PROTACs as Dual Motif Dmall Molecule Drugs: Past, present and future of Targeted Protein Degradation in Development
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".
Deadline for manuscript submissions: closed (1 November 2022) | Viewed by 645
Special Issue Editors
Interests: small molecule; fragments; PROTAC; structure/ligand based; drug development; nanoparticles/fibers/materials; drug delivery; formulations
Special Issues, Collections and Topics in MDPI journals
Interests: transcription factors; HDACi; SALL4; PROTAC; drug discovery & development
Special Issues, Collections and Topics in MDPI journals
2. Distinguished Professor, Department of Medicine, National University of Singapore; and Director, Cancer Science Institute of Singapore, Singapore
Interests: hematopoiesis; transcription factors; SALL4; C/EBPa; PROTAC; RNA biology; drug development
Special Issues, Collections and Topics in MDPI journals
2. Associate Professor, Harvard Medical School, Boston, MA, USA
Interests: transcription factors; C/EBPa; EGFR tyrosine kinase inhibitors; drug discovery and development
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
Combinatorial modes of tackling multidrug resistance diseases have benefitted patients with unmet medical needs. However, drug developers are still looking for multiple targeting single molecule drugs with broad spectrum activity and reduced toxicity. Recently, dual and multiple drug motifs containing small molecules have emerged as successful drugs for the treatment of diseases through multiple pathways or by interaction with multiple targets. Ubiquitination-mediated protein degradation by proteolysis-targeting chimeras (PROTACs) capable of selectively degrading oncogenic proteins has emerged as a more promising approach to curing cancer. PROTACs are bifunctional small molecules with amino piperidinedione containing E3 ligase binding and specific target oncogenic protein-binding motifs. These molecules bring the target oncogenic/disease-causing protein in proximity to E3 ligase and induce proteosomal degradation of the target protein. Many pharma companies and start-up biotechs are involved in the development of PROTAC drugs because of their huge potential. The past and current status of PROTAC drugs will be the main objective of this Special Issue.
In this Special Issue, we invite researchers to submit their latest research findings or review articles related to PROTAC-type molecules and other multiple targeting single molecule drugs for treatment of cancer and other diseases. Different classes of ligands for target protein binding, E3 ligase binding, and chain length of the spacers will be helpful for readers/researchers in this type of drug development, and hence, we encourage submissions discussing these aspects as well. Apart from conventional bifunctional target protein degraders, we invite articles based on molecular glues, large molecule-based degraders, and other less common unconventional degraders.
Dr. Sridhar RadhakrishnanProf. Li Chai
Prof. Daniel G. Tenen
Prof. Susumu Kobayashi
Guest Editor
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Keywords
- Proteolysis targeting chimera (PROTAC)
- Targeted protein degradation
- Dual motif drug molecules
- CRBN binders, linkers/conjugates
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