{"entity": "publication", "iuid": "becc2681bf4f4635b135e0ef6f982e0f", "timestamp": "2026-08-22T08:30:21.676Z", "links": {"self": {"href": "https://publications-affiliated.scilifelab.se/publication/becc2681bf4f4635b135e0ef6f982e0f.json"}, "display": {"href": "https://publications-affiliated.scilifelab.se/publication/becc2681bf4f4635b135e0ef6f982e0f"}}, "title": "Discovery of 2-Aryl-4-aminoquinazolin-Based LSD1 Inhibitors to Activate Immune Response in Gastric Cancer.", "authors": [{"family": "Wang", "given": "Bo", "initials": "B", "orcid": "0000-0001-8149-6439", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/4a6a7297732742e78efbbbfc815bb87f.json"}}, {"family": "Wang", "given": "Shu-Wu", "initials": "SW"}, {"family": "Zhou", "given": "Ying", "initials": "Y"}, {"family": "Wang", "given": "Shao-Peng", "initials": "SP"}, {"family": "Gao", "given": "Ya", "initials": "Y", "orcid": "0000-0002-3093-9727", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/196ff96cfbbf4edf8656e59e1ff361af.json"}}, {"family": "Liu", "given": "Hui-Min", "initials": "HM"}, {"family": "Ji", "given": "Shi-Kun", "initials": "SK"}, {"family": "Wang", "given": "Sai-Qi", "initials": "SQ"}, {"family": "Zheng", "given": "Yi-Chao", "initials": "YC", "orcid": "0000-0002-2662-3770", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/562f44443813490aab5a05ea28ba55ad.json"}}, {"family": "Zhang", "given": "Cheng", "initials": "C"}, {"family": "Mardinoglu", "given": "Adil", "initials": "A"}, {"family": "Liu", "given": "Hong-Min", "initials": "HM"}, {"family": "Chen", "given": "Xiao-Bing", "initials": "XB"}, {"family": "Dai", "given": "Xing-Jie", "initials": "XJ", "orcid": "0000-0001-7531-044X", "researcher": {"href": "https://publications-affiliated.scilifelab.se/researcher/57be2edadc104e97bc316b221f0e1889.json"}}], "type": "journal article", "published": "2024-09-26", "journal": {"title": "J Med Chem", "issn": "1520-4804", "volume": "67", "issue": "18", "pages": "16165-16184", "issn-l": "0022-2623"}, "abstract": "LSD1 (histone lysine-specific demethylase 1) has been gradually disclosed to act as an immunomodulator to enhance antitumor immune response. Despite the identification of numerous potent LSD1 inhibitors, there remains a lack of LSD1 inhibitors approved for marketing. Novel LSD1 inhibitors with different mechanisms are therefore needed. Herein, we reported a series of novel quinazoline-based LSD1 inhibitors. Among them, compound Z-1 exhibited the best LSD1 inhibitory activity (IC50 = 0.108 \u03bcM). Z-1 also acted as a selective and cellular active as an LSD1 inhibitor. Furthermore, Z-1 promoted response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuated the PD-1/PD-L1 interaction. In vivo, Z-1 exhibited significant suppression effect on the growth of gastric cancer cells without obvious toxicity. Therefore, Z-1 represents a potential novel immunomodulator that targets LSD1, providing a lead compound with new function mechanism for gastric cancer treatment.", "doi": "10.1021/acs.jmedchem.4c00972", "pmid": "39264726", "labels": [], "xrefs": [], "notes": [], "created": "2026-08-20T08:10:50.299Z", "modified": "2026-08-20T08:10:50.455Z"}