Structural Basis of the Allosteric Inhibition of Human ABCG2 by Nanobodies
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Tumors consist of cells whose growth and morphological characteristics are markedly different from those of normal cells. Observation of human and animal models argue that tumor development proceeds via a process formally analogous to Darwinian evolution, ...
Telomerase, a ribonucleoprotein acting as a reverse transcriptase, has been identified as a target for cancer drug discovery. The synthetic, non-nucleosidic compound, BIBR1532, is a potent and selective telomerase inhibitor capable of inducing senescence i ...
Double trouble: A hybrid org.-inorg. (organometallic) inhibitor was designed to target glutathione transferases. The metal center is used to direct protein binding, while the org. moiety acts as the active-site inhibitor (see picture). The mechanism of inh ...
Lon (or La) is a soluble, homooligomeric ATP-dependent protease. Mass determination and cryoelectron microscopy of pure mitochondrial Lon from Saccharomyces cerevisiae identify Lon as a flexible ring-shaped heptamer. In the presence of ATP or 5'-adenylylim ...
Proceedings of the National Academy of Sciences1999
Cisplatin is one of the most important and widely used anticancer drug in clinical use. However, its effectiveness is limited by its high toxicity and incidence of drug resistance. This has provided motivation for the search for transition metal-based drug ...
A series of ruthenium(II)-arene (RAPTA) compds. were evaluated for their ability to inhibit thioredoxin reductase (either cytosolic or mitochondrial) and cathepsin B, two possible targets for anticancer metallodrugs. In general, inhibition of the thioredox ...
Enzymes that are involved in the synthesis and processing of oligosaccharides, such as glycosidases, are important catalysts for the specific assembly of oligosaccharide structures on proteins. Design and preparation of selective inhibitors of these enzyme ...
New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...
A proof-of-principle study on the application of a top-down electrospray ionization Fourier transform ion cyclotron resonance mass spectrometric approach for characterization of the primary binding sites of the platinum anticancer agents cisplatin, transpl ...