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Immunosuppressive properties of amino acid and peptide derivatives of mycophenolic acid.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-01-24 , DOI: 10.1016/j.ejmech.2020.112091
Agnieszka Siebert 1 , Grzegorz Cholewiński 1 , Piotr Trzonkowski 2 , Janusz Rachon 1
Affiliation  

Mycophenolic acid (MPA) was coupled with amino acids and biologically active peptides including derivatives of tuftsin to modify its immunosuppressive properties. Both amino acid unit in the case of simple MPA amides and modifications within peptide moiety of MPA - tuftsin conjugates influenced the observed activity. Antiproliferative potential of the obtained conjugates was investigated in vitro and MPA amides with threonine methyl ester and conjugate of MPA with retro-tuftisin occurred to be more selective against PBMC in comparison to parent MPA. Both amino acid and peptide derivatives of MPA acted as inosine-5'-monophosphate dehydrogenaze (IMPDH) inhibitors.

中文翻译:

霉酚酸氨基酸和肽衍生物的免疫抑制特性。

麦考酚酸(MPA)与氨基酸和生物活性肽(包括簇蛋白衍生物)偶联,以改变其免疫抑制特性。在简单的MPA酰胺的情况下,氨基酸单位和MPA-塔夫辛缀合物的肽部分内的修饰都会影响所观察到的活性。体外研究了获得的缀合物的抗增殖潜力,与母体MPA相比,MPA酰胺与苏氨酸甲酯以及MPA与反肌动蛋白的缀合物对PBMC的选择性更高。MPA的氨基酸和肽衍生物均充当肌苷5'-单磷酸脱氢(IMPDH)抑制剂。
更新日期:2020-01-24
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