Themed collection Articles behind our 2025 journal covers

Small-molecule and antibody-based targeted therapies for intrahepatic cholangiocarcinoma (iCCA): addressing promising oncogenic molecular alterations, including IDH1, FGFR2, BRAF, HER2, and the PD-1/PD-L1 axis.

The radiohybrid concept: a significant extension of radionuclide theranostics – a fast-growing field in radiopharmaceutical sciences offering personalised and precise treatment options by combining specific diagnosis with targeted endoradiotherapy.

Inhibitors of mycobacterial ATP synthase, such as bedaquiline, TBAJ-587, TBAJ-876, squaramides, GaMF1, and DeMF1, break the energy metabolism and effectively inhibit Mtb, offering promising strategies against mycobacterial infections.

The Wnt/β-catenin signaling pathway plays a critical role in various biological processes, including cell proliferation, differentiation, and tissue homeostasis.

Here we describe the design, synthesis and validation of the first NF-κB PROTAC degrader with demonstrable subunit selectivity for RelA/p65.

The first PROTAC degrader of ASK1, dASK1-VHL (60), was rationally designed and validated via in vitro assays and PK studies, demonstrating therapeutic efficacy in an MCD diet-induced MASH mouse model, underscoring its promise in metabolic diseases.

The key markers of immunogenic cell death were detected in mammalian cell cultures upon co-incubation with gramicidin S and its photoswitchable analogues at the sub-membranolytic concentrations, suggesting an immunotherapeutic potential for peptides.

Scaffold-hopping from luteolin led to a new class of submicromolar pseudoflavonoid-based influenza endonuclease inhibitors. A novel binding mode of compound 36 was observed in the PA-Nter active site.

New 1-(4-phenyl)adamantane and 1-(4-phenoxyphenyl)adamantane derivatives, functionalised with imidazolines, linear amidines, aminoguanylhydrazone and thiosemicarbazone moieties present activity against T. brucei.

Application of copper-catalyzed azide–alkyne cycloaddition (CuAAC) “click” reactions assemble bivalent proteolysis-targeting chimeras (PROTACs) constituents targeting tyrosyl-DNA phosphodiesterase 1 (TDP1).

Short MD simulations help identify the putative bioactive conformation of small molecule agonists at the NOP receptor providing useful information for the structure-based design of novel analgesic drugs.

Several fused-thiazole derivatives have been studied for antimelanoma properties. Lead compounds are effective tumor growth inhibitors in mice, which are potent β- and γ-actin cytoskeleton inhibitors with a probable mechanism of β-PARVIN inhibition.

In pursuit of novel anti-plasmodial agents, a library of triclosan-based dimers both with and without a 1H-1,2,3 triazole core were designed, synthesized and evaluated in order to achieve a multitargeted approach.

This article presents A-ring functionalized quinones via a modern and efficient new strategy involving the generation and capture of benzyne quinones and their evaluation against Trypanosoma cruzi.

Non-small cell lung cancer (NSCLC), the leading cause of cancer-related mortality worldwide, poses a formidable challenge due to its heterogeneity and the emergence of resistance to targeted therapies.