Category: Lymphoma

Pirtobrutinib is an Orally Active, Highly Selective and non-Covalent BTK Inhibitor

Bruton’s tyrosine kinase (BTK) is a non-receptor kinase that plays a crucial role in oncogenic signaling. It is critical for the proliferation and survival of leukemic cells in many B cell malignancies. BTK has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases...

Elimusertib is an Orally Available and Selective ATR Inhibitor

TM serine/threonine kinase (ATM) is a serine/threonine-protein kinase and can be recruited and activated by DNA double-strand breaks. Specifically, ATM phosphorylates several key proteins. These proteins initiate the activation of DNA damage checkpoints, leading to cell cycle arrest, DNA repair, or apoptosis. Besides, ATM belongs to the superfamily of...

CXD101 is a Selective and Orally Active Class I HDAC Inhibitor

Aberrant expression of classical HDACs associates with a variety of malignancies, including solid and hematological tumors. HDACs have also been found broadly dysregulated in multiple myeloma (MM). In particular, the mechanisms that HDACs regulate tumorigenesis are quite diverse. HDACs induce a range of cellular and molecular effects through the...

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...

CJ-2360 is a Potent and Orally Active ALK Inhibitor

Anaplastic lymphoma kinase (ALK) is a receptor tyrosine kinase belonging to the insulin receptor (IR) kinase superfamily. It highly expresses in adult brain tissue and exerts an important role in the development of the nervous system. Deregulation of ALK originally presents by the identification of at (2;5) chromosomal translocation...

BI-3802-Induced Polymerization Triggers Degradation of BCL6

PROTAC has been developed to degrade a wide range of clinically relevant targets. These small-molecule degraders engage both the E3 ligase and the target protein to promote the formation of a substrate–drug–ligase ternary complex. Although degraders can show notable efficacy and sustained depletion of targets, some proteins are resistant....

CC-90010 is a Reversible and Orally Active BET Inhibitor

Come straight to the point, CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. The bromodomain and extra-terminal domain (BET) proteins, epigenetic readers, recognize and bind acetylated lysine residues. The BET protein family comprises the ubiquitously expressed...