients with…”
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Journal Article -
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Synthesis and antimicrobial activity of N1-benzyl or N1-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamines
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…A series of N1-benzyl and N1-benzyloxy-1,6-dihydro-1,3,5-triazine-2,4-diamine derivatives were synthesized and investigated for their antimicrobial activity…”
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Abstract 898: Probing accessibility and conformational changes in ATP-binding sites during the catalytic cycle of human P-glycoprotein (ABCB1)
Published in Cancer research (Chicago, Ill.) (15-04-2013)“…Abstract P-glycoprotein (P-gp) is an ATP-binding cassette (ABC) efflux transporter implicated in the development of multidrug resistance in cancer cells. The…”
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Abstract LB-222: Chemical and structural flexibility contribute to the broad substrate and modulator specificity of multidrug resistance-linked P-glycoprotein (ABCB1)
Published in Cancer research (Chicago, Ill.) (15-04-2013)“…Abstract The human ATP-binding cassette (ABC) transporter ABCB1 (P-glycoprotein, P-gp) mediates efflux of cytotoxic anticancer agents from cells, thereby…”
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Chemical Flexibility of P-Glycoprotein for Interaction with Substrates and Modulators
Published in Biophysical journal (29-01-2013)Get full text
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Abstract 3398: Overexpression of ATP-binding cassette transporter ABCG2 as a potential mechanism of acquired resistance to vemurafenib in BRAF(V600E) mutant cancer cells
Published in Cancer research (Chicago, Ill.) (15-04-2013)“…Abstract Melanoma is the most serious type of skin cancer with a high potential for metastasis and very low survival rates. The discovery of constitutive…”
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Mapping Conformational Changes Associated with the Catalytic Cycle of Human P-Glycoprotein (ABCB1)
Published in Biophysical journal (31-01-2012)Get full text
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