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Towards Tuneable Retaining Glycosidase-Inhibiting Peptides by Mimicry of a Plant Flavonol Warhead
ChemBioChem ( IF 3.2 ) Pub Date : 2017-11-07 05:55:35 , DOI: 10.1002/cbic.201700457
Ryoji Yoshisada 1 , Lieke van Gijzel 1 , Seino A. K. Jongkees 1
Affiliation  

Stay tuned: Incorporating l-DOPA into a lariat peptide scaffold affords an inhibitor with a potency for the retaining glycosidase human pancreatic α-amylase that is increased tenfold. This represents an important first step towards mimicking a two-part natural-product-derived inhibitory motif in a peptide scaffold, thereby allowing its affinity to be tuned for diverse enzymes from this important class.

中文翻译:

拟态保留黄酮糖苷酶抑制肽的模仿植物黄酮醇战斗部。

敬请期待:将1- DOPA掺入套索肽支架中可提供一种抑制剂,该抑制剂可将糖苷酶人类胰腺α-淀粉酶的保留能力提高十倍。这代表了迈向肽支架中由两部分天然产物衍生的抑制性基序的重要的第一步,从而使其亲和力可针对这一重要类别的多种酶进行调节。
更新日期:2017-11-07
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