The Rh(III) complex 1 was identified as a direct, selective and potent inhibitor of KDM5A that directly abrogate KDM5A demethylase activity via antagonizing the KDM5A‐tri‐\\/di﹎ethylated histone 3 protein﹑rotein interaction (PPI) in vitro and in cellulo. Complex 1 induced accumulation of...
Targeting lysine-specific demethylase 1 (KDM1A/LSD1) impairs colorectal cancer tumorigenesis by affecting cancer cells stemness, motility, and differentiation Annamaria Antona, Giovanni Leo, Francesco Favero, Marco Varalda, Jacopo Venetucci, Stefania Faletti, Matilde Todaro, Eleonora Mazzucco,...
Lysine-specific demethylase 1 (LSD1 or KDM1A) overexpression correlates with poor survival and castration resistance in prostate cancer. LSD1 is a coregulator of ligand-independent androgen receptor signaling promoting c-MYC expression. We examined the antitumor efficacy of LSD1 inhibition with HCI-25...
Tripel-negativer BrustkrebsWirkstoffentwicklungLysine-specific demethylase 5A (KDM5A) has recentldoi:10.1002/ange.201807305Leung Chung-HangYang Guan-JunWang WanheMok Simon Wing FaiWu ChunLaw Betty Yuen KwanMiao Xiang-MinWu Ke-JiaZhong Hai-JingWong Chun-YuenAngewandte Chemie...
Lysine-Specific Demethylase 1A Is a Targetable Kidney Disease Causal Genedoi:10.1681/ASN.2024rx16pv5aKolligundla Lakshmi PrasannaUniversity of Pennsylvania, Philadelphia, Pennsylvania, United States;Dhanunjay MukhiUniversity of Pennsylvania, Philadelphia, Pennsylvania, United States;Hongbo Liu...
The subject compounds and compositions serve to inhibit lysine-specific demethylase-1. In addition, the subject compounds and compositions are useful in the treatment of cancer.Selection drawing Noneチェン,ヤング,ケイ.カノウニ,トウフィケ
Environmental factors such as nutritional state may act on the epigenome that consequently contributes to the metabolic adaptation of cells and the organisms. The lysine-specific demethylase-1 (LSD1) is a unique nuclear protein that utilizes flavin adenosine dinucleotide (FAD) as a cofactor. Here we...
Lysine-specific demethylase-1 (LSD1, also known as KDM1A) is a member of the flavin-containing amine oxidase family that, in general, represses transcription by removing the methyl group from mono-methylated and di-methylated lysine 4 of histone H3 (H3K4)6. LSD1 is also involved in the ...
Lysine-specific demethylase 1 (LSD1) is involved in gene regulation and development; however, its precise function, molecular targets and underlying mechanisms during development are poorly understood. Here we show that LSD1 is required for neuronal progenitor cell (NPC) maintenance during cortical dev...