Category: Lymphoma

Aderbasib is a Highly Potent and Orally Active Inhibitor of ADAM10 and ADAM17

ADAMs (a disintegrin and metalloproteinases), originally also known as MDC proteins (metalloproteinase/disintegrin/cysteine-rich). And ADAMs belong to the Metzincins superfamily of metalloproteases. Recently, studies have found ADAM genes exist in animals, choanoflagellates, fungi and some groups of green algae. Importantly, ADAMs mediates proteolytic ectodomain release. And the ectodomain shedding is...

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...

Lenalidomide, a Ligand of CRBN, is an Orally Active Immunomodulator

Immunomodulatory imide drugs (IMiDs) are a class of immunomodulatory drugs containing an imide group. The discovery of anti-angiogenic and anti-inflammatory properties promoted the development of Thalidomide analogs. These compounds bind Cereblon (CRBN), the substrate adaptor for the CRBN-CRL4 E3 ubiquitin ligase, and modulate the substrate specificity of the enzyme....

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...

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...