Tag: PROTAC

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...

dCBP-1 is a Selective PROTAC Degrader of p300/CBP

The paralogous chromatin regulators CREB-binding protein (CBP) and p300 are factors critical for establishing and activating enhancer-mediated transcription. The CREB-binding protein (CBP) and p300 are important factors for activating enhancer-mediated transcription. These proteins consist of at least 10 distinct functional domains. Most of them interact with over 400 other proteins,...

JH-XI-10-02 is a Highly Potent and Selective PROTAC CDK8 Degrader

PROteolysis Targeting Chimeras (PROTACs) regulate protein function by degrading target proteins instead of inhibiting them, providing more sensitivity to drug-resistant targets. PROTACs show better selectivity compared to classic inhibitors. PRTOACs have outperformed not only in cancer diseases but also in immune disorders, viral infections, and neurodegenerative diseases. PROTACs present...

MZP-54 is a Selective BRD3/4 PROTAC Degrader

PROTACs are bivalent chemical protein degraders. In particular, PROTACs degrade a specific endogenous protein of interest (POI) by harnessing the E3 ubiquitin ligase pathway. Especially, PROTACs is a powerful small-molecule approach for inducing protein degradation. Moreover, PROTACs conjugate a target warhead to an E3 ubiquitin ligase ligand via a...

VZ185 is a Selective Dual BRD7/9 PROTAC Degrader

Targeted protein degradation is an emerging strategy to use small molecules to knock down a protein by hijacking the ubiquitin-proteasome system. PROTACs are bifunctional degrader molecules. They compose a ligand for the target protein and a ligand for E3 ligase recruitment, connected by a linker. An attractive feature of...