Manzamine A, an Orally Active β-Carboline Alkaloid with Antiviru, Antimalarial and Anticancer Activities
AManzamine A is an orally active β-carboline alkaloid effective against HSV-1, Cancer, and Malaria. For HSV-1， It is estimated that approximately 80% of the population worldwide are carriers of HSV-1 and approximately 40% suffer from recurrent infections. Unfortunately, this recurrent nature is a leading cause of corneal disease and...
Retro-2 is a Selective Inhibitor of Retrograde Protein Trafficking
Viruses critically depend on host cellular factors to establish a productive infection. Retro-2 is an inhibitor of endosome-to-Golgi retrograde transport of the plant toxin ricin and bacterial Shiga toxin. However, the efficacy of Retro-2 also has been examined against enveloped viruses, such as filoviruses. As a result, Retro-2 is...
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....
NVS-CECR2-1 is a CECR2 BRD (non-BET Family) Inhibitor
A Bromodomain (BRD) is a protein domain of about 110 amino acids and is a “reader” of lysine acetylation. Specifically, BRDs recognize acetylated lysine residues, such as those on the N-terminal tail of histones. Besides, BRD is responsible for the transduction of signals carried by acetylated lysine residues and...