Tag: Apoptosis

E64FC26 is a pan-Inhibitor of the Protein Disulfide Isomerase (PDI) Family

Multiple myeloma (MM) is an incurable hematological malignancy. MM results in the accumulation of clonal plasma cells within the bone marrow. The natural biology of the plasma cell makes MM uniquely sensitive to disruptions in protein homeostasis. Subsequently, it proposes targeting protein folding as a strategy for the treatment...

CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor

Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...

Ro 90-7501, a Radiosensitizer, is an Aβ42 Fibril Assembly and PP5 Inhibitor

Cervical cancer is one of the most common cancers among women worldwide. Ro 90-7501 is an inhibitor of the amyloid β42 (Aβ42) fibril assembly. It is associated with Alzheimer’s disease. The usual method for Cervical cancer treatment is Radiotherapy, especially for locally advanced cancer. However, the treatment results are...

ML141 is a Selective, Reversible and Non-competitive Cdc42 GTPase Inhibitor

Cdc42 protein is an essential GTPase that belongs to the Rho/Rac subfamily of Ras-like GTPases. These proteins act as molecular switches to activate downstream components of a biological pathway. CDC42 plays an important role in cytoskeleton organization, cell cycle progression, signal transduction, and vesicle trafficking. Particularly, Overactive Cdc42 implicates...

ZLDI-8, an ADAM-17 and Notch Inhibitor, Enhances Chemotherapeutic Effects

ADAM metallopeptidase domain 17 (ADAM17) is an enzyme that belongs to the ADAM protein family of metalloproteases. ADAM17 plays a prominent role in the Notch signaling pathway. In this study, researchers demonstrated the discovery of ZLDI-8. ZLDI-8 is a novel inhibitor for Notch activating/cleaving enzyme ADAM-17. In particular, ZLDI-8...

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...

MSN-125 is a Potent Bax and Bak Oligomerization Inhibitor

Aberrant apoptosis can lead to acute or chronic degenerative diseases. Apoptosis largely divides into two pathways ultimately leading to caspase activation and subsequent cellular disintegration. Extracellular signals activating death receptors triggers the extrinsic pathway, and intracellular stress activates the intrinsic pathway. It largely regulated at the mitochondrial outer membrane...