Targeted Degradation of Proteins and Beyond

Dear Colleagues,

Highlighted by the development of the proteolysis-targeting chimera (PROTAC) technology in 2001, targeted protein degradation (TPD) has had a revolutionary impact on drug discovery. The degrader molecules, mostly designed and chimeric in structure, physically link the protein of interest with the degradation effectors and, through hijacking proteasomal, lysosomal, and other cellular degradation pathways, efficiently eliminate the target proteins located intracellularly, extracellularly, or on the cell membrane. The proximity-induced and event-driven pharmacology of TPD greatly expands the potential for drug development against a large number of disease-causing proteins, many of which were previously considered undruggable. In recent years, the principle and capability of TPD has been expanded to cellular targets beyond proteins, including other biomacromolecules, including RNA, cellular organelles, such as damaged mitochondria, and even small molecules. Significant progress has also been made in overcoming the many challenges imposed by the unique physicochemical properties and modes of action of TPD drugs, such as low systemic bioavailability due to a relatively large molecular weight, poor ability to cross physiologic barriers and the cell membrane, potential off-target and on-target toxicity, the undesirable Hook effect, and acquired resistance. This Special Issue of Pharmaceutics on "Targeted Degradation of Proteins and Beyond" welcomes original research papers, communications, or review articles related to the science and technology of targeted degradation, including but not limited to the design, engineering, molecular and cell biology, formulations, delivery, pharmaceutics, pharmacodynamics, and toxicology of targeted degraders.

Prof. Dr. Longping Wen
Prof. Dr. Yunjiao Zhang
Guest Editors

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