Tag: PROTAC

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...

BSJ-4-116 is a Highly Potent and Selective PROTAC Based CDK12 Degrader

CDKs are serine/threonine protein kinases. They play major roles in regulating many different aspects of mammalian cellular function, most notably cell cycle and transcription. CDK12 is an emerging therapeutic target due to its role in regulating the transcription of DNA-damage response (DDR) genes. For example, ovarian and triple-negative breast...

ARV-110 is an Orally Active, Specific Androgen Receptor (AR) PROTAC Degrader

Proteolysis targeting chimeras also names PROTAC protein degraders. PROTACs are emerging as an excellent class of small molecule therapies for cancer and other diseases. As we all know, conventional inhibitors or antagonists usually block the enzymatic or signaling activity of target proteins. PROTACs harness a system present within every...

MD-222 is a First-in-Class Highly Potent PROTAC Degrader of MDM2

PROTACs are heterobifunctional molecules that connect a POI ligand to an E3 ubiquitin ligase recruiting ligand with an optimal linker. Researchers reported the discovery of MD-222. MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53...

LC-2 is a First-in-Class PROTAC-Based KRAS G12C Degrader

KRAS gene is one of the most frequently mutated oncogenes in cancer. KRAS encodes a small, membrane-bound GTPase that relays signals from receptor tyrosine kinases (RTKs). It promotes cell proliferation, cell differentiation, or cell survival. In normal cells, KRAS functions as a molecular switch, cycling between an inactive, GDP-bound “off” state and...