Teno, Naoki published the artcileSynthesis and evaluation of tripeptidic plasmin inhibitors with nitrile as warhead, Category: iodides-buliding-blocks, the publication is Journal of Peptide Science (2012), 18(10), 620-625, database is CAplus and MEDLINE.
Plasmin is best known as the key mol. in the fibrinolytic system, which is critical for clot lysis and can initiate matrix metalloproteinase (MMP) activation cascade. Along with MMP, plasmin is suggested to be involved in physiol. processes that are linked to the risk of carcinoma formation. Plasmin inhibitors could be perceived as a promising new principle in the treatment of diseases triggered by plasmin. On the basis of the peptidic sequence derived from the synthetic plasmin substrate, a series of peptidic plasmin inhibitors possessing nitrile as warhead were prepared and evaluated for their inhibitory activities against plasmin and other serine proteases, plasma kallikrein and urokinase. The most potent peptidic inhibitors with the nitrile warhead exhibit potency toward plasmin (IC50 = 7.7-11 μM) and are characterized by their selectivity profile against plasma kallikrein and urokinase. The results and mol. modeling of the peptidic inhibitor complexed with plasmin reveal that the P2 residue makes favorable contacts with the open binding pocket comprising the S2 and S3 subsites of plasmin.
Journal of Peptide Science published new progress about 161370-66-7. 161370-66-7 belongs to iodides-buliding-blocks, auxiliary class Chiral,Iodide,Amine,Aliphatic hydrocarbon chain,Ester,Amide, name is (S)-tert-Butyl 2-((tert-butoxycarbonyl)amino)-4-iodobutanoate, and the molecular formula is C12H14O2, Category: iodides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Iodide,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com