《Semi-quantitative models for identifying potent and selective transthyretin amyloidogenesis inhibitors》 was written by Connelly, Stephen; Mortenson, David E.; Choi, Sungwook; Wilson, Ian A.; Powers, Evan T.; Kelly, Jeffery W.; Johnson, Steven M.. Recommanded Product: 626-40-4This research focused ontransthyretin amyloidogenesis inhibitor algorithm modeling amyloid polyneuropathy; Amyloid; Familial amyloid polyneuropathy; In silico docking; Inhibitor; Prediction algorithms; Senile systemic amyloidosis; Structural biology; Structure-based drug design; TTR; Thyroid hormone receptors; Transthyretin. The article conveys some information:
Rate-limiting dissociation of the tetrameric protein transthyretin (TTR), followed by monomer misfolding and misassembly, appears to cause degenerative diseases in humans known as the transthyretin amyloidoses, based on human genetic, biochem. and pharmacol. evidence. Small mols. that bind to the generally unoccupied thyroxine binding pockets in the native TTR tetramer kinetically stabilize the tetramer, slowing subunit dissociation proportional to the extent that the mols. stabilize the native state over the dissociative transition state-thereby inhibiting amyloidogenesis. Herein, the authors use previously reported structure-activity relationship data to develop two semi-quant. algorithms for identifying the structures of potent and selective transthyretin kinetic stabilizers/amyloidogenesis inhibitors. The viability of these prediction algorithms, in particular the more robust in silico docking model, is perhaps best validated by the clin. success of tafamidis, the first-in-class drug approved in Europe, Japan, South America, and elsewhere for treating transthyretin aggregation-associated familial amyloid polyneuropathy. Tafamidis is also being evaluated in a fully-enrolled placebo-controlled clin. trial for its efficacy against TTR cardiomyopathy. These prediction algorithms will be useful for identifying second generation TTR kinetic stabilizers, should these be needed to ameliorate the central nervous system or ophthalmol. pathol. caused by TTR aggregation in organs not accessed by oral tafamidis administration. In the part of experimental materials, we found many familiar compounds, such as 3,5-Dibromoaniline(cas: 626-40-4Recommanded Product: 626-40-4)
3,5-Dibromoaniline(cas: 626-40-4) belongs to anime.Typically the presence of an amine functional group is deduced by a combination of techniques, including mass spectrometry as well as NMR and IR spectroscopies. 1H NMR signals for amines disappear upon treatment of the sample with D2O. In their infrared spectrum primary amines exhibit two N-H bands, whereas secondary amines exhibit only one.Recommanded Product: 626-40-4
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary