Category: Lymphoma

Iberdomide (CC-220) is an Orally Active Cereblon (CRBN) E3 Ligase Modulator (CELMoD)

Cereblon (CRBN) is a key protein in autosomal recessive nonsyndromic mental retardation. Specifically, it plays an intermediary role in helping immunomodulatory drugs play their immunomodulatory and tumor-killing roles. Besides, CRBN is highly conserved from plants to mammals, and mRNA expression in humans, rats, and mice is common. CRBN interacts...

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...