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...
CC-90010 is a Reversible and Orally Active BET Inhibitor
Come straight to the point, CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors. The bromodomain and extra-terminal domain (BET) proteins, epigenetic readers, recognize and bind acetylated lysine residues. The BET protein family comprises the ubiquitously expressed...
ASP4132 is an Orally Active AMPK Activator
Adenosine monophosphate (AMP)-activated protein kinase (AMPK) is an enzyme that plays a role in cellular energy homeostasis. Specifically, it is important in largely to activate glucose and fatty acid uptake and oxidation when cellular energy is low. Besides, AMP or adenosine diphosphate (ADP) levels increase during metabolic stress such...