In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. The reactant in an enzyme-catalyzed reaction is called a substrate. name: 6-Chlorobenzo[b]thiophene-2-carboxylic acid, C9H5ClO2S. A document type is Article, introducing its new discovery., name: 6-Chlorobenzo[b]thiophene-2-carboxylic acid
Deoxyhypusine synthase (DHPS) utilizes spermidine and NAD as cofactors to incorporate a hypusine modification into the eukaryotic translation initiation factor 5A (eIF5A). Hypusine is essential for eIF5A activation, which, in turn, plays a key role in regulating protein translation of selected mRNA that are associated with the synthesis of oncoproteins, thereby enhancing tumor cell proliferation. Therefore, inhibition of DHPS is a promising therapeutic option for the treatment of cancer. To discover novel lead compounds that target DHPS, we conducted synthetic studies with a hit obtained via high-throughput screening. Optimization of the ring structures of the amide compound (2) led to bromobenzothiophene (11g) with potent inhibitory activity against DHPS. X-ray crystallographic analysis of 11g complexed with DHPS revealed a dramatic conformational change in DHPS, which suggests the presence of a novel allosteric site. These findings provide the basis for the development of novel therapy distinct from spermidine mimetic inhibitors.
I am very proud of our efforts over the past few months and hope to 26018-73-5 help many people in the next few years. name: 6-Chlorobenzo[b]thiophene-2-carboxylic acid
Reference：
Benzothiophene – Wikipedia,
Benzothiophene | C8H6S – PubChem