Themed collection Celebrating the 5th Anniversary of RSC Medicinal Chemistry

A brief review of the history and current status of proximity induced modalities and a look at some of the opportunities for further exploiting these and related modalities, with a particular focus on opportunities beyond degradation.

We discuss how native mass spectrometry (nMS) is contributing important analytical insights to guide contemporary drug discovery and development. We focus on diverse modalities including targeted protein degradation (TPD), fragments (FBDD) and mRNA.

This article presents for the first time a critical analysis of emerging microbiota-sparing innovative therapeutic strategies, target-specificity and molecule-to-medicinal properties.

This review highlights recent advances (2020–2024) in 2,4-thiazolidinedione derivatives as anticancer agents, focusing on SAR insights, molecular mechanisms, and their potential to overcome drug resistance.

A general framework for target agnostic screening to exploit chemically induced proximity (CIP): key factors to consider balancing screening and mechanism of action (MoA) deconvolution.

A combinatorial approach integrating BLI and ligand-based NMR for RNA-focused fragment-based drug discovery.

This study identified HSN748 as a potent RET kinase solvent-front mutant inhibitor with a high central nervous system (CNS) permeability.

Accessible synthesis of DNA-encoded libraries of up to 3 million-members via sequential amide coupling, validated by CAIX screening. In silico analysis showed lead-like properties, and the libraries are available to support academic drug discovery.

The first degrader of an ER-resident protein (IRE1α) is described with properties more akin to a molecular glue than a traditional PROTAC, thus challenging the dogma of categorizing degrader modalities based on their physicochemical features.