Search Results - "Fernández, Amaury"

Halogen–Aromatic π Interactions Modulate Inhibitor Residence Times by Heroven, Christina, Georgi, Victoria, Ganotra, Gaurav K., Brennan, Paul, Wolfreys, Finn, Wade, Rebecca C., Fernández‐Montalván, Amaury E., Chaikuad, Apirat, Knapp, Stefan

“…Prolonged drug residence times may result in longer‐lasting drug efficacy, improved pharmacodynamic properties, and “kinetic selectivity” over off‐targets with…”
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Binding Kinetics Survey of the Drugged Kinome by Georgi, Victoria, Schiele, Felix, Berger, Benedict-Tilman, Steffen, Andreas, Marin Zapata, Paula A, Briem, Hans, Menz, Stephan, Preusse, Cornelia, Vasta, James D, Robers, Matthew B, Brands, Michael, Knapp, Stefan, Fernández-Montalván, Amaury

“…Target residence time is emerging as an important optimization parameter in drug discovery, yet target and off-target engagement dynamics have not been clearly…”
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Characterization of 12 GnRH peptide agonists – a kinetic perspective by Nederpelt, Indira, Georgi, Victoria, Schiele, Felix, Nowak‐Reppel, Katrin, Fernández‐Montalván, Amaury E., IJzerman, Adriaan P., Heitman, Laura H.

“…Background and Purpose Drug‐target residence time is an important, yet often overlooked, parameter in drug discovery. Multiple studies have proposed an…”
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A miniaturized mode-of-action profiling platform enables high throughput characterization of the molecular and cellular dynamics of EZH2 inhibition by Falkenstern, Lilia, Georgi, Victoria, Bunse, Stefanie, Badock, Volker, Husemann, Manfred, Roehn, Ulrike, Stellfeld, Timo, Fitzgerald, Mark, Ferrara, Steven, Stöckigt, Detlef, Stresemann, Carlo, Hartung, Ingo V., Fernández-Montalván, Amaury

“…The market approval of Tazemetostat (TAZVERIK) for the treatment of follicular lymphoma and epithelioid sarcoma has established “enhancer of zeste homolog 2”…”
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BAY 1125976, a selective allosteric AKT1/2 inhibitor, exhibits high efficacy on AKT signaling‐dependent tumor growth in mouse models by Politz, Oliver, Siegel, Franziska, Bärfacker, Lars, Bömer, Ulf, Hägebarth, Andrea, Scott, William J., Michels, Martin, Ince, Stuart, Neuhaus, Roland, Meyer, Kirstin, Fernández‐Montalván, Amaury Ernesto, Liu, Ningshu, von Nussbaum, Franz, Mumberg, Dominik, Ziegelbauer, Karl

“…The PI3K‐AKT‐mTOR signaling cascade is activated in the majority of human cancers, and its activation also plays a key role in resistance to chemo and targeted…”
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Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis by Sugawara, Tatsuo, Nevedomskaya, Ekaterina, Heller, Simon, Böhme, Annika, Lesche, Ralf, Ahsen, Oliver, Grünewald, Sylvia, Nguyen, Holly M., Corey, Eva, Baumgart, Simon J., Georgi, Victoria, Pütter, Vera, Fernández‐Montalván, Amaury, Vasta, James D., Robers, Matthew B., Politz, Oliver, Mumberg, Dominik, Haendler, Bernard

“…Prostate cancer is a frequent malignancy in older men and has a very high 5‐year survival rate if diagnosed early. The prognosis is much less promising if the…”
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In vitro and in silico analysis of the effects of D2 receptor antagonist target binding kinetics on the cellular response to fluctuating dopamine concentrations by Witte, Wilhelmus E A, Versfelt, Joost W, Kuzikov, Maria, Rolland, Solene, Georgi, Victoria, Gribbon, Philip, Gul, Sheraz, Huntjens, Dymphy, Graaf, Piet Hein, Danhof, Meindert, Fernández‐Montalván, Amaury, Witt, Gesa, Lange, Elizabeth C M

“…Background and Purpose Target binding kinetics influence the time course of the drug effect (pharmacodynamics) both (i) directly, by affecting the time course…”
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Probing the catalytic functions of Bub1 kinase using the small molecule inhibitors BAY-320 and BAY-524 by Baron, Anna P, von Schubert, Conrad, Cubizolles, Fabien, Siemeister, Gerhard, Hitchcock, Marion, Mengel, Anne, Schröder, Jens, Fernández-Montalván, Amaury, von Nussbaum, Franz, Mumberg, Dominik, Nigg, Erich A

“…The kinase Bub1 functions in the spindle assembly checkpoint (SAC) and in chromosome congression, but the role of its catalytic activity remains controversial…”
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ANALYSIS OF THE SOMACLONAL VARIATION IN TWO IN VITRO REGENERATED AGAVE SPECIES by Velasco, Irene Martínez, Fernandez, Amaury-M. Arzate

