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Journal articleAzzarito V, Rowell P, Barnard A, et al., 2016,
Probing Protein Surfaces: QSAR Analysis with Helix Mimetics
, Chembiochem, Vol: 17, Pages: 768-773, ISSN: 1439-7633α-Helix-mediated protein–protein interactions (PPIs) are important targets for small-molecule inhibition; however, generic approaches to inhibitor design are in their infancy and would benefit from QSAR analyses to rationalise the noncovalent basis of molecular recognition by designed ligands. Using a helix mimetic based on an oligoamide scaffold, we have exploited the power of a modular synthesis to access compounds that can readily be used to understand the noncovalent determinants of hDM2 recognition by this series of cell-active p53/hDM2 inhibitors.
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Journal articleBarnard A, Long K, Martin HL, et al., 2015,
Selective and potent proteomimetic inhibitors of intracellular protein–protein interactions
, Angewandte Chemie - International Edition, Vol: 54, Pages: 2960-2965, ISSN: 1433-7851Inhibition of protein–protein interactions (PPIs) represents a major challenge in chemical biology and drug discovery. α-Helix mediated PPIs may be amenable to modulation using generic chemotypes, termed “proteomimetics”, which can be assembled in a modular manner to reproduce the vectoral presentation of key side chains found on a helical motif from one partner within the PPI. In this work, it is demonstrated that by using a library of N-alkylated aromatic oligoamide helix mimetics, potent helix mimetics which reproduce their biophysical binding selectivity in a cellular context can be identified.
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Journal articleBarnard A, Miles JA, Burslem GM, et al., 2014,
Multivalent helix mimetics for PPI-inhibition
, Organic & Biomolecular Chemistry, Vol: 13, Pages: 258-264, ISSN: 1477-0539The exploitation of multivalent ligands for the inhibition of protein–protein interactions has not yet been explored as a supramolecular design strategy. This is despite the fact that protein–protein interactions typically occur within the context of multi-protein complexes and frequently exploit avidity effects or co-operative binding interactions to achieve high affinity interactions. In this paper we describe preliminary studies on the use of a multivalent N-alkylated aromatic oligoamide helix mimetic for inhibition of p53/hDM2 and establish that protein dimerisation is promoted, rather than enhanced binding resulting from a higher effective concentration of the ligand.
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Journal articleBarnard A, Posocco P, Fermeglia M, et al., 2014,
Double-degradable responsive self-assembled multivalent arrays - temporary nanoscale recognition between dendrons and DNA
, ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 12, Pages: 446-455, ISSN: 1477-0520- Author Web Link
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- Citations: 30
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Journal articleBarnard A, Long K, Yeo DJ, et al., 2014,
Orthogonal functionalisation of α-helix mimetics
, ORGANIC & BIOMOLECULAR CHEMISTRY, Vol: 12, Pages: 6794-6799, ISSN: 1477-0520- Author Web Link
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- Citations: 23
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Journal articleTschiche A, Staedtler AM, Malhotra S, et al., 2014,
Polyglycerol-based amphiphilic dendrons as potential siRNA carriers for <i>in vivo</i> applications
, JOURNAL OF MATERIALS CHEMISTRY B, Vol: 2, Pages: 2153-2167, ISSN: 2050-750X- Author Web Link
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- Citations: 28
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Journal articlePrabhakaran P, Barnard A, Murphy NS, et al., 2013,
Aromatic Oligoamide Foldamers with a "Wet Edge" as Inhibitors of the -Helix-Mediated p53-hDM2 Protein-Protein Interaction
, EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, Vol: 2013, Pages: 3504-3512, ISSN: 1434-193X- Author Web Link
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- Citations: 24
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Journal articleBromfield SM, Barnard A, Posocco P, et al., 2013,
Mallard Blue: A High-Affinity Selective Heparin Sensor That Operates in Highly Competitive Media
, JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, Vol: 135, Pages: 2911-2914, ISSN: 0002-7863- Author Web Link
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- Citations: 95
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Journal articleBarnard A, Smith DK, 2012,
Self-Assembled Multivalency: Dynamic Ligand Arrays for High-Affinity Binding
, ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, Vol: 51, Pages: 6572-6581, ISSN: 1433-7851- Author Web Link
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- Citations: 149
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Journal articleOttaviani MF, Cangiotti M, Fiorani L, et al., 2012,
Probing dendron structure and nanoscale self-assembly using computer-aided analysis of EPR spectra
, NEW JOURNAL OF CHEMISTRY, Vol: 36, Pages: 469-476, ISSN: 1144-0546- Author Web Link
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- Citations: 10
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