Month: January 2022

IACS-15414 is an Orally Active SHP2 Inhibitor

Src-homology-2-containing protein tyrosine phosphatase 2 (SHP2), encoded by the PTPN11 gene, is a classical nonreceptor protein tyrosine phosphatase (PTP). SHP2 is a ubiquitous protein tyrosine phosphatase with a relatively conserved structure and function. It has emerged as a key downstream regulator of several receptor tyrosine kinases (RTKs) and cytokine...

ML-099 is a pan Ras-Related GTPases Activator

To date, we identified 167 small GTPases in humans which are key signal transducing enzymes. Small GTPases comprise five main families whose eponymous members are Ras, Rho, Rab, ADP-ribosylation factor (Arf) and Ran. Small GTPases link extracellular cues to the neuronal responses required for the construction of neuronal networks,...

VU0359595 is a Selective PLD1 Inhibitor

Phospholipase is a member of a very complex group of enzymes that break down phospholipids into fatty acids and other compounds. Phospholipase D (PLD) is an enzyme of the phospholipase superfamily. There are two mammalian isoforms of PLD, coined PLD1 and PLD2, and despite conserved regulatory and catalytic domains....

SD-1029 is a JAK2/STAT3 Activation Inhibitor

Janus kinase (JAK) is a family of intracellular, nonreceptor tyrosine kinases that transduce cytokine-mediated signals via the JAK-STAT pathway. JAK includes JAK1, JAK2, JAK3 and TYK2. JAK serves as the cytoplasmic signaling components of cytokine receptors and are activated through cytokine-mediated trans-phosphorylation. The pseudokinase domain of JAKs is crucial...

Tirabrutinib is a Selective BTK Inhibitor

The BTK kinases comprise 5 structural domains, including pleckstrin homology, TEC homology, Src homology, Src homology, and kinase domains. The activation of BTK kinase depends on recruitment to the plasma membrane via the pleckstrin homology domain. In humans, BTK mutations result in arrested B-cell development. Besides, it leads to...

β-Lapachone, a Naturally Occurring O-naphthoquinone, is a Topoisomerase I Inhibitor

β-Lapachone is an ortho-naphthoquinone and inhibits topoisomerase I. β-Lapachone is a classic quinone-containing antitumor NQO1-bioactivatable drug that directly kills NQO1-overexpressing cancer cells. NQO1 is an antioxidative enzyme that helps recover renal oxidative status. β-Lapachone reduces cisplatin-induced nephrotoxicity. In cancer cells, cisplatin forms cross-link with  DNA, which inhibits DNA  replication,...