Vepdegestrant: The First PROTAC Heading to FDA Approval for Breast Cancer
Arvinas and Pfizer have submitted an NDA for vepdegestrant (ARV-471), making it the first PROTAC degrader to reach FDA review for hormone receptor-positive breast cancer.
Category Archives: PROTAC & Targeted Degradation
Targeted Degradation of Kinases: PROTAC Tools for Undruggable Kinase Targets
Discover how kinase-targeting PROTACs offer advantages over inhibitors: complete degradation, resistance overcoming, and scaffolding function elimination.
PROTAC Linker Design: How Linker Length and Chemistry Affect Degradation Efficiency
Explore how PROTAC linker design, length, and chemistry impact degradation efficiency. Learn about PEG, alkyl, and click chemistry linkers.
BET Degraders: PROTACs Targeting BRD4 for Cancer and Inflammation Research
BET proteins drive oncogenic transcription in cancer. Learn how PROTAC-based BET degraders like ARV-771 and dBET1 achieve complete protein degradation – and why degradation is superior to inhibition. Explore research tools and combination strategies.
E3 Ligase Ligands: CRBN, VHL, IAP, and MDM2 – Choosing the Right Warhead for Your PROTAC
Selecting the right E3 ligase warhead is critical for PROTAC success. Compare cereblon, VHL, IAP, and MDM2 ligands with practical guidance for warhead selection in different biological contexts.
Molecular Glues vs PROTACs: Two Approaches to Targeted Protein Degradation
Compare PROTACs and molecular glues: two complementary approaches to targeted protein degradation. Understand their design principles, advantages, and experimental applications.
PROTACs Explained: How Targeted Protein Degradation Works and Why It Matters
PROTACs hijack the cell’s ubiquitin-proteasome system to eliminate target proteins entirely. Learn the mechanism, the three building blocks (warhead, E3 ligase ligand, linker), and how to start PROTAC research with ready-to-use degrader compounds.
