Themed collection Editors' collection: Chemical Biology

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

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.

F20 exhibits strong antibacterial activity through interacting with FtsZ.

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

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.

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

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

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

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

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.

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

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

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

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

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

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

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

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

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.

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.

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

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.

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

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

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

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.

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

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.

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.

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.

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

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.

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

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