Tag: AML

Talacotuzumab is an IgG1 CD123-Neutralizing Monoclonal Antibody

Interleukin-3 receptor (CD123) is a soluble cytokine that is important for the immune system. CD123 is the receptor of interleukin 3 α Chain is a cytokine receptor. Meanwhile, CD123 is overexpressed in a variety of hematological malignancies. Compared with non-tumor hematopoietic stem cells, CD123 expression was high in leukemia...

Olutasidenib, a Brain-Penetrant Mutant IDH1 Selective Inhibitor For AML Research

On December 1, 2022, FDA approved Rezlidhea (Olutasidenib) to treat adults with relapsed or refractory acute myeloid leukemia (AML) with a susceptible (IDH1) mutation. Olutasidenib (FT2102) is a highly potent, orally active, brain-penetrant, and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1). As a result, The IC50 values are...

DD1 is a Proteasome Inhibitor Used for Acute Myeloid Leukemia (AML) Research

Acute myeloid leukemia (AML) is clinically and genetically heterogeneous hematopoietic cancer. Leukemia cells are unable to undergo growth arrest and terminal differentiation. The conventional chemotherapeutic approach for AML contains a combination of anthracycline with cytarabine. However, due to either refractory to front-line therapy or subsequent relapse, AML remains a...

ML390 is a Potent DHODH Inhibitor

Dihydrowhey dehydrogenase (DHODH) catalyzes the fourth enzymatic step of pyrimidine biosynthesis, namely, ubiquinone mediated oxidation of dihydrowhey acid to whey acid. Specifically, DHODH is a mitochondrial protein located on the outer surface of the mitochondrial inner membrane (IMM). Inhibitors of the enzyme are used to treat autoimmune diseases such...

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...