Apitolisib is an Orally Active Class I PI3K and mTORC1/2 Inhibitor
Activation of the pathway occurs following activating point mutations or amplification of the PIK3CA gene encoding the p110a PI3K isoform. Oncogenes such as PI3K, AKT, epidermal growth factor receptor (EGFR), and human epithelial growth factor receptor 2 (HER2) stimulate proliferation, growth, and survival by activating mTOR kinase. The mTOR...
Infigratinib (BGJ-398) is an Orally Active FGFR Inhibitor
The fibroblast growth factor receptor (FGFR) family of receptor tyrosine kinases (RTKs) comprises four members (FGFR1, FGFR2, FGFR3, and FGFR4) that share significant sequence homology. This family of RTKs serves as high-affinity receptors for the fibroblast growth factors (FGFs) that control cell proliferation, apoptosis, and differentiation and are involved...
Inupadenant is an Orally Active and Highly Selective A2A Receptor Antagonist
Adenosine receptors (AR), including P1 purinergic receptors, belong to G protein-coupled receptors (GPCR). Specifically, Adenosine is an autogenous acid in all tissues and body fluids. Besides, AR contains four subtypes, A1, A2A, A2B, and A3. They are activated by extracellular adenosine and play a central role in a wide...
SG3199, an ADC Cytotoxin, is a Cytotoxic DNA Minor Groove Interstrand Crosslinking PDB Dimer
The pyrrolobenzodiazepines (PBD) are a class of compound that may have antibiotic or anti-tumor properties. They exert their biological activity by binding in the minor groove of DNA. PBD dimers are a class of exquisitely potent DNA minor groove interstrand crosslinking agents. An important feature of the interstrand cross-links...
Venadaparib (IDX-1197) is a Potent and Selective PARP Inhibitor
PARP is an enzyme that involved in a number of cellular processes such as DNA repair, and programmed cell death. The PARP family comprises 17 members. They have all very different structures and functions in the cell. Importantly, the main role is to detect and signal single-strand DNA breaks...
Rosabulin is a Potent Microtubule Inhibitor
Chemotherapy is a cornerstone in the development of present-day cancer therapy. Moreover, Chemotherapy is one of the most effective and potent strategies to treat malignant tumors. However, Chemotherapy resistance occurs when cancers that have been responding to therapy suddenly begin to grow. Rosabulin is a potent tubulin inhibitor. In...
Barasertib, a Pro-Drug of Barasertib-hQPA, is a Highly Selective Aurora B Inhibitor
Aurora kinases play an important role during mitosis for chromosome alignment, segregation, and cytokinesis. Selective Targeting of Aurora B kinase may be a promising therapeutic approach for the treatment of a range of malignancies. In this study, researchers explored the effect of Barasertib. In particular, Barasertib is a highly...