Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. In an article, author is Craciun, Anda-Mihaela, once mentioned the application of 5704-04-1, Name is 2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)acetic acid, molecular formula is C6H13NO5, molecular weight is 179.1711, MDL number is MFCD00004277, category is amides-buliding-blocks. Now introduce a scientific discovery about this category, Application In Synthesis of 2-((1,3-dihydroxy-2-(hydroxymethyl)propan-2-yl)amino)acetic acid.
Design, Synthesis, Molecular Dynamics Simulation, and Functional Evaluation of a Novel Series of 26RFa Peptide Analogues Containing a Mono- or Polyalkyl Guanidino Arginine Derivative
26RFa, the endogenous QRFPR ligand, is implicated in several physiological and pathological conditions such as the regulation of glucose homeostasis and bone mineralization; hence, QRFPR ligands display therapeutic potential. At the molecular level, functional interaction occurs between residues Arg(25) of 26RFa and Gln(125) of QRFPR. We have designed 26RFa((20-26)) analogues incorporating arginine derivatives modified by alkylated substituents. We found that the Arg(25) side chain length was necessary to retain the activity of 26RFa((20-26)) and that N-monoalkylation of arginine was accommodated by the QRFPR active site. In particular, [(Me)(omega)Arg25]26RFa((20-26)) (5b, LV-2186) appeared to be 25-fold more potent than 26RFa((20-26)) and displayed a position in a QRFPR homology model slightly different to that of the unmodified heptapeptide. Other peptides were less potent than 26RFa((20-26)), exhibited partial agonistic activity, or were totally inactive in accordance to different ligand-bound structures. In vivo, [(Me)(omega)Arg(25))]26RFa((20-26)) exerted a delayed 26RFa-like hypoglycemic effect. Finally, N-methyl substituted arginine-containing peptides represent lead compounds for further development of QRFPR agonists.
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