Themed collection 2021 RSC Chemical Biology HOT Article Collection

In vivo imaging has become in recent years an incredible tool to study biological events and has found critical applications in diagnostic medicine.

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.

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.

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.

G-rich nucleic acid sequences encompassing G-tracts of varying lengths can fold into different non-canonical G-quadruplexes with distinct structural features.

This review discusses the development of sulfonyl–triazoles and highlights the merits and opportunities for deploying this sulfur electrophile for biological discovery.

Chemical biology strategies can play important roles in studying the complexity of SARS-CoV-2–host interactions at molecular level detail.

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.

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.

In this review, we give a concise overview of the known biosynthetic princples of class III and IV lanthipeptide synthtases.

An overview of the latest tools and technologies to investigate the roles of site-specific O-GlcNAcylation in vitro and in vivo.

Co-crystallization and biochemical analyses with structurally defined oligosaccharides show the low reactivity of HS 3-OST-3 toward 6-O-sulfated substrates is due to inhibition of enzyme activity by 6-O-sulfated oligosaccharides.

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.

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.

A revision is proposed to the biosynthetic pathway to the well-known red pigment prodigiosin via a new thioester intermediate.

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.

Cyclic peptides containing unnatural amino acids can modulate Lys-48 ubiquitin chains in cells and animals.

Using the protein–protein interaction of Mcl-1/Noxa, two methods for efficient modulator discovery are directly compared.

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.

We identified potent, functionalisable BMX inhibitors and revealed their covalent mode of binding to BMX by X-ray crystallography.

Altering local dielectric properties induced by solvent shielding, enhances polar interactions and leads to enthalpically driven recognition of polar substrates.

Naphthalimide-appended oligopyridylamide peptidomimetic modulate islet amyloid polypeptide amyloidogenesis and disaggregate preformed oligomers and fibrils into non-toxic conformations at substoichiometric concentration.

In-depth study of intriguing bacterial interrupted adenylation domains from seven distinct families and six different types.