Fig. 1: Schematic illustration of the proposed drug design strategy and the current work. | Nature Communications

Fig. 1: Schematic illustration of the proposed drug design strategy and the current work.

From: Pharmacophore hybridisation and nanoscale assembly to discover self-delivering lysosomotropic new-chemical entities for cancer therapy

Fig. 1: Schematic illustration of the proposed drug design strategy and the current work.The alternative text for this image may have been generated using AI.

a An interdisciplinary drug design strategy is proposed to integrate the conventional fields of medicinal chemistry and nanomedicine. Drugs are named as one-component new-chemical-entity nanomedicines (ONNs), which are designed according to the strategies of conventional drug design and molecular self-assembly so that they could acquire the advantages from the perspectives of both drug discovery and drug delivery. b The proof-of-concept experiment in this work: discovery of self-delivering lysosomotropic bisaminoquinoline (BAQ) derivatives for cancer therapy. The BAQ derivatives, generated from the hybridisation of lysosomotropic detergents and the BAQ-based autophagy inhibitor, can self-assemble into BAQ ONNs that show enhanced functions in vitro, excellent delivery profiles and significant in vivo therapeutic effects as single agents. Moreover, they also possess high drug-loading efficiency to deliver the additional drug into tumour sites, thus generating a promising application of combination therapy.

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