Themed collection Meet the Editor webinar: celebrating our speakers and their contributions to the field

Dual-functional therapeutics with the ability to tackle both bacterial infection and associated hyper-inflammation hold great promise for mitigating complicated infections and sepsis.

A two-in-one vancomycin derivative that acts through multiple mechanisms to inhibit drug-resistant Gram-positive bacteria and resensitizes critical priority Gram-negative pathogens to carbapenems.

Gram-negative bacteria pose a significant challenge due to two major resistance elements: impermeability of the outer membrane and the overexpression of efflux pumps, contributing to antibiotic resistance. SMA tackles both and aids in antibiotic rejuvenation.

Peptidomimetic antimicrobials exhibit a selective interaction with bacterial cells over mammalian cells once they have achieved an optimum amphiphilic balance (hydrophobicity/hydrophilicity) in the molecular architecture.

Presently, there are several challenges that need to be overcome in the development of treatments that can effectively inhibit tumor growth, prevent the spread of tumor metastases, and protect the host against recurrence.

A set of triazinedione peptidomimetics of an Arg-Trp-x-x-Trp motif found in MraY were found to show antimicrobial activity against antibiotic-resistant clinical isolates, via a novel mechanism of action.

Structure-guided design led to the discovery of a small and potent peptide inhibitor of measles virus fusion protein.

Potent and stable cyclic peptide inhibitors of Cx43 were identified. Their therapeutic potential was enhanced by the addition of a lipid motif (preserving water solubility), and a targeting peptide, for delivery to cardiac endothelial cells.

We designed and synthesized novel IOX1-based PROTACs, which can selectively degrade KDM3A and KDM3B to eliminate colorectal cancer stem cells through inhibition of Wnt signaling.

Pseudo-natural products (PNPs) combine fragments derived from NPs in ways that are not found in nature, and may lead to the discovery of novel chemotypes for unexpected targets or the identification of unprecedented bioactivities.

The large language models GPT-3 and GTP-3.5 were challenged to predict the activity and hemolysis of antimicrobial peptides from their sequence and compared to recurrent neural networks and support vector machines.

IL-6 production in treated human synovial fibroblasts from rheumatoid arthritis patients has been utilised to select candidates from a targeted library of queuine tRNA ribosyltransferase (QTRT) substrates for subsequent in vivo screening in murine experimental autoimmune encephalomyelitis.

Dysregulation of the networking of RNA-binding proteins (RBPs) and RNAs drives many human diseases, including cancers, and the targeting of RNA–protein interactions (RPIs) has emerged as an exciting area of RNA-targeted drug discovery.

We report the synthesis, characteristics, and biological evaluations of a novel theranostic agent, P14, for both in vitro and in vivo imaging of central Aβ plaques, inhibition of Aβ aggregation, and neuronal damage as well as behavioral deficits.

Utilizing a combination of structure-based design, MCR synthesis, biophysics, and protein crystallography to innovate a novel tetrazole scaffold targeting the PD-1/PD-L1 immune checkpoint protein complex.

We introduced a concept of prodrugs activated by H₂O₂ and mitochondrial OH⁻, which is applicable to camptothecin and its derivatives.

In this study, a unique strategy of scaffold-hopping-based molecular editing of a bioactive agent NSC-666719 was investigated, which led to the development of new benzodithiazinedioxide-guanidine based anticancer agents with Polβ inhibition.

Maleimide is used in antibody–drug conjugate (ADC) generation to attach the drug-linker to the antibody. Maleimide linkers with hydrolysis-enabled maleimides were designed. Corresponding ADCs were made and subjected to thermal stress, and succinimide ring hydrolysis and drug release were measured.