ArticleJournal of medicinal chemistry2026
Discovery of a Highly Potent and Selective ENL Degrader.
Kaixiu Luo, Zhaoyu Xue, Lihuai Qin, Zhefan Wang, Pengcheng Gao, Ling Xie, Yangzhou Su, Xian Chen, H Ümit Kaniskan, Hong Wen and 1 more
Abstract read
In one paragraphArticle in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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What it found
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2 · The registryThe trial behind it
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3 · Its place in the literatureWho cites it
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4 · The recordCorrections and comments
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5 · Who and what moneyAuthors and funding
11 authors.
Kaixiu LuoMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, the Mount Sinai Tisch Cancer Center, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Zhaoyu XueDepartment of Epigenetics, Van Andel Institute, Grand Rapids, