Tag: cancer

JNJ-9350 is an inhibitor of Spermine Oxidase (SMOX)

Spermine oxidase (SMOX) is a highly inducible enzyme. Specifically, its imbalance can change polyamine homeostasis. SMOX, spermine spermidine acetyltransferase (SSAT), and acetyl polyamine oxidase (APAO) are the main enzymes regulating the reverse transformation of polyamines. Besides, SMOX and SSAT are highly inducible, but APAO is constitutively expressed. SMOX is...

GNE-9815 is a highly selective pan-RAF inhibitor, can be used to research KRAS mutant cancers

Rapidly accelerated fibrous sarcoma (RAF) kinases are a family of three serine/threonine-specific protein kinases associated with retroviral oncogenes. They play key roles in several cellular processes, including cell cycle progression, cell proliferation, cell metabolism, cell migration, cell differentiation, and apoptosis. Activation of RAF kinases requires interaction with RAS-GTPases. RAF...

EM127 is a SMYD3 Covalent Inhibitor

SMYD3 is a methyltransferase (MTase) catalyzing the methylation of specific lysine residues. Notably, it induces cell proliferation and regulates gene expression, including histones H3 (Histone H3 Lysine 4, H3K4) and H4 (Histone H4 Lysine 5, VEGFR1 receptor, AKT1, HER2, and MAP3K2 protein. Importantly, SMYD3 plays a role in transcriptional...

CP681301 is a Potent CDK5 Inhibitor

CDKs (Cyclin-dependent kinases) are serine-threonine kinases first discovered for their role in regulating the cell cycle. They are also involved in regulating transcription, mRNA processing, and the differentiation of nerve cells. CDK5 is one of the Cyclin-dependent kinases. Importantly, CDK5 is an unconventional Cdk that regulates developmental and adult...

BLU2864 is An Orally Active PRKACA Kinase Inhibitor

Fibrolamellar carcinoma (FLC) is a rare, difficult-to-treat liver cancer primarily affecting pediatric and adolescent patients. An analysis of FLC tumor samples shows that protein kinase A (PKA) alpha catalytic subunit (PRKACA) is a critical molecular event in FLC pathogenesis. In this article, we will introduce an orally active, highly selective, ATP-competitive PRKACA...

FL118, a Camptothecin Analogue, is a Survivin Inhibitor with Anti-Cancer Activity

Survivin is the smallest member of the inhibitor of apoptosis (IAP) protein family. Specifically, survivin is a 142 amino acid, 16.5 kDa protein. Survivin participates in the inhibition of apoptosis and the regulation of the cell cycle. Besides, survivin can inhibit caspase and block cell death. Moreover, survivin was...