8UTL

Bovine trypsin in complex with Thr3Dap mutated microviridin J

8UTL の概要

• エントリーDOI: 10.2210/pdb8utl/pdb
• 関連するPDBエントリー: 8UO7
• 分子名称: Cationic trypsin, Thr3Dap mutated microviridin J, GLYCEROL, ... (6 entities in total)
• 機能のキーワード: hydrolase inhibitor, hydrolase
• 由来する生物種: Bos taurus (cattle); 詳細
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 25424.50

構造登録者

Chen, W.,Bruner, S.D. (登録日: 2023-10-31, 公開日: 2024-02-14, 最終更新日: 2024-02-28)

主引用文献

Patel, K.P.,Chen, W.T.,Delbecq, L.,Bruner, S.D.
Alternative Linkage Chemistries in the Chemoenzymatic Synthesis of Microviridin-Based Cyclic Peptides.
Org.Lett., 26:1138-1142, 2024

PubMed Abstract: Engineering biosynthetic pathways to ribosomally synthesized and post-translationally modified peptides (RiPPs) offers several advantages for both and applications. Here we probe the ability of peptide cyclases to generate trimacrocycle microviridin analogs with non-native cross-links. The results demonstrate that diverse chemistries are tolerated by macrocyclases in the ATP-grasp family and allow for the construction of unique cyclic peptide architectures that retain protease inhibition activity. In addition, cocomplex structures of analogs bound to a model protease were determined, illustrating how changes in functional groups maintain peptide conformation and target binding.

PubMed: 38306609
DOI: 10.1021/acs.orglett.3c04045

実験手法

X-RAY DIFFRACTION (1.56 Å)