About this Research Topic

Background

Identification of the cellular targets of bioactive compounds is a persistent hot topic in chemical biology, pharmacology, and translational medicine. Successful identification of new drug targets can not only promote the elucidation of the novel molecular mechanisms of action, but also boost innovative drug R&D. In fact, there are many well-known research cases in history focusing on cellular targets identification, including FK506 targeting calcineurin, taxol targeting tubulin, epinephrine targeting adrenergic receptors, saxitoxin targeting ion channels, morphine targeting opioid receptor, as well as aspirin targeting cyclooxygenase.

However, there are still a large number of promising bioactive compounds without clearly identified cellular targets, severely hindering subsequent investigations of pharmacological mechanism and drug developments in clinical trials. Therefore, how to establish reliable and diversiform approaches has remained a rate-limiting step in advancing cellular target identification of bioactive compounds. Currently, several novel methodologies have been developed. For example, affinity-based probes play an important role in directly capturing the potential target proteins of bioactive compounds. Moreover, chemical proteomics and photo-cross-linked approaches further promote the process of this research area that can be considered as more unbiased methods for target identification. However, the current challenge for target identification resides in the lack of diversified and universal methodologies, urgently requiring further development.

In view of the significance of this scientific issue, this Research Topic invites the submission of high-quality manuscripts in the form of Reviews and Original Research articles, as well as Communication and Perspective papers covering novel methodologies for identifying drug targets and potential druggable targets discovery including:

1. Chemical probe design and synthesis for target identification
2. Identifying the cellular targets using affinity-based probes
3. Identifying the cellular targets by chemical proteomics, photo-cross-linked approaches, etc.
4. Identifying the cellular targets without chemical probe synthesis and other innovative approaches

Keywords: Target identification, Methodologies, Probes, Chemical proteomics, Photo-cross-link

Important note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

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