X‑Ray Conformation and Structure–Activity Relationships of MA026, a Reversible Tight Junction Opener

MA026, a cyclic lipodepsipeptide, opens the tight junction (TJ) probably via binding to claudin-1. We reported that (1) TJ-opening activity is dependent on the amino acid sequence order at Glu10-Leu11; (2) an epimer at the C3 position of the N-terminal acyl tail decreased the TJ-opening activity; an...

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Veröffentlicht in:	Journal of medicinal chemistry 2023-07, Vol.66 (13), p.8717-8724
Hauptverfasser:	Mukaiyama, Minagi, Uchiyama, Chihiro, Fukuda, Akane, Nakazawa, Yoshiki, Kuramochi, Yuka, Shibata, Yudai, Konno, Sho, Muguruma, Kyohei, Matsugaki, Naohiro, Asari, Tomo, Ogawa, Kazuyoshi, Taguchi, Akihiro, Takayama, Kentaro, Taniguchi, Atsuhiko, Nagumo, Yoko, Senda, Toshiya, Hayashi, Yoshio, Usui, Takeo
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acid Sequence Claudin-1 - metabolism Structure-Activity Relationship Tight Junctions - metabolism X-Rays
Online-Zugang:	Volltext
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