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Colocalization Features for Classification of Tumors Using Desorption Electrospray Ionization Mass Spectrometry Imaging.
Supervised modeling of mass spectrometry imaging (MSI) data is a crucial component for the detection of the distinct molecular characteristics of cancerous tissues. Currently, two types of supervised analyses are mainly used on...
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Antikörpergerichtete Therapien
In its various forms, cancer remains a leading cause of mortality and morbidity worldwide. Thus, it is widely accepted that finding innovative, life-changing drugs and therapeutic regimens is key for successful future cancer...
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Protein-Protein Conjugates
The residues cysteine and lysine are the undisputed champions of bioconjugation chemistry. Targeting other amino acids has been touted as a potential way to improve the synthesis of protein–peptide and protein–protein conjugates...
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The Impact of Activity-Based Protein Profiling in Malaria Drug Discovery.
Activity-based protein profiling (ABPP) is an approach used at the interface of chemical biology and proteomics that uses small molecular probes to provide dynamic fingerprints of enzymatic activity in complex proteomes. Malaria...
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Bioorthogonal Decaging Reactions for Targeted Drug Activation.
Bioorthogonal decaging reactions are highly selective transformations which involve the cleavage of a protecting group from a molecule of interest. Decaging reactions can be classified into subgroups depending on the nature of...
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Development of Antibody-Directed Therapies
Less is more: The efficacy of antibody-drug conjugates (ADCs) for cancer therapy is traditionally associated with cleavable linkers for payload release. Evidence now suggests that simpler constructs without cleavable moieties...
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Editorial overview
Chemical biology, a terminology coined early on in the mid-1940s in acorrespondence from George Beadle to Linus Pauling, has been laterdefined as ‘work in chemistry which is of biological interestdand to thatwork in biology in...
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A Sweet Galactose Transfer
The introduction of chemical reporter groups into glycan structures through metabolic oligosaccharide engineering (MOE) followed by bio-orthogonal ligation is an important tool to study glycosylation. We show the incorporation...
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The role of reversible and irreversible covalent chemistry in targeted protein degradation.
Proteolysis-targeting chimeras (PROTACs) that degrade disease-causing proteins by hijacking the endogenous ubiquitin-proteasome system have emerged as an exciting and transformative technology in both chemical biology and drug...
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Tetrazine Carbon Nanotubes for Pretargeted In Vivo "Click-to-Release" Bioorthogonal Tumour Imaging.
The bioorthogonal inverse-electron-demand Diels-Alder (IEDDA) cleavage reaction between tetrazine and trans-cyclooctene (TCO) is a powerful way to control the release of bioactive agents and imaging probes. In this study, a...
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π-Clamp-Mediated Homo- and Heterodimerization of Single-Domain Antibodies via Site-Specific Homobifunctional Conjugation.
Post-translational protein-protein conjugation produces bioconjugates that are unavailable via genetic fusion approaches. A method for preparing protein-protein conjugates using π-clamp-mediated cysteine arylation with...
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Site-selective installation of an electrophilic handle on proteins for bioconjugation.
Site-selective protein modification strategies can be used to insert non-natural functional groups into protein structures. Herein, we report on the use of the bis-electrophile 3-bromo-2-bromomethyl-1-propene as a reagent to...
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Chemical and Enzymatic Methods for Post-Translational Protein-Protein Conjugation.
Fusion proteins play an essential role in the biosciences but suffer from several key limitations, including the requirement for N-to-C terminal ligation, incompatibility of constituent domains, incorrect folding, and loss of...
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Posttranslational Chemical Mutagenesis
The field of chemical site-selective modification of proteins has progressed extensively in recent decades to enable protein functionalization for imaging, drug delivery, and functional studies. In this Perspective, we provide...
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