Themed collection Most popular 2021 chemical biology articles

30 items
Open Access Review Article

Fluorescent probes for visualizing ROS-associated proteins in disease

Abnormal proteins, influenced by reactive oxygen species (ROS), are directly related to the development of various diseases.

Graphical abstract: Fluorescent probes for visualizing ROS-associated proteins in disease
From the themed collection: Most popular 2021 chemical biology articles
Open Access Review Article

Recent advances in activity-based probes (ABPs) and affinity-based probes (AfBPs) for profiling of enzymes

This review highlights the recent advances in the use of activity-based probes (ABPs) and affinity-based probes (AfBPs), and summarizes their design strategies (based on inhibitors and substrates) and detection approaches.

Graphical abstract: Recent advances in activity-based probes (ABPs) and affinity-based probes (AfBPs) for profiling of enzymes
From the themed collection: Most popular 2021 chemical biology articles
Open Access Review Article

Synergizing the potential of bacterial genomics and metabolomics to find novel antibiotics

Antimicrobial resistance is a major public concern and novel antibiotics are largely based on natural products. We summarize recent analytical and genome based technological developments that gain increasing importance in the natural products field.

Graphical abstract: Synergizing the potential of bacterial genomics and metabolomics to find novel antibiotics
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Improved broad-spectrum antibiotics against Gram-negative pathogens via darobactin biosynthetic pathway engineering

Heterologous expression of a synthetically engineered darobactin gene cluster in E. coli yields new darobactin derivatives with improved anti-Gram-negative activity. Targeted gene deletions provide first insights into biosynthetic steps.

Graphical abstract: Improved broad-spectrum antibiotics against Gram-negative pathogens via darobactin biosynthetic pathway engineering
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Contributions to cytochrome c inner- and outer-sphere reorganization energy

Efficient delocalization of the redox-active molecular orbital (RAMO) in HtWT results in an increase in HAB value which in turn accelerates the electron transfer (ET) rate in spite of the higher reorganization energy (λ) than the HtQ64V mutant.

Graphical abstract: Contributions to cytochrome c inner- and outer-sphere reorganization energy
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Coumarin luciferins and mutant luciferases for robust multi-component bioluminescence imaging

Near-infrared probes were developed from coumarin-modified luciferins and engineered luciferases, enabling facile multiplexed bioluminescence imaging.

Graphical abstract: Coumarin luciferins and mutant luciferases for robust multi-component bioluminescence imaging
From the themed collection: 2021 Chemical Science HOT Article Collection
Open Access Edge Article

RE-SELEX: restriction enzyme-based evolution of structure-switching aptamer biosensors

RE-SELEX is the first homogenous method for in vitro evolution of structure-switching DNA aptamers.

Graphical abstract: RE-SELEX: restriction enzyme-based evolution of structure-switching aptamer biosensors
From the themed collection: 2021 Chemical Science HOT Article Collection
Open Access Edge Article

Mechanistic insights into dopaminergic and serotonergic neurotransmission – concerted interactions with helices 5 and 6 drive the functional outcome

Neurotransmitter contacts within the receptor binding site differentially contribute to the overall functional response: transmembrane helix (TM) 5 contacts promote G protein coupling whereas concerted TM5–TM6 contacts enhance β-arrestin recruitment.

Graphical abstract: Mechanistic insights into dopaminergic and serotonergic neurotransmission – concerted interactions with helices 5 and 6 drive the functional outcome
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Monitoring phagocytic uptake of amyloid β into glial cell lysosomes in real time

Glial cell phagocytosis of pH-dependent amyloid-β, AβpH, in live and fixed cultures, brain tissue sections, retina, cortex and in live animals useful for studying function in health and disease.

Graphical abstract: Monitoring phagocytic uptake of amyloid β into glial cell lysosomes in real time
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Discovering protein–protein interaction stabilisers by native mass spectrometry

Stabilising protein–protein interactions is challenging, yet therapeutically important. Native mass spectrometry can be used to monitor binding equilibria, allowing identification and measurement of novel protein–protein interaction stabilisers.

