Category: Neuroblastoma

MYCMI-6 is a Selective Endogenous MYC:MAX Inhibitor

The MYC family of oncogenes (MYC, MYCN, and MYCL), encodes basic helix-loop-helix leucine zipper (bHLHZip) transcription factors. Through the HLHZip domain, MYC heterodimerizes with the bHLHZip protein MAX, which enables the MYC:MAX complex to bind E-box regulatory DNA elements throughout the genome. Therefore, it controls the transcription of a...

AKOS-22, a VDAC1 Oligomerization and Apoptosis Inhibitor, Protects Against Mitochondrial Dysfunction

Apoptosis plays a critical role in several pathological processes, such as neurodegenerative diseases and various cardiovascular diseases. Besides, it is therefore not surprising that mitochondrial dysfunction is associated with various human diseases. Located at the outer mitochondrial membrane (OMM), 2 the voltage-dependent anion channel (VDAC) serves as a mitochondrial gatekeeper. Moreover, the...

GPP78 is a Nampt Inhibitor and an Autophagy Inducer

Nicotinamide phosphoribosyltransferase (NAMPT) is an enzyme that catalyzes the synthesis of nicotinamide mononucleotide (NMN) from nicotinamide (NM) and PRPP. Therefore, NAMPT plays an important role in the cyclic biosynthetic pathway of nicotinamide adenine dinucleotide (NAD). Especially, NAMPT acts as an extracellular proinflammatory cytokine, able to induce cellular expression of...

JTE-013 is a Specific S1P2 Antagonist in Neuroblastoma

Sphingosine-1-phosphate ( S1P ), the bioactive sphingolipid metabolite, is a critical regulator of many physiological and pathophysiological processes, including cancer, atherosclerosis, diabetes and osteoporosis. S1P and its receptors (S1P1-5) play critical roles in many pathologic processes, including cancer. S1P/sphingosine-1-phosphate receptor (S1PR) axis plays critical role in a wide variety...

LDN-192960 is a Dual Haspin and DYRK2 Inhibitor

Haspin is a serine/threonine kinase that phosphorylates Thr-3 of histone H3 in mitosis. This phosphorylation generates a binding site on H3 for Survivin. Thus, the positions the Chromosome Passenger Complex at centromeres regulate chromosome segregation, and it also displaces proteins such as TFIID. It normally bind to H3 through methylated...

TH34, an HDAC6/8/10 Inhibitor, Induces Caspase-Dependent Programmed Cell Death

HDAC (Histone deacetylases) are a group of proteins that act on histones. They remove acetyl groups from N-acetyl lysine amino acid on a histone. As a result, histones wrap DNA more tightly. The enzymes have opposite function to histone acetyltransferase. But, they both regulate DNA expression. HDAC is a...