Month: October 2021

CX-5461 is an Orally Active rRNA Synthesis Inhibitor

RNA polymerase is an enzyme that synthesizes RNA from a DNA template. Specifically, RNA synthesis or transcription is the process of transcribing DNA nucleotide sequence information into RNA sequence information. Besides, RNA synthesis is catalyzed by a large enzyme called RNA polymerase. The basic biochemistry of RNA synthesis is...

SB 258719 is a Selective 5-HT7 Receptor Antagonist

The neurotransmitter 5-hydroxytryptamine (5-HT) has an array of pharmacological and physiological roles within the central nervous system. It has the potential to develop a number of useful medicines. The selective 5-hydroxytryptamine (5-HT, serotonin) reuptake inhibitors (SSRIs) show potency in major depression. 5-HT receptors divide into seven major classes (5-HT1-7)....

Brusatol (NSC 172924) is a Nrf2 Inhibitor

Keap1-Nrf2 is the major regulator of cytoprotective responses to electrophilic chemicals or reactive oxygen species (ROS).  Upregulation of Nrf2 inducing by inactivation of Keap1 is often observed in cancer cells. Aberrant activation of Nrf2 in cancer cells accelerates proliferation and metabolism. Meanwhile, Nrf2 is a transcription factor that regulates cellular...

Quizartinib (AC220) is an Orally Active and Highly Selective FLT3 Tyrosine Kinase Inhibitor

Receptor tyrosine kinase FMS like tyrosine kinase 3 (FLT3) is a member of the class III receptor tyrosine kinase family. The family also includes FMS, kit, and platelet-derived growth factor (PDGF) receptors. Specifically, FLT3 is relevant to regulating the survival, proliferation, and differentiation of hematopoietic stem/progenitor cells. The normal...

Saracatinib (AZD0530) is a potent Src Family Inhibitor

Src is a prototypical non-receptor tyrosine kinase. It also includes c-Yes and Fyn. Src transduces signals that control processes involved in cell proliferation, adhesion, and motility. Clinical evidence supports a link between deregulation of Src activity and tumor progression and metastasis. Src over-expression and activation are associated with numerous...

Cytochalasin B is a Mycotoxin binding to the Barbed end of Actin Filaments

Actin, a family of globular multi-functional proteins, is the most abundant protein in most eukaryotic cells. It forms microfilaments in the cytoskeleton, and the thin filaments in muscle fibrils. Actin participates in many important cellular processes, including muscle contraction, cell motility, cell division and cytokinesis, vesicle and organelle movement,...

Atuveciclib is a Highly Selective and Orally Active PTEFb, CDK9 Inhibitor

Positive transcription elongation factor P-TEFb is a kinase composed of CDK9 and cyclin T. Specifically, P-TEFb plays an important role in the transcriptional regulation of RNA polymerase II (pol II) in eukaryotes. Besides, P-TEFb mediates the positive transcriptional extension of the new mRNA chain by phosphorylating the S2 residue...