1. Signaling Pathways
  2. PROTAC
  3. PROTAC

PROTAC

PROTACs (Proteolysis Targeting Chimeric Molecules) are heterobifunctional nanomolecules that structurally comprised of two functional motifs linked by a linker. One motif is a small molecule ligand for the target protein of interest, while the other recognizes a specific E3 ligase. By recruiting an E3 ligase to a target protein and formation of a ligase:PROTAC:target ternary complex, A PROTAC leads to polyubiquitylation and subsequent degradation of target through ubiquitin-proteasome system (UPS). PROTACs have desirable features such as the ability to target the “undruggable” proteome and overcome the accumulation of the drug targets and will be promising targeted therapeutics for cancers.

Among the hundreds of E3 ligases, VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and cIAP (cellular inhibitor of apoptosis 1) are reported to target kinases (such as MEK, KRAS, CDK and Bcr/Abl), transcription factors (such as p53, STAT, RAR, ER and AR), and epigenetic readers (BET bromodomain such as BRD family) and are most widely used in the development of PROTACs. There are also some specific types of PROTACs, such as homo-PROTACs and general PROTACs for tagged fusion proteins. Homo-PROTACs intend to dimerize an E3 ligase and then induce its self-degradation, while general PROTACs for tagged fusion proteins can bind to general tags(such as HaloTag and FKBP12) and then induce the degradation of fusion proteins.

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