title: Orthogonal functionalisation of α-helix mimetics.
abstract: α-Helix mediated protein-protein interactions are of major therapeutic importance. As such, the design of inhibitors of this class of interaction is of significant interest. We present methodology to modify N-alkylated aromatic oligoamide α-helix mimetics using 'click' chemistry. The effect is shown to modulate the binding properties of a series of selective p53/hDM2 inhibitors.
authors: School of Chemistry, University of Leeds, Woodhouse Lane, Leeds, LS2 9JT, UK.
authors: Anna
authors: A
authors: Barnard
authors: Kérya
authors: K
authors: Long
authors: David J
authors: DJ
authors: Yeo
authors: Jennifer A
authors: JA
authors: Miles
authors: Valeria
authors: V
authors: Azzarito
authors: George M
authors: GM
authors: Burslem
authors: Panchami
authors: P
authors: Prabhakaran
authors: Thomas
authors: T
authors: A Edwards
authors: Andrew J
authors: AJ
authors: Wilson
mesh_terms: D000577:Amides / Q000737:chemistry; D032701:Biomimetics; D057930:Click Chemistry; D006801:Humans; D020128:Inhibitory Concentration 50; D064549:Myeloid Cell Leukemia Sequence 1 Protein / Q000737:chemistry; D011485:Protein Binding; D025941:Protein Interaction Mapping; D017433:Protein Structure, Secondary; D040901:Proteomics / Q000379:methods; D051736:Proto-Oncogene Proteins c-mdm2 / Q000037:antagonists & inhibitors / Q000737:chemistry*; D012997:Solvents / Q000737:chemistry; D013499:Surface Properties; D016159:Tumor Suppressor Protein p53 / Q000037:antagonists & inhibitors / Q000737:chemistry*; D051020:bcl-X Protein / Q000737:chemistry
chemical_list: D000577:Amides; C579095:MCL1 protein, human; D064549:Myeloid Cell Leukemia Sequence 1 Protein; D012997:Solvents; C495901:TP53 protein, human; D016159:Tumor Suppressor Protein p53; D051020:bcl-X Protein; C497206:MDM2 protein, human; D051736:Proto-Oncogene Proteins c-mdm2