FTI-2153 is a Highly Selective Farnesyltransferase Inhibitor
Farnesyltransferase (FTase) is a zinc enzyme that has been the subject of particular attention in anti-cancer research. Inhibitors of farnesyltransferase (FTase) have been designed for use as anti-Ras and anti-cancer drugs, but in fact they are selective for FTase, not for Ras. The non-thiol-containing FTI-2148 is highly selective for...
IPR-803 is a Potent Inhibitor of the uPAR•uPA Protein-Protein Interaction
The uPAR·uPA protein-protein interaction (PPI) is involved in signaling and proteolytic events. They promote tumor invasion and metastasis. Nearly every step of cancer metastasis, including cell migration, adhesion, angiogenesis, and invasion implicates uPAR. This has led to attempts to inhibit its protein interactions. IPR-803 emerges from a substructure search of commercial chemical...
OTS964 is an Orally Active TOPK and CDK11 Inhibitor
TOPK (T–lymphokine-activated killer cell–originated protein kinase, also known as PBK or PDZ-binding kinase) is a Ser/Thr protein kinase. Many types of human cancer, including breast and lung cancers, highly expresses it. Thus, TOPK might be a promising molecular target for drug development. Moreover, TOPK is in the “consensus stemness...
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...
BI 167107 is a Highly Potent Agonist of the β2 Adrenergic Receptor
G protein-coupled receptors (GPCRs) exhibit a spectrum of functional behaviors in response to natural and synthetic ligands. Researchers generated the human β2 adrenergic receptor (β2AR) that exhibits G protein-like behavior. The active G protein-coupled state of the β2AR exhibits characteristic functional properties. Agonists promote Gs binding to the β2AR...
Tasisulam, an Antitumor Agent, Inhibits Mitotic Progression and Induces Apoptosis
Tasisulam is an acyl sulfonamide with a unique antitumor dual mechanism of action. It involves antiangiogenesis and mitotic inhibition. Tasisulam has a broad range of activity in 60 tumor cell lines. It includes leukemia, melanoma, non-small-cell lung cancer, colon, ovarian, renal, and breast cancers. In this study, Tasisulam is...
sAJM-589 is a Myc Inhibitor by Disrupts the Myc-Max Heterodimer
The proto-oncogene Myc belongs to the basic helix-loop-helix leucine zipper (B-HLH-LZ) transcription factor family. It plays a key role in cellular proliferation, differentiation, and apoptosis. Myc expression is normally under tight control. Its expression is transient and responsive to mitogen stimulation. Indeed, in more than 70% of human malignancies,...