Graphical abstract: Discovering protein–protein interaction stabilisers by native mass spectrometry
From the themed collection: 2021 ChemSci Pick of the Week Collection
Open Access Edge Article

A copper-free and enzyme-free click chemistry-mediated single quantum dot nanosensor for accurate detection of microRNAs in cancer cells and tissues

A copper-free and enzyme-free click chemistry-mediated single quantum dot nanosensor enables sensitive detection of microRNAs in cancer cells and tissues.

Graphical abstract: A copper-free and enzyme-free click chemistry-mediated single quantum dot nanosensor for accurate detection of microRNAs in cancer cells and tissues
From the themed collection: 2021 Chemical Science HOT Article Collection
Open Access Edge Article

Cellular delivery of dinucleotides by conjugation with small molecules: targeting translation initiation for anticancer applications

Ligand assisted cellular delivery of negatively charged dinucleotides, which are potential antagonists of the protooncogenic protein eIF4E.

Graphical abstract: Cellular delivery of dinucleotides by conjugation with small molecules: targeting translation initiation for anticancer applications
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Genetically-encoded discovery of proteolytically stable bicyclic inhibitors for morphogen NODAL

A two-fold symmetric linchpin (TSL) converts readily available phage-displayed disulfide peptide libraries to proteolytically stable bicyclic peptides. The bicyclic phage library was screened to discover an antagonist of NODAL morphogen.

Graphical abstract: Genetically-encoded discovery of proteolytically stable bicyclic inhibitors for morphogen NODAL
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries

Highly efficient forward and reverse on-DNA amide couplings were developed exploiting hydrophobic linkers in combination with the micelle forming surfactant TPGS-750M. The method is highly effective for a wide range of substrates in the synthesis of DNA-encoded libraries.

Graphical abstract: Highly efficient on-DNA amide couplings promoted by micelle forming surfactants for the synthesis of DNA encoded libraries
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Cell–cell interactions via non-covalent click chemistry

We designed complementary artificial markers that were introduced on the surface of cells previously modified by metabolic glycoengineering. These recognition markers enable unnatural cell–cell adhesion through non-covalent click chemistry.

Graphical abstract: Cell–cell interactions via non-covalent click chemistry
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Rapid and robust cysteine bioconjugation with vinylheteroarenes

Vinylheteroarene linkers can chemoselectively modify cysteine residues in proteins and antibodies. These linkers give stable bioconjugates, and were used to synthesise efficacious antibody-drug conjugates.

Graphical abstract: Rapid and robust cysteine bioconjugation with vinylheteroarenes
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Quantitative interrogation of protein co-aggregation using multi-color fluorogenic protein aggregation sensors

A little leak will sink a great ship! We prepared a series of multi-color protein aggregation sensors and developed a dual-color thermal shift assay to simultaneously and quantitatively report on protein co-aggregation of two different proteins.

Graphical abstract: Quantitative interrogation of protein co-aggregation using multi-color fluorogenic protein aggregation sensors
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Evaluation of fully-functionalized diazirine tags for chemical proteomic applications

The chemical proteomic properties of five diazirine-based, fully-functionalized photoaffinity tags, including a newly developed, minimal tag, were compared. This study provides guidance for the development of new photoaffinity probes.

Graphical abstract: Evaluation of fully-functionalized diazirine tags for chemical proteomic applications
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Total synthesis, isolation, surfactant properties, and biological evaluation of ananatosides and related macrodilactone-containing rhamnolipids

We show that macrolactonization of gluco- and rhamnolipids dramatically interfere with their surfactant properties and biological activity.

Graphical abstract: Total synthesis, isolation, surfactant properties, and biological evaluation of ananatosides and related macrodilactone-containing rhamnolipids
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Phase separation of p53 precedes aggregation and is affected by oncogenic mutations and ligands

Mutant p53 tends to form aggregates with amyloid properties, especially amyloid oligomers inside the nucleus, which are believed to cause oncogenic gain-of-function (GoF).

Graphical abstract: Phase separation of p53 precedes aggregation and is affected by oncogenic mutations and ligands
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Linchpins empower promiscuous electrophiles to enable site-selective modification of histidine and aspartic acid in proteins

Linchpin-enabled promiscuous electrophile uncovers an unchartered reactivity landscape for the precision engineering of proteins.

