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  • A Novel Methodology for the Incorporation of Chiral Linkers in Stapled Peptides 

    Serrano, JC; Sipthorp, J; Xu, W; Itzhaki, LS; Ley, SV
    Stapled peptides have arisen as a new class of chemical probe and potential therapeutic agents to modulate protein-protein interactions. Here, we report the first two-component i,i+7 stapling methodology using two orthogonal, ...
  • The binding orientations of structurally-related ligands can differ; A cautionary note 

    Ruepp, M-D; Wei, H; Leuenberger, M; Lochner, M; Thompson, AJ (Elsevier, 2017-06-01)
    Crystal structures can identify ligand-receptor interactions and assist the development of novel therapeutics, but experimental challenges sometimes necessitate the use of homologous proteins. Tropisetron is an orthosteric ...
  • Macrocyclized Extended Peptides: Inhibiting the Substrate-Recognition Domain of Tankyrase 

    Xu, W; Lau, YH; Fischer, G; Tan, YS; Chattopadhyay, A; de la Roche, M; Hyvönen, M et al. (American Chemical Society, 2017-02-15)
    We report a double-click macrocyclization approach for the design of constrained peptide inhibitors having non-helical or extended conformations. Our targets are the tankyrase proteins (TNKS), poly(ADP-ribose) polymerases ...
  • The binding orientation of epibatidine at α7 nACh receptors 

    Thompson, AJ; Metzger, S; Lochner, M; Ruepp, M-D (Elsevier, 2017-04-01)
    Epibatidine is an alkaloid toxin that binds with high affinity to nicotinic and muscarinic acetylcholine receptors, and has been extensively used as a research tool. To examine binding interactions at the nicotinic receptor, ...

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