Chen, Po-Han, et al. “Modulation of phosphoprotein activity by phosphorylation targeting chimeras (PhosTACs).” ACS chemical biology 16.12 (2021): 2808-2815. In the rapidly evolving field of drug development, targeting protein post-translational modifications (PTMs) has emergedRead More…
Protein-degraders: The New Go-to For Tackling Autoimmune Issues
Protein targeted degradation chimera is an emerging protein degradation strategy that has been booming in recent years. It was first proposed by Craig Crews et al. in 2001. Its basic principle isRead More…
Can PROTAC Therapy Be a Hope for AIDS Patients?
Nef is an accessory protein encoded by HIV-1, HIV-2, and other primate lentiviruses and is closely related to viral replication, persistent infection, and the development of AIDS. Nef interacts with a varietyRead More…
Exploring the Impact of E3 Ligase Choice on PROTAC Effectiveness
The field of drug discovery is witnessing a revolutionary shift with the advent of Proteolysis Targeting Chimeras (PROTACs). This innovative therapeutic strategy is redefining how we approach the degradation of proteins, especiallyRead More…
Linker Matters in PROTAC Design
Proteolysis targeting chimera (PROTAC) technology represents a breakthrough development in the field of drug discovery, utilizing the ubiquitin proteasome system to specifically degrade disease-related proteins. PROTACs are characterized by their unique heterobifunctionalRead More…
New Role Introduced: PDF-Bin, Protein Targeting the Degradation “Dumpcart”
Over the past two decades, protein-targeting degradation technologies (TPD), epitomized by PROTAC (proteolysis targeting chimera), have undergone rapid development and are considered one of the most promising breakthrough technologies for tackling difficult-to-drugRead More…
Extracellular Protein Targeted Degradation (eTPD): Six Drug Discovery Modalities
Targeted protein degradation (TPD) has emerged over the past decade as a major novel drug modality for the removal of intracellular proteins with bispecific small molecules that recruit proteins of interest (POIs)Read More…
Review: Molecular Glue vs. PROTAC
Targeted protein degradation (TPD) primarily degrades target proteins through the ubiquitin-proteasome and lysosome, and according to the specific mechanism of action, it can be further subdivided into nearly 10 different technical routes,Read More…
A New PROTAC Targeting the METTL3-METTL14 Complex Has Arrived!
N 6-methyladenosine (m6A) methylation is the most abundant type of RNA modification, primarily catalyzed by the METTL3-METTL14 methyltransferase complex (MTC). This complex includes the core catalytic proteins METTL3 and METTL14, as wellRead More…
Researchers Have Made New Advances in the Field of Protein Degradation
ROTAC technology has advantages such as targeting non-druggable targets, high catalytic activity, and overcoming drug resistance, making it a new strategy in drug development. Traditional PROTAC design and synthesis require a significantRead More…