Search Results - "Pleban, Karin"
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P-glycoprotein substrate binding domains are located at the transmembrane domain/transmembrane domain interfaces: a combined photoaffinity labeling-protein homology modeling approach
Published in Molecular pharmacology (01-02-2005)“…P-glycoprotein (P-gp) is an energy-dependent multidrug efflux pump conferring resistance to cancer chemotherapy. Characterization of the mechanism of drug…”
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Inhibitors of p-glycoprotein--lead identification and optimisation
Published in Mini reviews in medicinal chemistry (01-02-2005)“…The membrane bound drug efflux pump P-glycoprotein (P-gp) transports a wide variety of functionally and structurally diverse cytotoxic drugs out of tumour…”
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A three-dimensional model for the substrate binding domain of the multidrug ATP binding cassette transporter LmrA
Published in Molecular pharmacology (01-11-2004)“…Multidrug resistance presents a major obstacle to the treatment of infectious diseases and cancer. LmrA, a bacterial ATP-dependent multidrug transporter,…”
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Homology model of the multidrug transporter LmrA from Lactococcus lactis
Published in Bioorganic & medicinal chemistry letters (06-12-2004)“…Starting from the dimeric crystal structure of Vibrio cholerae MsbA, two homology models of the ATP-dependent multidrug transporter LmrA were generated. LmrA…”
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Structure–Activity Relationships, Ligand Efficiency, and Lipophilic Efficiency Profiles of Benzophenone-Type Inhibitors of the Multidrug Transporter P-Glycoprotein
Published in Journal of medicinal chemistry (12-04-2012)“…The drug efflux pump P-glycoprotein (P-gp) has been shown to promote multidrug resistance (MDR) in tumors as well as to influence ADME properties of drug…”
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Resveratrol analogues as selective cyclooxygenase-2 inhibitors: synthesis and structure–activity relationship
Published in Bioorganic & medicinal chemistry (01-11-2004)“…A series of hydroxylated and methoxylated trans-stilbenes were synthesized and evaluated for their ability to inhibit COX-1 and COX-2. Some of the hydroxylated…”
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Conjugation to 4-aminoquinoline improves the anti-trypanosomal activity of Deferiprone-type iron chelators
Published in Bioorganic & medicinal chemistry (01-02-2013)“…Iron is an essential growth component in all living organisms and plays a central role in numerous biochemical processes due to its redox potential and high…”
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Insights into Phenylalanine Derivatives Recognition of VLA-4 Integrin: From a Pharmacophoric Study to 3D-QSAR and Molecular Docking Analyses
Published in Journal of Chemical Information and Computer Sciences (01-09-2004)“…The very late antigen-4 (VLA-4), also known as integrin α4β1, is expressed on monocytes, T- and B-lympohocytes, basophils, and eosinophils and is involved in…”
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Targeting drug-efflux pumps -- a pharmacoinformatic approach
Published in Acta biochimica polonica (01-01-2005)“…In line with our studies on propafenone-type inhibitors of P-glycoprotein (P-gp), we applied several methods to approach virtual screening tools for…”
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Intramolecular Distribution of Hydrophobicity Influences Pharmacological Activity of Propafenone-type MDR Modulators
Published in Archiv der Pharmazie (Weinheim) (01-06-2004)“…Lipophilicity is one of the major determining physicochemical descriptors for P‐glycoprotein (P‐gp) inhibitory activity. Recently, Pajeva and Wiese showed that…”
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