Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo1,2-apyridine-5-carboxylic acid series of heparanase-1 inhibitor

Heparanase-1 (HPSE1) is an endo-β-d-glucuronidase that is the only mammalian enzyme known to cleave heparan sulfate (HS) of heparan sulfate proteoglycans (HSPG), a key component of the glycocalyx layer of the vascular endothelium matrix. Inhibition of HPSE1 has therapeutic potential for cancer and p...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2023-10, Vol.93, p.117460
Hauptverfasser:	Imai, Yudai, Suzuki, Ryo, Wakasugi, Daisuke, Matsuda, Daisuke, Tanaka-Yamamoto, Nozomi, Ohki, Yuta, Mima, Masashi, Endo, Mayumi, Tabata, Ryotaro, Matsuzawa, Hitomi, Hasegawa, Yoshitaka, Kato, Sota, Sugisaki, Mami, Miyagawa, Hiroh, Fujimoto, Natsuko, Fukunaga, Takuya, Kato, Sayaka, Takahashi, Teisuke, Kakinuma, Hiroyuki
Format:	Artikel
Sprache:	eng
Online-Zugang:	Volltext
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