201740-78-5Relevant academic research and scientific papers
Design of a Hyperpolarized Molecular Probe for Detection of Aminopeptidase N Activity
Hata, Ryunosuke,Nonaka, Hiroshi,Takakusagi, Yoichi,Ichikawa, Kazuhiro,Sando, Shinsuke
, p. 1765 - 1768 (2016)
Aminopeptidase N (APN) is an important enzyme that is involved in tumor angiogenesis. Detection of APN activity can thus lead to early diagnosis and elucidation of tumor development. Although some molecular probes for APN have been developed, the detection of APN activity in opaque biological samples remains a challenge. To this end, we designed a hyperpolarized NMR probe [1-13C]Ala-NH2 which satisfies the prerequisites for APN detection, namely, sufficient retention of the hyperpolarized state, a high reactivity to APN, and an APN-induced chemical shift change. The [1-13C]Ala-NH2 probe allowed sensitive detection of APN activity using 13C NMR spectroscopy.
Effect of residual water and microwave heating on the half-life of the reagents and reactive intermediates in peptide synthesis
Pernille Tofteng,Pedersen, S?ren L.,Staerk, Dan,Jensen, Knud J.
, p. 9024 - 9031 (2012)
Precise microwave heating has changed the way many small molecules are being synthesized and, currently, the field of solid-phase peptide synthesis is undergoing dramatic changes owing to the use of microwave heating. To fully reap the benefits of precise microwave heating for the formation of amide bonds in peptide synthesis, it is important to understand the kinetics of formation and break-down of activated esters and their N-acylation of the nascent peptide chain at elevated temperatures. Herein, we present systematic studies of, first, the rate of formation of activated esters by NMR spectroscopy and, second, their N-acylation during peptide synthesis. A study of the amount of residual water in the solvents revealed a significant effect on electrophilic reagents and intermediates. This observation was expanded into a general study of microwave heating in peptide synthesis.
Method of evaluating pharmacological effects of medicine
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Page/Page column 21-22, (2008/12/07)
A diagnostic reagent for use in the evaluation of a pharmacological effect of a medicine containing a pharmaceutical agent including an enzyme, an enzyme inhibitor or a receptor ligand or a prodrug of the pharmaceutical agent is provided. Further, a method of screening pharmaceutical agents each comprising an enzyme, an enzyme inhibitor or a receptor ligand and/or prodrugs of the pharmaceutical agents is provided.
