Encyclopedia

  • Iodination of salicylic acid improves its binding to transthyretin☆
  • Add time:08/31/2019         Source:sciencedirect.com

    Transthyretin (TTR) is a plasma homotetrameric protein associated with senile systemic amyloidosis and familial amyloidotic polyneuropathy. In theses cases, TTR dissociation and misfolding induces the formation of amyloidogenic intermediates that assemble into toxic oligomeric species and lead to the formation of fibrils present in amyloid deposits. The four TTR monomers associate around a central hydrophobic channel where two thyroxine molecules can bind simultaneously. In each thyroxine binding site there are three pairs of symmetry related halogen binding pockets which can accommodate the four iodine substituents of thyroxine. A number of structurally diverse small molecules that bind to the TTR channel increasing the protein stability and thereafter inhibiting amyloid fibrillogenesis have been tested. In order to take advantage of the high propensity to interactions between iodine substituents and the TTR channel we have identified two iodinated derivatives of salicylic acid, 5-iodosalicylic acid and 3,5-diiodosalicylic acid, available commercially. We report in this paper the relative binding affinities of salicylic acid and the two iodinated derivatives and the crystal structure of TTR complexed with 3,5-diiodosalicylic acid, to elucidate the higher binding affinity of this compound towards TTR.

    We also recommend Trading Suppliers and Manufacturers of 5-Iodosalicylic acid (cas 119-30-2). Pls Click Website Link as below: cas 119-30-2 suppliers


    Prev:The determination of the sodium salt of 5-Iodosalicylic acid (cas 119-30-2) and its metabolites in urine
    Next: Bupivacaine salts of diflunisal and other aromatic hydroxycarboxylic acids: Aqueous solubility and release characteristics from solutions and suspensions using a rotating dialysis cell model)

About|Contact|Cas|Product Name|Molecular|Country|Encyclopedia

Message|New Cas|MSDS|Service|Advertisement|CAS DataBase|Article Data|Manufacturers | Chemical Catalog

©2008 LookChem.com,License: ICP

NO.:Zhejiang16009103

complaints:service@lookchem.com Desktop View