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Themed collection Editors' collection: Chemical Biology

35 items
Open Access Paper

Novel designed azo substituted semi-cyanine fluorescent probe for cytochrome P450 reductase detection and hypoxia imaging in cancer cells

An NIR hypoxia activated fluorescent probe was designed with fast performance and sensitivity response to hypoxic conditions.

Graphical abstract: Novel designed azo substituted semi-cyanine fluorescent probe for cytochrome P450 reductase detection and hypoxia imaging in cancer cells
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Aza-BODIPY probe for selective visualization of cyclooxygenase-2 in cancer cells

A bivalent indomethacin/Aza-BODIPY conjugate can selectively visualize the COX-2 enzyme in cancer and inflamed cells confirming its potential as a COX-2-specific biomarker in clinical applications.

Graphical abstract: Aza-BODIPY probe for selective visualization of cyclooxygenase-2 in cancer cells
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative

F20 exhibits strong antibacterial activity through interacting with FtsZ.

Graphical abstract: Antibacterial activity and mechanism of action of a thiophenyl substituted pyrimidine derivative
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery of human TyrRS inhibitors by structure-based virtual screening, structural optimization, and bioassays

A small molecule with potent activity diverts human Tyrosyl-tRNA synthetase (TyrRS) to the nucleus for protection against DNA damage.

Graphical abstract: Discovery of human TyrRS inhibitors by structure-based virtual screening, structural optimization, and bioassays
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Insights into the stereoselectivity of human SETD7 methyltransferase

This work clearly reveals the interaction of SAM/hSET7/(R/S)-PFI-2 systems, and confirms that the different bioactive energy barriers of (R)-PFI-2 and (S)-PFI-2 lead to the tremendously different inhibitory activities between these two antipodes.

Graphical abstract: Insights into the stereoselectivity of human SETD7 methyltransferase
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Novel cathepsin K inhibitors block osteoclasts in vitro and increase spinal bone density in zebrafish

Cathepsin K (Cat K) is a predominant cysteine protease and highly potent collagenase expressed in osteoclasts.

Graphical abstract: Novel cathepsin K inhibitors block osteoclasts in vitro and increase spinal bone density in zebrafish
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled via alkyl/amide linkers

A series of secondary amine-substituted isoindoline-1,3-dione-4-aminoquinolines were prepared via microwave heating and assayed for their anti-mycobacterial activities.

Graphical abstract: Synthesis, anti-mycobacterial and cytotoxic evaluation of substituted isoindoline-1,3-dione-4-aminoquinolines coupled via alkyl/amide linkers
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

A lysosome-targetable fluorescent probe for the simultaneous sensing of Cys/Hcy and GSH from different emission channels

A novel lysosome targetable fluorescent probe, Lyso-AC, that can selectively sense lysosome Cys/Hcy and GSH from different emission channels was developed.

Graphical abstract: A lysosome-targetable fluorescent probe for the simultaneous sensing of Cys/Hcy and GSH from different emission channels
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Design and synthesis of cysteine-specific labels for photo-crosslinking studies

The design and synthesis of cysteine specific diazirine containing labels is described.

Graphical abstract: Design and synthesis of cysteine-specific labels for photo-crosslinking studies
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity

The structure–activity and structure–kinetic relationships of a new tert-butylphenylthiazole series with oxadiazole linkers were conducted with the objective of obtaining a new orally available antibacterial compounds.

Graphical abstract: tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery of trisubstituted nicotinonitrile derivatives as novel human GCN5 inhibitors through AlphaScreen-based high throughput screening

The trisubstituted nicotinonitrile derivative DC_HG24-01 was discovered as a novel potent hGCN5 inhibitor with efficient bioactivity against MV4-11 cells.

Graphical abstract: Discovery of trisubstituted nicotinonitrile derivatives as novel human GCN5 inhibitors through AlphaScreen-based high throughput screening
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

In vitro evaluation of anti-hepatoma activity of brevilin A: involvement of Stat3/Snail and Wnt/β-catenin pathways

Brevilin A, a natural sesquiterpene lactone extracted from Centipeda minima, has been found to exhibit anti-tumor effect.

Graphical abstract: In vitro evaluation of anti-hepatoma activity of brevilin A: involvement of Stat3/Snail and Wnt/β-catenin pathways
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Effect of alternan versus chitosan on the biological properties of human mesenchymal stem cells

Alternan α-1,3- and α-1,6-linked glucan, promotes proliferation, migration, and differentiation of human MSCs.

