A Glycosylated Prodrug to Attenuate Neuroinflammation and Improve Cognitive Deficits in Alzheimer's Disease Transgenic Mice

Kim, Mingeun; Park, Min Hee; Nam, Geewoo; Lee, Misun; Kang, Juhye; Song, Im-Sook; Choi, Min-Koo; Jin, Hee Kyung; Bae, Jae-Sung; Lim, Mi Hee

doi:10.1021/acs.molpharmaceut.0c00677

상세 보기

A Glycosylated Prodrug to Attenuate Neuroinflammation and Improve Cognitive Deficits in Alzheimer's Disease Transgenic Mice

Kim, Mingeun;
Park, Min Hee;
Nam, Geewoo;
Lee, Misun;
Kang, Juhye;
... Song, Im-Sook;
... Jin, Hee Kyung;
... Bae, Jae-Sung;
외 2명

Citations

WEB OF SCIENCE

10

Citations

SCOPUS

11

초록

We report a prodrug, Glu-DAPPD, to overcome the shortcomings of an anti-neuroinflammatory molecule, N,N'-diacetyl-p-phenylenediamine (DAPPD), in biological applicability for potential therapeutic applications. We suspect that Glu-DAPPD can release DAPPD through endogenous enzymatic bioconversion. Consequently, Glu-DAPPD exhibits in vivo efficacies in alleviating neuroinflammation, reducing amyloid-beta aggregate accumulation, and improving cognitive function in Alzheimer's disease transgenic mice. Our studies demonstrate that the prodrug approach is suitable and effective toward developing drug candidates against neurodegeneration.

키워드

Alzheimer's disease; prodrug; anti-neuroinflammation; microglial function; amyloid-beta; ARYLAMINE N-ACETYLTRANSFERASES; MESENCHYMAL STEM-CELLS; MICROGLIAL DYSFUNCTION; BETA-GLUCOSIDASES; SPECIFICITY; TARGET; METABOLISM; CLEARANCE; MECHANISM; PROTEIN

제목: A Glycosylated Prodrug to Attenuate Neuroinflammation and Improve Cognitive Deficits in Alzheimer's Disease Transgenic Mice

저자: Kim, Mingeun; Park, Min Hee; Nam, Geewoo; Lee, Misun; Kang, Juhye; Song, Im-Sook; Choi, Min-Koo; Jin, Hee Kyung; Bae, Jae-Sung; Lim, Mi Hee

DOI: 10.1021/acs.molpharmaceut.0c00677

발행일: 2021-01-04

유형: Article

저널명: Molecular Pharmaceutics

권: 18

호: 1

페이지: 101 ~ 112

언어: ENG

출판사: AMER CHEMICAL SOC

발행국가: 미국

분량: 12 페이지

ISSN: E 1543-8392
P 1543-8384