Category: Acute Lymphoblastic Leukemia

SZUH280 is a Potent And Selective PROTAC HDAC8 Degrader

Histone deacetylase 8 (HDAC8) is a class I histone deacetylase. Unlike other class I HDACs, it localizes both in the nucleus and in the cytoplasm. HDAC8 can also target non-histone proteins, such as the structural maintenance of chromosome 3 (SMC3) cohesin protein, retinoic acid induced 1 (RAI1) and p53....

MMRi62, a Ferroptosis Inducer Targeting MDM2-MDM4

MDM2 and MDM4 have established cancer drug targets. Additionally, they are also inhibitors of p53 activity and are amplified in many cancer types. In particular, the targeting of MDM2–p53 interactions is a novel strategy that is pursued to unleash the antitumor activity of p53. Furthermore,  there needs to cover...

SJ988497, a PROTAC JAK2 Degrader, used for Acute Lymphoblastic Leukemia Research

CRLF2-rearranged (CRLF2r) acute lymphoblastic leukemia (ALL) is relevant with a poor outcome in children and adults. CRLF2r-ALL accounts for more than half of Philadelphia chromosome-like (Ph-like) ALL. Noticeably, the overexpression of CRLF2 activates JAK-STAT and parallel signaling pathways. However, small molecules inhibiting JAKs are variable and limited. Importantly, Using...

U7D-1 is a Selective USP7 PROTAC Degrader For Leukemia Research

Ubiquitin-specific proteinase 7 (USP7) is a kind of de ubiquitination enzyme (DUB), which can remove ubiquitin and protect substrate protein from degradation. Besides, the full activity of USP7 requires the C-terminal Ub-like domain to fold back to the catalytic domain. Moreover, this allows the active site to be remodeled...

MPM-1, an Anticancer agent, is a Marine Eusynstyelamides Mimic

Autophagy  is the natural and conservative degradation of cells. Specifically, it can remove unnecessary or dysfunctional components through lysosomal-dependent regulation mechanisms. Besides, it allows the orderly degradation and recycling of cellular components. It eliminates molecular and subcellular elements through lysosomal-mediated degradation. This includes nucleic acids, proteins, lipids, and organelles...

Reversine is a ATP-Competitive Aurora Kinase Inhibitor

Aurora kinases are serine/threonine kinases that play a prominent role in mitotic regulation. The Aurora A kinase, the “polar” kinase resides at spindle poles during mitosis. It is implicated in the control of centrosome duplication, maturation, and separation. Aurora A is important for the formation of a bipolar mitotic...