Ganetespib (STA-9090) is a HSP90 Inhibitor
Hsp90 is a molecular chaperone that regulates the posttranslational folding, stability, and function of its protein substrates (client proteins), many of which play critical roles in cell growth, differentiation, and survival. The Hsp90 machinery serves as a biochemical buffer for a number of oncogenic signaling proteins causally implicated in...
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...
OT-82 is an Orally Active NAMPT Inhibitor with Antineoplastic Activity
Treatment of hematopoietic (HP) malignancies such as leukemia, lymphoma, and myeloma need improvement due to the drug high toxicity. Some effective anticancer agents are tissue-selective but not cancer-specific targets. These agents cannot distinguish normal and transformed cells. Besides they are usually against lineage-specific metabolic deficiency or lineage-specific surface antigen,...
CM-272, a First-in-class, Reversible and Dual G9a/DNMTs Inhibitor
Therapy of hematological malignancies is undergoing a paradigm shift. It is away from the traditional chemotherapy towards the targeting of proteins driving the cancer phenotype. The novel therapeutic approach relies on the use of epigenetic drugs. It aims to reverse critical epigenetic events underlying human cancer pathogenesis, particularly abnormalities...
CC-223 is an Orally Bioavailable mTOR Kinase Inhibitor
mTOR is a serine/threonine kinase that regulates cell growth, metabolism, proliferation, and survival. mTORC1 is a master regulator of cell growth and metabolism. mTORC1 positively regulates cell growth and proliferation. mTORC2 regulates cytoskeletal organization. CC-223 is a potent mTOR kinase inhibitor with an IC50 of 0.016 μM. CC-223 is...
TAS4464, a Highly Potent and Selective Inhibitor of NEDD8 Activating Enzyme, Shows Antitumor Activity
TAS4464, a highly potent and selective inhibitor of NEDD8 activating enzyme, shows antitumor activity. NEDD8 activating enzyme (NAE) is an essential regulator of the NEDD8 conjugation pathway. The ubiquitin-like modifier NEDD8 controls the stability and activity of its target proteins via a conjugation cascade (the neddylation pathway). NAE controls...
Alisertib is an Oral Active and Selective Aurora A Kinase Inhibitor
As we all know, Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor. Aurora kinases are essential mediators in cell mitosis. Amplification of these kinases can lead to the development of malignancy and may be associated with inferior survival. Alisertib is an oral aurora kinase inhibitor which...