Editorial Board Members’ Collection Series: Multitarget-Directed Ligands for the Treatment of Multifactorial Diseases

Dear Colleagues,

The current disease treatments used in clinical use are based on the principle of “one molecule - one target - one malady”. However, problems are observed related to the development of resistance to therapy, overexpression of anti-apoptotic proteins, mutations in key signaling molecules, overexpression of drug efflux pumps, etc.

The design strategy for multi-target-directed ligands (MTDLs) is based on the incorporation of two or more distinct pharmacophores of different drugs in a single structure to develop hybrid molecules. MTDLs can bind/inhibit two or more targets simultaneously, following a poly-pharmacological/pleiotropic approach.

Modern drug discovery has the power to identify potential multifunctional ligands for biologically and clinically validated targets among a large number of compounds. The MTDL approach holds great potential in multifactorial diseases since it may significantly simplify treatment with respect to standard combination therapy, reduce the risk of possible drug–drug interactions, and most importantly, limit the insurgence of resistance in cancer therapy. Multi-factorial diseases such as cancer, neuroinflammation and stroke may greatly benefit from therapies that simultaneously target multiple key pathways and/or their pathogenic cross-talk.

In the present Special Issue, several multi-targeted approaches to multifactorial diseases are given in original articles, reviews and discussed from an interdisciplinary point of view, providing an updated picture of the latest progress in the field of “Multitarget-Directed Ligands for the Treatment of Multifactorial Diseases”.

Prof. Dr. Dimitra Hadjipavlou-Litina
Prof. Dr. Simona Rapposelli
Guest Editors

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