Tag: PROTAC

ARV-471 is an Estrogen Receptor PROTAC Degrader for Breast Cancer

PROTAC is a heterobifunctional molecule containing two small molecule binding moieties. Specifically, PROTACs in cells seek and selectively bind to target proteins. PROTAC then recruits specific E3 ligases to the target protein. Besides, it forms a ternary complex in close proximity to the target protein and E3 ligase. In...

MS159 is a First-In-class NSD2 PROTAC degrader for Multiple Myeloma Research

Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule, including two active domains, and a linker. Importantly, it can remove specific unwanted proteins. PROTAC is a technology based on the ligand binding of TAP and then the degradation of TAP. PROTAC provides an alternative approach to those so-called non-druggable...

MS170 is a PROTAC AKT Degrader

The alternative name of serine/threonine kinase AKT is protein kinase B (PKB). Three closely related genes in humans: AKT1 (PKB-α), AKT2 (PKB-β), and AKT3 (PKB-γ) encode PKB. AKT is an important component of the PI3K/AKT/mammalian target of rapamycin (m-TOR) signaling pathway.  It also regulates fundamental cellular and physiological processes,...

MS4322 is a First-in-Class PRMT5 PROTAC Degrader

PRMT5 is a member of type II protein arginine methyltransferases (PRMTs). When interacting with its binding partner MEP50, PRMT5 catalyzes monomethylation and symmetric dimethylation of arginine residues of its histone substrates. These substrates include H3R2, H3R8, and H4R3, and its nonhistone substrates, including p53, EGFR, N-MYC, SmD3, and RNA...

SIM1 is a PROTAC Based BET Family Degrader

Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule that acts by inducing selective intracellular proteolysis. Specifically, bifunctional PROTAC molecule is including ligands of target protein (POI) and covalent ligands of E3 ubiquitin ligase (E3). After binding to POI, PROTAC can recruit E3 for POI ubiquitination. This ubiquitination is...

XY028-140 is a Selective CDK4 and CDK6 PROTAC Degrader

CDKs (Cyclin-dependent kinases) are the families of protein kinases first discovered for their role in regulating the cell cycle. By definition, a CDK binds a regulatory protein called a cyclin. Without cyclin, CDK has little kinase activity; only the cyclin-CDK complex is an active kinase. The four major mechanisms...

DP-C-4 is a CRBN-Based dual PROTAC for EGFR and PARP

Proteolysis targeting chimera (PROTAC) is a bifunctional small molecule. Interestingly, dual PROPACs are dual-targeted degradation molecules that combine the concepts of PROTAC and dual-targeting. Dual PROPACs degrade two completely different pathway targets while simultaneously taking advantage of both PROTAC and dual-target drugs. Thus, dual PROPACs not only achieve the...