Emma E. Cawood
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View article: Proteome-Wide Target Identification Using Reactive Metallo-Scaffolds (r-mS): A Platform for Metallodrug Discovery
Proteome-Wide Target Identification Using Reactive Metallo-Scaffolds (r-mS): A Platform for Metallodrug Discovery Open
Metal complexes offer unique opportunities as scaffolds in chemical biology and drug discovery, with tuneable geometry, modular coordination environments, and structural features not readily accessible with organic molecules. Here, we intr…
View article: Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening
Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening Open
Reactive fragment (RF) screening has emerged as an efficient method for ligand discovery across the proteome, irrespective of a target's perceived tractability. To date, however, the efficiency of subsequent optimisation campaigns has larg…
View article: Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening
Expedited SARS‐CoV‐2 Main Protease Inhibitor Discovery through Modular ‘Direct‐to‐Biology’ Screening Open
Reactive fragment (RF) screening has emerged as an efficient method for ligand discovery across the proteome, irrespective of a target's perceived tractability. To date, however, the efficiency of subsequent optimisation campaigns has larg…
View article: Robust proteome profiling of cysteine-reactive fragments using label-free chemoproteomics
Robust proteome profiling of cysteine-reactive fragments using label-free chemoproteomics Open
Identifying pharmacological probes for human proteins represents a key opportunity to accelerate the discovery of new therapeutics. High-content screening approaches to expand the ligandable proteome offer the potential to expedite the dis…
View article: Understanding β-strand mediated protein–protein interactions: tuning binding behaviour of intrinsically disordered sequences by backbone modification
Understanding β-strand mediated protein–protein interactions: tuning binding behaviour of intrinsically disordered sequences by backbone modification Open
Systematic backbone N -methylation of a SIM peptide results in faster, tighter binging to SUMO driven by a reduced entropy of activation; this opens new opportunities to develop inhibitors of β-strand mediated protein–protein interactions.
View article: Understanding β-strand mediated protein-protein interactions using peptidomimetics: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification
Understanding β-strand mediated protein-protein interactions using peptidomimetics: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification Open
A significant challenge in chemical biology is to understand and modulate protein-protein interactions (PPIs). Given that many PPIs involve a folded protein domain and a peptide sequence that is intrinsically disordered in isolation, pepti…
View article: Peptidomimetic inhibitors of β-strand mediated protein-protein interactions: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification
Peptidomimetic inhibitors of β-strand mediated protein-protein interactions: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification Open
A significant challenge for chemical biology is to develop methods that enable targeting of protein-protein interactions (PPIs). Given that many PPIs involve a folded protein domain and a peptide that is intrinsically disordered in isolati…
View article: Peptidomimetic inhibitors of β-strand mediated protein-protein interactions: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification
Peptidomimetic inhibitors of β-strand mediated protein-protein interactions: tuning binding affinity of intrinsically disordered sequences by covalent backbone modification Open
A significant challenge for chemical biology is to develop methods that enable targeting of protein-protein interactions (PPIs). Given that many PPIs involve a folded protein domain and a peptide that is intrinsically disordered in isolati…
View article: Bioorthogonal, Bifunctional Linker for Engineering Synthetic Glycoproteins
Bioorthogonal, Bifunctional Linker for Engineering Synthetic Glycoproteins Open
Post-translational glycosylation of proteins results in complex mixtures of heterogeneous protein glycoforms. Glycoproteins have many potential applications from fundamental studies of glycobiology to potential therapeutics, but generating…
View article: Microsecond Backbone Motions Modulate the Oligomerization of the DNAJB6 Chaperone
Microsecond Backbone Motions Modulate the Oligomerization of the DNAJB6 Chaperone Open
DNAJB6 is a prime example of an anti‐aggregation chaperone that functions as an oligomer. DNAJB6 oligomers are dynamic and subunit exchange is critical for inhibiting client protein aggregation. The T193A mutation in the C‐terminal domain …
View article: Microsecond Backbone Motions Modulate the Oligomerization of the DNAJB6 Chaperone
Microsecond Backbone Motions Modulate the Oligomerization of the DNAJB6 Chaperone Open
DNAJB6 is a prime example of an anti‐aggregation chaperone that functions as an oligomer. DNAJB6 oligomers are dynamic and subunit exchange is critical for inhibiting client protein aggregation. The T193A mutation in the C‐terminal domain …
View article: Microsecond backbone motions modulate the oligomerization of the DNAJB6 chaperone
Microsecond backbone motions modulate the oligomerization of the DNAJB6 chaperone Open
This directory contains data associated with 'Microsecond backbone motions modulate the oligomerization of the DNAJB6 chaperone'Cawood E.E, Clore G.M, Karamanos T.K1. relaxation: The residue numbering of reference 9 is used here. In order …
View article: Towards optimizing peptide-based inhibitors of protein–protein interactions: predictive saturation variation scanning (PreSaVS)
Towards optimizing peptide-based inhibitors of protein–protein interactions: predictive saturation variation scanning (PreSaVS) Open
An experimentally validated approach for in silico modification of peptide based protein–protein interaction inhibitors is described.
View article: Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules
Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules Open
Protein-protein interactions (PPIs) are involved in many of life's essential biological functions yet are also an underlying cause of several human diseases, including amyloidosis. The modulation of PPIs presents opportunities to gain mech…
View article: Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules
Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules Open
Protein-protein interactions (PPIs) are involved in many of life’s essential biological functions yet are also an underlying cause of several human diseases, including amyloidosis. The modulation of PPIs presents opportunities to gain mech…
View article: Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules
Modulation of Amyloidogenic Protein Self-Assembly Using Tethered Small Molecules Open
Protein-protein interactions (PPIs) are involved in many of life’s essential biological functions yet are also an underlying cause of several human diseases, including amyloidosis. The modulation of PPIs presents opportunities to gain mech…
View article: The role of the IT-state in D76N β2-microglobulin amyloid assembly: A crucial intermediate or an innocuous bystander?
The role of the IT-state in D76N β2-microglobulin amyloid assembly: A crucial intermediate or an innocuous bystander? Open
The D76N variant of human β2-microglobulin (β2m) is the causative agent of a hereditary amyloid disease. Interestingly, D76N-associated amyloidosis has a distinctive pathology compared with aggregation of WT-β2m, which occurs in dialysis-r…
View article: Structural mapping of oligomeric intermediates in an amyloid assembly pathway
Structural mapping of oligomeric intermediates in an amyloid assembly pathway Open
Transient oligomers are commonly formed in the early stages of amyloid assembly. Determining the structure(s) of these species and defining their role(s) in assembly is key to devising new routes to control disease. Here, using a combinati…