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Small molecules, big targets: drug discovery faces the protein–protein interaction challenge
DE Scott, AR Bayly, C Abell, J Skidmore - Nature Reviews Drug …, 2016 - nature.com
Protein–protein interactions (PPIs) are of pivotal importance in the regulation of biological
systems and are consequently implicated in the development of disease states. Recent work …
systems and are consequently implicated in the development of disease states. Recent work …
Modulators of protein–protein interactions
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
How proteins bind macrocycles
EA Villar, D Beglov, S Chennamadhavuni… - Nature chemical …, 2014 - nature.com
The potential utility of synthetic macrocycles (MCs) as drugs, particularly against low-
druggability targets such as protein-protein interactions, has been widely discussed. There …
druggability targets such as protein-protein interactions, has been widely discussed. There …
Modulating protein–protein interactions: the potential of peptides
L Nevola, E Giralt - Chemical Communications, 2015 - pubs.rsc.org
Protein–protein interactions (PPIs) have emerged as important and challenging targets in
chemical biology and medicinal chemistry. The main difficulty encountered in the discovery …
chemical biology and medicinal chemistry. The main difficulty encountered in the discovery …
Crystal engineering of hand-twisted helical crystals
A strategy is outlined for the design of hand-twisted helical crystals. The starting point in the
exercise is the one-dimensional (1D) plastic crystal, 1, 4-dibromobenzene, which is then …
exercise is the one-dimensional (1D) plastic crystal, 1, 4-dibromobenzene, which is then …
Systematic targeting of protein–protein interactions
Over the past decade, protein–protein interactions (PPIs) have gone from being neglected
as 'undruggable'to being considered attractive targets for the development of therapeutics …
as 'undruggable'to being considered attractive targets for the development of therapeutics …
Group-Based Optimization of Potent and Cell-Active Inhibitors of the von Hippel–Lindau (VHL) E3 Ubiquitin Ligase: Structure–Activity Relationships Leading to the Chemical Probe (2S,4R …
The von Hippel–Lindau tumor suppressor protein is the substrate binding subunit of the VHL
E3 ubiquitin ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) …
E3 ubiquitin ligase, which targets hydroxylated α subunit of hypoxia inducible factors (HIFs) …
Determination of protein-ligand interactions using differential scanning fluorimetry
M Vivoli, HR Novak, JA Littlechild… - Journal of visualized …, 2014 - pmc.ncbi.nlm.nih.gov
A wide range of methods are currently available for determining the dissociation constant
between a protein and interacting small molecules. However, most of these require access …
between a protein and interacting small molecules. However, most of these require access …
Overcoming chemical, biological, and computational challenges in the development of inhibitors targeting protein-protein interactions
Protein-protein interactions (PPIs) underlie the majority of biological processes, signaling,
and disease. Approaches to modulate PPIs with small molecules have therefore attracted …
and disease. Approaches to modulate PPIs with small molecules have therefore attracted …
[HTML][HTML] Hot spot-based design of small-molecule inhibitors for protein–protein interactions
Protein–protein interactions (PPIs) are important targets for the development of chemical
probes and therapeutic agents. From the initial discovery of the existence of hot spots at PPI …
probes and therapeutic agents. From the initial discovery of the existence of hot spots at PPI …