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Edward Jeffrey Will

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Related publications (5)

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Discovery of De Novo Macrocycle Inhibitors of Histone Deacetylase 11

Christian Heinis, Alexander Lund Nielsen, Edward Jeffrey Will, Anne Sofie Luise Zarda

Histone deacetylase (HDAC) enzymes are epigenetic regulators that affect diverse protein function by removing acyl groups from lysine side chains throughout the proteome. The most recently discovered human isozyme, HDAC11, differs from other HDACs in subst ...

2025

Large Libraries of Structurally Diverse Macrocycles Suitable for Membrane Permeation

Christian Heinis, Alessandro Angelini, Alexander Lund Nielsen, Mischa Schüttel, Manuel Leonardo Merz, Xinjian Ji, Anne Sofie Luise Zarda, Ganesh Kumar Mothukuri, Zsolt Bognár, Edward Jeffrey Will

Macrocycles offer an attractive format for drug development due to their good binding properties and potential to cross cell membranes. To efficiently identify macrocyclic ligands for new targets, methods for the synthesis and screening of large combinator ...

Wiley-VCH Verlag GmbH2024

Discovery of macrocyclic inhibitors of challenging protein-protein interactions

Edward Jeffrey Will

Macrocycles are a therapeutic modality of interest for drugging challenging disease targets due to their high binding affinity and membrane permeability, enabling the discovery of orally delivered and efficacious therapeutics. Recent methods have enabled t ...

EPFL2024

Solid-phase peptide synthesis in 384-well plates

Christian Heinis, Alexander Lund Nielsen, Sevan Mleh Habeshian, Mischa Schüttel, Gontran Sangouard, Edward Jeffrey Will, Anne Sofie Luise Zarda

Newer solid-phase peptide synthesis and release strategies enable the production of short peptides with high purity, allowing direct screening for desired bioactivity without prior chromatographic purification. However, the maximum number of peptides that ...

2024

Screening macrocyclic peptide libraries by yeast display allows control of selection process and affinity ranking

Christian Heinis, Edward Jeffrey Will, Lluc Farrera Soler

Springer Science and Business Media LLC2025