IMT1 is a First-in-Class Specific and Noncompetitive Human POLRMT Inhibitor
Mitochondria provide cellular energy through its oxidative phosphorylation system, which needs to coordinate the expression of genes encoded by nuclear and mitochondrial genomes (mtDNA). Specifically, the transcription of mtDNA in circular mammals depends on a single mitochondrial RNA polymerase (POLRMT). Besides, three proteins are required for mitochondrial transcription initiation:...
TAS-119 is a Selective and Orally Active Aurora A Inhibitor
Aurora kinases represent a serine/threonine kinase family crucial for cell-cycle control. In particular, Aurora kinases are important and indispensable in multiple steps of mitotic progression. Specifically, Aurora kinase A acts primarily during the prophase of mitosis. Overexpression of Aurora A in HeLa cells attenuates the antiproliferative activity of Paclitaxel....
Ro 90-7501, a Radiosensitizer, is an Aβ42 Fibril Assembly and PP5 Inhibitor
Cervical cancer is one of the most common cancers among women worldwide. Ro 90-7501 is an inhibitor of the amyloid β42 (Aβ42) fibril assembly. It is associated with Alzheimer’s disease. The usual method for Cervical cancer treatment is Radiotherapy, especially for locally advanced cancer. However, the treatment results are...
COTI-2 is an Orally Available Mutant p53 Activator
TP53 (p53) is the single most frequently altered gene in human cancers, with mutations being present in approximately 50% of all invasive tumors. Besides, p53 is mutated in at least 80% of samples in some of the most difficult-to-treat cancers. Therefore, the mutant p53 protein is an important candidate...
VERU-111 is an Orally Active Tubulin Inhibitor
Microtubules play a critical role in the proliferation of cancer cells. Meanwhile, microtubule dynamics is therefore one of the most productive therapeutic targets for cancer treatment. Microtubule-targeting agents can interfere with functions of microtubules, thereby disrupting the formation of the mitotic spindle, eventually leading to mitotic arrest at the...