Graphical abstract: Effect of alternan versus chitosan on the biological properties of human mesenchymal stem cells
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Insight into the effect of quinic acid on biofilm formed by Staphylococcus aureus

QA effectively inhibited S. aureus biofilm formation. The key genes of biofilm inhibition induced by QA were agrA and sarA.

Graphical abstract: Insight into the effect of quinic acid on biofilm formed by Staphylococcus aureus
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents

Novel compounds comprising 2,2-dimethylbenzopyran and cinnamic acid were synthesized. BN-07 significantly increased survival rate of primary neurons, superior to edaravone.

Graphical abstract: Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Site-specific labeling of an anti-MUC1 antibody: probing the effects of conjugation and linker chemistry on the internalization process

Four antibody conjugates were prepared to investigate how the conjugation and linker chemistry would impact ADC endocytosis and intracellular trafficking.

Graphical abstract: Site-specific labeling of an anti-MUC1 antibody: probing the effects of conjugation and linker chemistry on the internalization process
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Design, synthesis and broad-spectrum Bcr-Abl inhibitory activity of novel thiazolamide–benzamide derivatives

3m showed good broad-spectrum Bcr-Abl inhibition of wild-type and T315I mutant.

Graphical abstract: Design, synthesis and broad-spectrum Bcr-Abl inhibitory activity of novel thiazolamide–benzamide derivatives
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery of novel elongator protein 2 inhibitors by compound library screening using surface plasmon resonance

This study employed a label-free high-throughput library screening method and verified a drug candidate to reduce TNF-α induced differentiation inhibition.

Graphical abstract: Discovery of novel elongator protein 2 inhibitors by compound library screening using surface plasmon resonance
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Tetra-fluorinated aromatic azide for highly efficient bioconjugation in living cells

A fast strain-promoted azide–alkyne cycloaddition based on tetra-fluorinated aromatic azide was developed and applied to label proteins and living cells with high efficiency.

Graphical abstract: Tetra-fluorinated aromatic azide for highly efficient bioconjugation in living cells
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

2′-Deoxy-5-(hydroxymethyl)cytidine: estimation in human cancer cells with a simple chemosensor

A new chemosensor, CS-1, has been developed and characterized for the selective detection and quantification of 2′-deoxy-5-(hydroxymethyl)cytidine (5hmC) in human cancer cells.

Graphical abstract: 2′-Deoxy-5-(hydroxymethyl)cytidine: estimation in human cancer cells with a simple chemosensor
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Bufalin suppresses colorectal cancer cell growth through promoting autophagy in vivo and in vitro

Specific groups in Asia, including the Chinese, are more susceptible to colorectal cancer (CRC).

Graphical abstract: Bufalin suppresses colorectal cancer cell growth through promoting autophagy in vivo and in vitro
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Halogen bonding for the design of inhibitors by targeting the S1 pocket of serine proteases

BrBA binds to the S1 pocket of urokinase with Br facing the base of the pocket by halogen bonds, while iodine of IBA binds to the S1 in the opposite way.

Graphical abstract: Halogen bonding for the design of inhibitors by targeting the S1 pocket of serine proteases
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Compound F779-0434 causes synthetic lethality in BRCA2-deficient cancer cells by disrupting RAD52–ssDNA association

A novel compound named F779-0434 caused synthetic lethality in BRCA2-deficient cancer cells by disrupting RAD52–ssDNA associations.

Graphical abstract: Compound F779-0434 causes synthetic lethality in BRCA2-deficient cancer cells by disrupting RAD52–ssDNA association
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Bicyclo[2.2.1]heptane containing N,N′-diarylsquaramide CXCR2 selective antagonists as anti-cancer metastasis agents

Novel bicyclo[2.2.1]heptane containing N,N′-diarylsquaramide CXCR2 selective antagonists were identified as potent anti-cancer metastatic agents.

Graphical abstract: Bicyclo[2.2.1]heptane containing N,N′-diarylsquaramide CXCR2 selective antagonists as anti-cancer metastasis agents
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery of novel inhibitors of RNA silencing suppressor P19 based on virtual screening

The combined virtual and experimental screening method is a efficient strategy to discover inhibitors of RNA silencing suppressor.