“…Background: Plant tissue culture has been shown to be an efficient technique for the propagation of diverse Agave species using different in vitro regeneration…”
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Probe dependency in the determination of ligand binding kinetics at a prototypical G protein-coupled receptor by Bosma, Reggie, Stoddart, Leigh A., Georgi, Victoria, Bouzo-Lorenzo, Monica, Bushby, Nick, Inkoom, Loretta, Waring, Michael J., Briddon, Stephen J., Vischer, Henry F., Sheppard, Robert J., Fernández-Montalván, Amaury, Hill, Stephen J., Leurs, Rob

“…Drug-target binding kinetics are suggested to be important parameters for the prediction of in vivo drug-efficacy. For G protein-coupled receptors (GPCRs), the…”
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Characterization of the Menin-MLL Interaction as Therapeutic Cancer Target by Brzezinka, Krzysztof, Nevedomskaya, Ekaterina, Lesche, Ralf, Haegebarth, Andrea, Ter Laak, Antonius, Fernández-Montalván, Amaury E, Eberspaecher, Uwe, Werbeck, Nicolas D, Moenning, Ursula, Siegel, Stephan, Haendler, Bernard, Eheim, Ashley L, Stresemann, Carlo

“…Inhibiting the interaction of menin with the histone methyltransferase MLL1 (KMT2A) has recently emerged as a novel therapeutic strategy. Beneficial…”
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Biochemical characterization of USP7 reveals post‐translational modification sites and structural requirements for substrate processing and subcellular localization by Fernández‐Montalván, Amaury, Bouwmeester, Tewis, Joberty, Gerard, Mader, Robert, Mahnke, Marion, Pierrat, Benoit, Schlaeppi, Jean‐Marc, Worpenberg, Susanne, Gerhartz, Bernd

“…Ubiquitin specific protease 7 (USP7) belongs to the family of deubiquitinating enzymes. Among other functions, USP7 is involved in the regulation of stress…”
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CHARACTERIZATION OF THE SENESCENCE-ASSOCIATED PROTEASES OF THE “TIGER FLOWER” (Tigridia pavonia) L.F. DC by Piña Escutia, José Luis, Norman Mondragón, Thomas Héctor, Arzate Fernández, Amaury Martín

“…Background: Tigridia pavonia is a Mexican native ornamental plant that displays great beauty and color of its flower. However, its quick senescence limits its…”
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Differential analyte derivatization enables unbiased MALDI-TOF-based high-throughput screening: A proof-of-concept study for the discovery of catechol-o-methyltransferase inhibitors by Winter, Martin, Simon, Roman P., Wang, Yuting, Bretschneider, Tom, Bauer, Margit, Magarkar, Aniket, Reindl, Wolfgang, Fernández-Montalván, Amaury, Montel, Florian, Büttner, Frank H.

“…Recent advances in label-free high-throughput screening via matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry (MS) offer…”
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Karyotype analysis and physical mapping of the 5S and 45S rDNA genes in Tigridia pavonia var. Dulce (Iridaceae) by Arroyo-Martínez, Hugo Abelardo, Arzate-Fernández, Amaury Martín, Barba-González, Rodrigo, Piña-Escutia, José Luis

“…Tigridia pavonia Redouté (Iridaceae) is a species with great ornamental potential of which nine different varieties are known. Among them, Tigridia pavonia…”
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A universal homogeneous assay for high-throughput determination of binding kinetics by Schiele, Felix, Ayaz, Pelin, Fernández-Montalván, Amaury

“…There is an increasing demand for assay technologies that enable accurate, cost-effective, and high-throughput measurements of drug–target association and…”
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Karyotype determination of three Tigridia species (Asparagales, Iridaceae) by Arroyo Martínez, Hugo Abelardo, Arzate Fernández, Amaury Martín, Barba González, Rodrigo, Piña Escutia, José Luis

“…Studies of the genus Tigridia Jussieu show that there is inadequate cytological information, and variable basic numbers and karyotype features have been…”
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Targeting BET bromodomains for cancer treatment by Jung, Marie, Gelato, Kathy A, Fernández-Montalván, Amaury, Siegel, Stephan, Haendler, Bernard

“…The bromodomain and extraterminal (BET) subfamily of bromodomain-containing proteins has emerged in the last few years as an exciting, novel target group…”
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Affinity Map of Bromodomain Protein 4 (BRD4) Interactions with the Histone H4 Tail and the Small Molecule Inhibitor JQ1 by Jung, Marie, Philpott, Martin, Müller, Susanne, Schulze, Jessica, Badock, Volker, Eberspächer, Uwe, Moosmayer, Dieter, Bader, Benjamin, Schmees, Norbert, Fernández-Montalván, Amaury, Haendler, Bernard

“…Bromodomain protein 4 (BRD4) is a member of the bromodomain and extra-terminal domain (BET) protein family. It binds to acetylated histone tails via its tandem…”
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Considerations for improved performance of competition association assays analysed with the Motulsky–Mahan's “kinetics of competitive binding” model by Georgi, Victoria, Dubrovskiy, Alexey, Steigele, Stephan, Fernández‐Montalván, Amaury E.

“…Background and Purpose Target engagement dynamics can influence drugs' pharmacological effects. Kinetic parameters for drug:target interactions are often…”
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