Search Results - "Sawney, Helen"

Pharmacokinetic Benefits of 3,4-Dimethoxy Substitution of a Phenyl Ring and Design of Isosteres Yielding Orally Available Cathepsin K Inhibitors by Crawford, James J, Kenny, Peter W, Bowyer, Jonathan, Cook, Calum R, Finlayson, Jonathan E, Heyes, Christine, Highton, Adrian J, Hudson, Julian A, Jestel, Anja, Krapp, Stephan, Martin, Scott, MacFaul, Philip A, McDermott, Benjamin P, McGuire, Thomas M, Morley, Andrew D, Morris, Jeffrey J, Page, Ken M, Ribeiro, Lyn Rosenbrier, Sawney, Helen, Steinbacher, Stefan, Smith, Caroline, Dossetter, Alexander G

“…Rational structure-based design has yielded highly potent inhibitors of cathepsin K (Cat K) with excellent physical properties, selectivity profiles, and…”
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Isosteric replacements for benzothiazoles and optimisation to potent Cathepsin K inhibitors free from hERG channel inhibition by Dossetter, Alexander G., Bowyer, Jonathan, Cook, Calum R., Crawford, James J., Finlayson, Jonathan E., Heron, Nicola M., Heyes, Christine, Highton, Adrian J., Hudson, Julian A., Jestel, Anja, Krapp, Stephan, MacFaul, Philip A., McGuire, Thomas M., Morley, Andrew D., Morris, Jeffrey J., Page, Ken M., Ribeiro, Lyn Rosenbrier, Sawney, Helen, Steinbacher, Stefan, Smith, Caroline

“…The discovery of nitrile compound 4, a potent inhibitor of Cathepsin K (Cat K) with good bio-availability in dog is described. The compound was used to…”
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(1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly Selective Cathepsin K Inhibitor for the Treatment of Osteoarthritis by Dossetter, Alexander G, Beeley, Howard, Bowyer, Jonathan, Cook, Calum R, Crawford, James J, Finlayson, Jonathan E, Heron, Nicola M, Heyes, Christine, Highton, Adrian J, Hudson, Julian A, Jestel, Anja, Kenny, Peter W, Krapp, Stephan, Martin, Scott, MacFaul, Philip A, McGuire, Thomas M, Gutierrez, Pablo Morentin, Morley, Andrew D, Morris, Jeffrey J, Page, Ken M, Ribeiro, Lyn Rosenbrier, Sawney, Helen, Steinbacher, Stefan, Smith, Caroline, Vickers, Madeleine

“…Directed screening of nitrile compounds revealed 3 as a highly potent cathepsin K inhibitor but with cathepsin S activity and very poor stability to…”
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A cryptic matrix targeting signal of the yeast ADP/ATP carrier normally inserted by the TIM22 complex is recognized by the TIM23 machinery by Vergnolle, Maïlys A S, Sawney, Helen, Junne, Tina, Dolfini, Luisita, Tokatlidis, Kostas

“…The yeast ADP/ATP carrier (AAC) is a mitochondrial protein that is targeted to the inner membrane via the TIM10 and TIM22 translocase complexes. AAC is devoid…”
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