Graphical abstract: Discovery of novel inhibitors of RNA silencing suppressor P19 based on virtual screening
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity

6b17 and 9b are active against 3 tested bacteria while they block IL-6/STAT3, TLR4/NF-κB and TNF-α/NF-κB pathways. 7b1 and 8b1 are selectively active against E. faecalis but 7b1 selectively blocks TNF-α/NF-κB pathway and 8b1 selectively blocks TLR4/NF-κB pathway.

Graphical abstract: Discovery and preliminary SAR of 14-aryloxy-andrographolide derivatives as antibacterial agents with immunosuppressant activity
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Discovery of N-cyclobutylaminoethoxyisoxazole derivatives as novel sigma-1 receptor ligands with neurite outgrowth efficacy in cells

Herein we reported a series of 14 novel derivatives based on the N-cyclobutylaminoethoxyisoxazole scaffold.

Graphical abstract: Discovery of N-cyclobutylaminoethoxyisoxazole derivatives as novel sigma-1 receptor ligands with neurite outgrowth efficacy in cells
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

An innovative small molecule for promoting neuroreparative strategies

In this study, a new regenerative strategy to treat several neurodegenerative diseases is suggested by the use of a multitarget approach induced by our small molecule, MC111.

Graphical abstract: An innovative small molecule for promoting neuroreparative strategies
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Gs protein peptidomimetics as allosteric modulators of the β2-adrenergic receptor

From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors

Herein we describe the design, synthesis, and biological evaluation of a novel series of tranylcypromine-based LSD1 inhibitors via conformational restriction using spiro ring systems.

Graphical abstract: Novel spirocyclic tranylcypromine derivatives as lysine-specific demethylase 1 (LSD1) inhibitors
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Nucleobase-modified antisense oligonucleotides containing 5-(phenyltriazol)-2′-deoxyuridine nucleotides induce exon-skipping in vitro

We investigated the potential of nucleobase-modified antisense oligonucleotides to induce exon-skipping, and found that 5-(phenyltriazol)-2′-deoxyuridine-modified antisense oligonucleotides induced efficient exon-skipping in vitro.

Graphical abstract: Nucleobase-modified antisense oligonucleotides containing 5-(phenyltriazol)-2′-deoxyuridine nucleotides induce exon-skipping in vitro
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone

Indolizinone could selectively recognize c-myc promoter G-quadruplex.

Graphical abstract: Selective recognition of c-myc promoter G-quadruplex and down-regulation of oncogene c-myc transcription in human cancer cells by 3,8a-disubstituted indolizinone
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Development of a series of bis-triazoles as G-quadruplex ligands

Maintenance of telomeres – specialized complexes that protect the ends of chromosomes – is provided by the enzyme complex telomerase, which is a key factor that is activated in more than 80% of cancer cells, but absent in most normal cells.

Graphical abstract: Development of a series of bis-triazoles as G-quadruplex ligands
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Hydrophobic tagging-mediated degradation of Alzheimer's disease related Tau

HyT-Tau-CPP reduced Tau levels in Alzheimer's disease (AD) mouse model, and appeared to be a promising candidate for AD treatment.

Graphical abstract: Hydrophobic tagging-mediated degradation of Alzheimer's disease related Tau
From the themed collection: Editors' collection: Chemical Biology
Open Access Paper

Evaluation of structure–activity relationships of ginsenosides against amyloid β induced pathological behaviours in transgenic Caenorhabditis elegans

The systematic in vivo study comparing the effects of different ginsenosides on Aβ induced toxicity and cognitive impairment.

Graphical abstract: Evaluation of structure–activity relationships of ginsenosides against amyloid β induced pathological behaviours in transgenic Caenorhabditis elegans
From the themed collection: Editors' collection: Chemical Biology
35 items

About this collection

The use of chemical tools to explore biology has led to an explosion in new discoveries impacting cell biology and medicine. This includes the use of small molecules, peptides and natural products as chemical probes for the discovery of novel biology and validation of new therapeutic targets; the design of fluorescent probes for visualizing cellular and in vivo biology; and the development of new bioorthogonal chemistries with applicability to living systems.

This collection, guest edited by Associate Editor Amanda Garner (University of Michigan, USA), highlights exciting work in the area of chemical biology. It includes 35 recently published original research papers, in addition to 3 reviews, covering many areas related to the design, discovery and application of chemical tools to further our understanding of biology and medicine. This compilation serves as an excellent example of the high-quality and breadth of research that is showcased in RSC Advances, which will hopefully inspire new applications of chemistry to biological problems.

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