Search Results - "Masjost, Birgit"

Structure-Based Optimization of Novel Azepane Derivatives as PKB Inhibitors by Breitenlechner, Christine B, Wegge, Thomas, Berillon, Laurent, Graul, Klaus, Marzenell, Klaus, Friebe, Walter-Gunar, Thomas, Ulrike, Schumacher, Ralf, Huber, Robert, Engh, Richard A, Masjost, Birgit

“…Novel azepane derivatives were prepared and evaluated for protein kinase B (PKB-α) and protein kinase A (PKA) inhibition. The original (−)-balanol-derived lead…”
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Cobalt-Mediated [2+2+2] Cycloaddition versus CH and NH Activation of Pyridones and Pyrazinones with Alkynes: An Experimental Study by Aubert, Corinne, Betschmann, Patrick, Eichberg, Michael J., Gandon, Vincent, Heckrodt, Thilo J., Lehmann, Jürg, Malacria, Max, Masjost, Birgit, Paredes, Elisa, Vollhardt, K. Peter C., Whitener, Glenn D.

“…The reactivity of a range of pyridone and pyrazinone derivatives towards alkynes in the presence of cyclopentadienylcobaltbis(ethene) has been investigated…”
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Design and Crystal Structures of Protein Kinase B-Selective Inhibitors in Complex with Protein Kinase A and Mutants by Breitenlechner, Christine B, Friebe, Walter-Gunar, Brunet, Emmanuel, Werner, Guido, Graul, Klaus, Thomas, Ulrike, Künkele, Klaus-Peter, Schäfer, Wolfgang, Gassel, Michael, Bossemeyer, Dirk, Huber, Robert, Engh, Richard A, Masjost, Birgit

“…Protein kinase B (PKB)-selective inhibitors were designed, synthesized, and cocrystallized using the AGC kinase family protein kinase A (PKA, often called…”
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X-ray Crystal Structure of a Bisubstrate Inhibitor Bound to the Enzyme Catechol-O-methyltransferase: A Dramatic Effect of Inhibitor Preorganization on Binding Affinity by Lerner, Christian, Ruf, Armin, Gramlich, Volker, Masjost, Birgit, Zürcher, Gerhard, Jakob-Roetne, Roland, Borroni, Edilio, Diederich, François

“…With an IC50 value of 9 nM, 1 is the most potent known disubstrate inhibitor for catechol‐O‐methyltransferase (COMT). Inhibition of COMT is of significant…”
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Bisubstrate inhibitors for the enzyme catechol-O-methyltransferase (COMT): influence of inhibitor preorganisation and linker length between the two substrate moieties on binding affinity by Lerner, Christian, Masjost, Birgit, Ruf, Armin, Gramlich, Volker, Jakob-Roetne, Roland, Zürcher, Gerhard, Borroni, Edilio, Diederich, François

“…Inhibition of the enzyme catechol-O-methyltransferase (COMT) is an important approach in the treatment of Parkinson's disease. A series of new potent…”
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Structure-Based Design, Synthesis, and in vitro Evaluation of Bisubstrate Inhibitors for Catechol O-Methyltransferase (COMT) by Masjost, Birgit, Ballmer, Patrick, Borroni, Edilio, Zürcher, Gerhard, Winkler, Fritz K., Jakob-Roetne, Roland, Diederich, François

“…The enzyme catechol O‐methyltransferase (COMT) catalyzes the Me group transfer from the cofactor S‐adenosylmethionine (SAM) to the hydroxy group of catechol…”
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X-ray Crystal Structure of a Bisubstrate Inhibitor Bound to the Enzyme Catechol-O-methyltransferase: A Dramatic Effect of Inhibitor Preorganization on Binding Affinity We thank F. Hoffmann-La Roche for generous support of this work. We are grateful to P. Malherbe for the cloning of COMT, P. Caspers for the expression of COMT, A. Cesura for enzyme purification, B. Wipf for fermentation, and H. W. Lahm for sequencing by Lerner, Christian, Ruf, Armin, Gramlich, Volker, Masjost, Birgit, Zürcher, Gerhard, Jakob-Roetne, Roland, Borroni, Edilio, Diederich, François

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Structure-Based Design, Synthesis, and in vitro Evaluation of Bisubstrate Inhibitors for CatecholO-Methyltransferase (COMT) by Masjost, Birgit, Ballmer, Patrick, Borroni, Edilio, Zürcher, Gerhard, Winkler, Fritz K., Jakob-Roetne, Roland, Diederich, François

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X-ray Crystal Structure of a Bisubstrate Inhibitor Bound to the Enzyme Catechol-O-methyltransferase: A Dramatic Effect of Inhibitor Preorganization on Binding Affinity by Lerner, Christian, Ruf, Armin, Gramlich, Volker, Masjost, Birgit, Zürcher, Gerhard, Jakob-Roetne, Roland, Borroni, Edilio, Diederich, François

“…Mit einem IC50‐Wert von 9 nM ist 1 der wirksamste bekannte Disubstrat‐Inhibitor für Catechol‐O‐Methyl‐Transferase (COMT). Die Inhibierung von COMT ist für die…”
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