Design and synthesis of metabolic chemical reporters for the visualization and identification of glycoproteins
This review details a brief history of the synthesis and characterization of metabolic chemical reporters used to study glycosylation before describing recent applications and finishing with considerations and limitations of reporter molecules.
Fragment-based covalent ligand discovery
Covalent fragment-based ligand discovery greatly facilitates the discovery of useful fragments for drug discovery and helps unveil chemical-tractable biological targets in native biological systems.
Biological functions of supramolecular assemblies of small molecules in the cellular environment
Supramolecular assemblies of small molecules, exhibiting emergent properties, are becoming a new and dynamic molecular platform for biological functions and for developing novel therapeutic approaches.
Structural motifs and intramolecular interactions in non-canonical G-quadruplexes
G-rich nucleic acid sequences encompassing G-tracts of varying lengths can fold into different non-canonical G-quadruplexes with distinct structural features.
Development and biological applications of sulfur–triazole exchange (SuTEx) chemistry
This review discusses the development of sulfonyl–triazoles and highlights the merits and opportunities for deploying this sulfur electrophile for biological discovery.
The chemical biology of coronavirus host–cell interactions
Chemical biology strategies can play important roles in studying the complexity of SARS-CoV-2–host interactions at molecular level detail.
Transfer hydrogenation catalysis in cells
Recent developments in transfer hydrogenation catalysis and photocatalysis in cancer cells by synthetic metal complexes are reviewed. They offer exciting new ways to modulate biochemical pathways for drug development and biotechnology.
DNA folds threaten genetic stability and can be leveraged for chemotherapy
Alternative DNA structures (including G-quadruplexes and DNA junctions) represent promising targets for combinatorial chemotherapeutic treatments aiming at fostering genomic instability and impeding DNA repair.
Matters of class: coming of age of class III and IV lanthipeptides
In this review, we give a concise overview of the known biosynthetic princples of class III and IV lanthipeptide synthtases.
Tools for functional dissection of site-specific O-GlcNAcylation
An overview of the latest tools and technologies to investigate the roles of site-specific O-GlcNAcylation in vitro and in vivo.
Labelling of DNA and RNA in the cellular environment by means of bioorthogonal cycloaddition chemistry
Labelling of nucleic acids as biologically important cellular components is a crucial prerequisite for the visualization and understanding of biological processes.
In vivo delivery of a fluorescent FPR2/ALX-targeted probe using focused ultrasound and microbubbles to image activated microglia
Targeted imaging agent labels activated microglia when delivered into the brain with focused ultrasound and microbubbles – a tool to investigate inflammation in neurological disorders.
Metathramycin, a new bioactive aureolic acid discovered by heterologous expression of a metagenome derived biosynthetic pathway
Heterologous expression of an aromatic polyketide biosynthetic gene cluster recovered from a New Zealand soil metagenome library resulted in the discovery of new bioactive aureolic acids.
Hyaluronan (HA)-inspired glycopolymers as molecular tools for studying HA functions
Glycopolymers based on hyaluronan (HA) were synthesised as homopolymers and alternating copolymers and used as probes to study the interactions with known HA-binding proteins and peptides.
Revision in the first steps of the biosynthesis of the red antibiotic prodigiosin: use of a synthetic thioester to validate a new intermediate
A revision is proposed to the biosynthetic pathway to the well-known red pigment prodigiosin via a new thioester intermediate.
Site-specific modification and segmental isotope labelling of HMGN1 reveals long-range conformational perturbations caused by posttranslational modifications
Using protein semi-synthesis, segmentally isotope-labelled variants of nucleosome-binding protein HMGN1 were generated with site-specific posttranslational modifications to explore their structural and functional effects.
In vivo modulation of ubiquitin chains by N-methylated non-proteinogenic cyclic peptides
Cyclic peptides containing unnatural amino acids can modulate Lys-48 ubiquitin chains in cells and animals.
A live-cell assay for the detection of pre-microRNA–protein interactions
Leveraging bioorthogonal chemistry- and split-luciferase assay technologies, we have devised a new assay for the live-cell detection of RNA–protein interactions, RNA interaction with Protein-mediated Complementation Assay or RiPCA.
In silico peptide-directed ligand design complements experimental peptide-directed binding for protein–protein interaction modulator discovery
Using the protein–protein interaction of Mcl-1/Noxa, two methods for efficient modulator discovery are directly compared.
A peptidic inhibitor for PD-1 palmitoylation targets its expression and functions
We show for the first time that PD-1 is palmitoylated, identify DHHC9 as the predominant enzyme for its palmitoylation, and reveal the molecular mechanisms underlying its effects on PD-1 stability and functions. Importantly, we also designed PD1-PALM, a competitive inhibitor of PD-1 palmitoylation, and this first-in-class molecule may inspire the development of new checkpoint inhibitors.
Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors
We identified potent, functionalisable BMX inhibitors and revealed their covalent mode of binding to BMX by X-ray crystallography.
Enhancing the enthalpic contribution of hydrogen bonds by solvent shielding
Altering local dielectric properties induced by solvent shielding, enhances polar interactions and leads to enthalpically driven recognition of polar substrates.
Harnessing the PD-L1 interface peptide for positron emission tomography imaging of the PD-1 immune checkpoint
Leveraging interface peptides in PD-L1 for PET imaging of PD-1, providing a new paradigm for radiotracer development.
Sub-stoichiometric inhibition of IAPP aggregation: a peptidomimetic approach to anti-amyloid agents
Naphthalimide-appended oligopyridylamide peptidomimetic modulate islet amyloid polypeptide amyloidogenesis and disaggregate preformed oligomers and fibrils into non-toxic conformations at substoichiometric concentration.
A thorough analysis and categorization of bacterial interrupted adenylation domains, including previously unidentified families
In-depth study of intriguing bacterial interrupted adenylation domains from seven distinct families and six different types.
Macrocyclic peptides that inhibit Wnt signalling via interaction with Wnt3a
Discovery and optimization of de novo macrocyclic peptide binders of Wnt3a through RaPID screening against an afamin-stabilized Wnt3a complex, capable of inhibiting Wnt signalling by direct interaction to the Wnt protein.
About this collection
This collection celebrates the very best work published in RSC Chemical Biology, including articles personally chosen by our world-renowned editorial team, and articles highlighted as “HOT”. New selections will be added on a monthly basis.
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