Graphical abstract: Linchpins empower promiscuous electrophiles to enable site-selective modification of histidine and aspartic acid in proteins
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Chemoproteomic profiling of itaconations in Salmonella

Bioorthogonal probes have been developed to enable quantitative and site-specific profiling of itaconate modifications in Salmonella.

Graphical abstract: Chemoproteomic profiling of itaconations in Salmonella
From the themed collection: 2021 ChemSci Pick of the Week Collection
Open Access Edge Article

Light-guided intrabodies for on-demand in situ target recognition in human cells

Nanobodies are ideal to visualize and modulate targets in living cells. We designed a versatile platform for generating photo-conditional intrabodies by genetic code expansion. After illumination, the intrabodies show fast and stable binding.

Graphical abstract: Light-guided intrabodies for on-demand in situ target recognition in human cells
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Rational design of iridium–porphyrin conjugates for novel synergistic photodynamic and photothermal therapy anticancer agents

Iridium–porphyrin conjugates assembled in nanoparticles are photosensitizers that exhibit excellent photothermal imaging and synergistic PDT and PTT in vivo.

Graphical abstract: Rational design of iridium–porphyrin conjugates for novel synergistic photodynamic and photothermal therapy anticancer agents
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Target-templated de novo design of macrocyclic D-/L-peptides: discovery of drug-like inhibitors of PD-1

In silico design of heterochiral cyclic peptides that bind to a specific surface patch on the target protein (PD-1, in this case) and disrupt protein–protein interactions.

Graphical abstract: Target-templated de novo design of macrocyclic d-/l-peptides: discovery of drug-like inhibitors of PD-1
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Query-guided protein–protein interaction inhibitor discovery

Small-molecule protein–protein interaction inhibitors were prioritised on the basis of shape similarity to secondary structure-based queries incorporating hot-spot residues.

Graphical abstract: Query-guided protein–protein interaction inhibitor discovery
From the themed collection: 2021 Chemical Science HOT Article Collection
Open Access Edge Article

Nature-inspired dimerization as a strategy to modulate neuropeptide pharmacology exemplified with vasopressin and oxytocin

Structural and pharmacological study of parallel, antiparallel and N- to C-terminal cyclized homo- and heterodimers of vasopressin and oxytocin. This study spotlights dimerization as a strategy to modulate the pharmacology of neuropeptides.

Graphical abstract: Nature-inspired dimerization as a strategy to modulate neuropeptide pharmacology exemplified with vasopressin and oxytocin
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes

Sulfonyl-triazole probes modified with a kinase recognition element are developed for live cell activity-based profiling to identify tyrosine sites located in catalytic and regulatory domains that are important for kinase function.

Graphical abstract: Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes
From the themed collection: Most popular 2021 chemical biology articles
Open Access Edge Article

Traceless parallel peptide purification by a first-in-class reductively cleavable linker system featuring a safety-release

A first-in-class reductively cleavable linker system that enables parallel and traceless purification of peptides through a safety-release is introduced with three linker types and showcased by rapid production of 20 personalized neoantigen peptides.

Graphical abstract: Traceless parallel peptide purification by a first-in-class reductively cleavable linker system featuring a safety-release
From the themed collection: 2021 ChemSci Pick of the Week Collection
Open Access Edge Article

Fluorogenic probes for detecting deacylase and demethylase activity towards post-translationally-modified lysine residues

We developed “turn-on” fluorescent probes that detect enzymatic lysine deacylation and demethylation critical for epigenetic and other cellular phenomena, using intramolecular O- to N-ester transfer reactions.

Graphical abstract: Fluorogenic probes for detecting deacylase and demethylase activity towards post-translationally-modified lysine residues
From the themed collection: Most popular 2021 chemical biology articles
30 items

About this collection

This specially curated collection pulls together some of the most popular articles from 2021 in the field of chemical biology. The collection presents some outstanding contributions to the field, ranging from antibiotics to biosensors, and as with all Chemical Science articles – they are all completely free to access and read. We hope you enjoy browsing through this collection.


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