Themed collection Small molecules for chemical biology

17 items
Open Access Review Article

Targeting the RNA demethylase FTO for cancer therapy

Chemical modulation of the RNA m6A demethylase FTO for cancer therapy.

Graphical abstract: Targeting the RNA demethylase FTO for cancer therapy
Open Access Review Article

Wnt signaling activation: targets and therapeutic opportunities for stem cell therapy and regenerative medicine

Overview of the Wnt signaling pathway and targets of Wnt activators.

Graphical abstract: Wnt signaling activation: targets and therapeutic opportunities for stem cell therapy and regenerative medicine
Open Access Review Article

Natural Trojan horse inhibitors of aminoacyl-tRNA synthetases

The structures, biosynthesis, and modes of action of albomycin, microcin C and agrocin 84, antibiotics targeting aminoacyl-tRNA synthetases, are reviewed. Using bioinformatics several new putative aminoacyl-tRNA synthetase inhibitors are predicted.

Graphical abstract: Natural Trojan horse inhibitors of aminoacyl-tRNA synthetases
From the themed collection: Small molecules for chemical biology
Open Access Review Article

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.

Graphical abstract: Biological functions of supramolecular assemblies of small molecules in the cellular environment
Open Access Review Article

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.

Graphical abstract: Development and biological applications of sulfur–triazole exchange (SuTEx) chemistry
From the themed collection: Articles in 2021
Open Access Review Article

Modified nucleoside triphosphates in bacterial research for in vitro and live-cell applications

Modified nucleoside triphosphates (NTPs) are invaluable tools to probe bacterial enzymatic mechanisms, develop novel genetic material, and engineer drugs and proteins with new functionalities.

Graphical abstract: Modified nucleoside triphosphates in bacterial research for in vitro and live-cell applications
From the themed collection: Small molecules for chemical biology
Open Access Communication

Target identification of mouse stem cell probe CDy1 as ALDH2 and Abcb1b through live-cell affinity-matrix and ABC CRISPRa library

CDy1 is a powerful tool to distingusih embryonic stem cells for reprogramming studies and regeneration medicine.

Graphical abstract: Target identification of mouse stem cell probe CDy1 as ALDH2 and Abcb1b through live-cell affinity-matrix and ABC CRISPRa library
From the themed collection: Small molecules for chemical biology
Open Access Communication

A two-step resin based approach to reveal survivin-selective fluorescent probes

A dual-resin system was developed that united confocal-fluorescent imaging for hit identification and microscale NMR for hit isolation and structure elucidation. Using this approach, we identified two natural products that bound to the inhibitor of apoptosis protein, survivin.

Graphical abstract: A two-step resin based approach to reveal survivin-selective fluorescent probes
From the themed collection: Small molecules for chemical biology
Open Access Paper

Design, synthesis and evaluation of tryptophan analogues as tool compounds to study IDO1 activity

We report the rational design, novel syntheses and biophysical and in silico evaluation of tryptophan-inspired tool compounds to probe the illusive MOA of the clinically-relevant heme-dioxygenase protein, IDO1.

Graphical abstract: Design, synthesis and evaluation of tryptophan analogues as tool compounds to study IDO1 activity
From the themed collection: Small molecules for chemical biology
Open Access Paper

Alkyl vs. aryl modifications: a comparative study on modular modifications of triphenylphosphonium mitochondrial vectors

Alkyl chain extension and aryl methylation can be employed to enhance mitochondrial uptake in triphenylphosphonium vectors. Here we compare these complementary strategies and their mitochondrial-targeting effects using a modular synthetic approach.

Graphical abstract: Alkyl vs. aryl modifications: a comparative study on modular modifications of triphenylphosphonium mitochondrial vectors
Open Access Paper

Dual concentration-dependent effect of ascorbic acid on PAP(248–286) amyloid formation and SEVI-mediated HIV infection

Human semen contains various amyloidogenic peptides derived from Prostatic Acid Phosphatase (PAP) and Semenogelin proteins that are capable of enhancing HIV-1 infection when assembled into fibrils.

Graphical abstract: Dual concentration-dependent effect of ascorbic acid on PAP(248–286) amyloid formation and SEVI-mediated HIV infection
From the themed collection: Small molecules for chemical biology
Open Access Paper

Phosphinate esters as novel warheads for activity-based probes targeting serine proteases

Phosphinate electrophiles are developed as activity-based probes for serine proteases. They can be used for gel-based profiling as well as for microscopy-based detection, and their use is here demonstrated on neutrophil serine proteases.

Graphical abstract: Phosphinate esters as novel warheads for activity-based probes targeting serine proteases
From the themed collection: Small molecules for chemical biology
Open Access Paper

Xanthine-based photoaffinity probes allow assessment of ligand engagement by TRPC5 channels

Diazirine-containing photoaffinity probes, based on the potent and selective TRPC1/4/5 channel inhibitor Pico145, allowed the development of an assay to probe cellular interactions between TRPC5 protein and xanthine-based TRPC5 channel modulators.

Graphical abstract: Xanthine-based photoaffinity probes allow assessment of ligand engagement by TRPC5 channels
From the themed collection: Small molecules for chemical biology
Open Access Paper

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.

Graphical abstract: Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors
Open Access Paper

Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools

Discovery of a potent, small-molecule, fluorescent agonist of the follicle-stimulating hormone receptor (FSHR) for selective staining of FSHR-expressing cells.

Graphical abstract: Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools
From the themed collection: Small molecules for chemical biology
Open Access Paper

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.

Graphical abstract: Macrocyclic peptides that inhibit Wnt signalling via interaction with Wnt3a
From the themed collection: RSC Chemical Biology Editors' Choice
Open Access Paper

A mechanism-inspired UDP-N-acetylglucosamine pyrophosphorylase inhibitor

UDP-N-acetylglucosamine pyrophosphorylase (UAP1) catalyses the last step in eukaryotic biosynthesis of uridine diphosphate-N-acetylglucosamine (UDP-GlcNAc), converting UTP and GlcNAc-1P to the sugar nucleotide.

Graphical abstract: A mechanism-inspired UDP-N-acetylglucosamine pyrophosphorylase inhibitor
17 items

About this collection

The use of small molecules in chemical biology encompasses a wide range of multidisciplinary research, including the use of chemical tools as probes for imaging and target identification, small molecule inhibitors of protein-protein interactions, signal inhibition and the assessment of ligand engagement among others.  Small molecule research can compliment and contribute to the development of pharmaceuticals and other approaches to tackling disease.

This collection is intended to highlight the importance of multidisciplinary research at the chemistry-biology interface.  Much of this exciting and ground-breaking research using small molecules has been published in RSC Chemical Biology and is collected here for you to explore.

New articles on the topic will be added periodically.

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