SIAIS178 is a Potent and Selective PROTAC-Based BCR-ABL Degrader

Proteolysis targeting chimeras (PROTACs) work by inducing selective intracellular proteolysis rather than acting as a conventional enzyme inhibitor. Besides, PROTACs consists of two covalently linked protein-binding molecules. One can engage an E3 ubiquitin ligase, and another binds to a target protein meant for degradation. Moreover, PROTACs need only to...

BETd-260 is a Potent PROTAC BET Degrader

The bromodomain and extra-terminal (BET) family proteins consist of BRD2, BRD3, BRD4, and testis-specific BRDT members. They are epigenetic “readers” and play a key role in the regulation of gene transcription. BET proteins are attractive therapeutic targets for cancer and other human diseases. In this study, BETd-260 is capable...

ZXH-3-26 is a Selective PROTAC BRD4 Degrader

Targeting protein degradation refers to small molecule induces ubiquitination and degradation of disease targets. These small molecules simultaneously recruit both a ubiquitin E3 ligase and the target protein, then to be ubiquitinated. Therefore, PROTACs represent a functional application of chemically induced protein dimerization. BRD4 acts as an attractive target...

dTRIM24 is a Selective PROTAC Degrader of TRIM24

TRIM24 is a multidomain protein characterized as a co-regulator of transcription. Especially, dTRIM24 acts as a chemical probe of an emerging cancer dependency. Recruitment of the VHL E3 ubiquitin ligase by dTRIM24 elicits potent and selective degradation of TRIM24. TRIM24 has been posited as a dependency in numerous cancers,...

DT2216 is a Selective PROTAC Degrader of BCL-XL

BCL-XL is a member of the Bcl-2 protein family and a transmembrane molecule in mitochondria. Specifically, it acts as an anti-apoptotic protein by blocking the release of mitochondrial contents such as cytochrome c. Besides, BCL-XL is a well-validated cancer target and eventually leads to caspase activation and eventually programmed...

Tetrac is a Thyrointegrin Receptor Antagonist

In the angiogenesis process, integrins are members of a family of cell surface transmembrane receptors. They play a critical role particularly in blood vessel formation and the local release of vascular growth factors. Thyroid hormones such as T4 and T3 promote angiogenesis and tumor cell proliferation via integrin αvβ3...

Cilengitide is a Selective Integrin Inhibitor for αvβ3 and αvβ5 Receptor

Integrins are heterodimeric cell surface adhesion receptors that consist of two noncovalently associated alpha and beta subunits. In particular, Integrins are heterodimeric transmembrane proteins composed of one α and one β subunit. Especially, Integrins are crucially important because they are the main receptor proteins that cells use to bind...