Tag: AML

BTSA1 is a High Affinity and Orally Active BAX Activator

The BCL-2 family protein BAX is a central mediator of apoptosis. Besides, overexpression of anti-apoptotic BCL-2 proteins contributes to tumor development and resistance to therapy by suppressing BAX and its activators. Cancer cells depend on their ability to enforce cell survival pathways and block cell death mechanisms. Moreover, pro-apoptotic...

MRT199665 is a ATP-Competitive MARK/SIK/AMPK Inhibitor

In acute myeloid leukemia (AML), chemotherapy resistance remains prevalent and poorly understood. AML are cancers of the blood. They originate in the hematopoietic progenitor cells as a result of the accumulation of genetic mutations that lead to cell transformation. Prevalence of mutations of genes encoding regulators of gene expression...

A-366 is a Potent Histone Methyltransferase G9a Inhibitor

Epigenetic alterations to the genome take place via modifications to the DNA or histones. Meanwhile, those modifications lead to changes in gene expression. Generally, histone lysine methylation is a prominent kind of epigenetic regulation for change of the structure chromatin and gene expression. HMTs have recently generated increasing interest...

ASLAN003 is an Orally Active hDHODH Inhibitor

Dihydroorotate dehydrogenase (DHODH) is a highly conserved enzyme. All organisms express it. Class-1 DHODHs are cytoplasmic and single-domain enzymes. Conversely, class-2 DHODHs are membrane-associated and two-domain enzymes. Both classes of DHODHs use FMN to oxidize DHODH. To regenerate FMN, class-1 enzymes use a soluble cofactor, such as NAD+ or fumarate,...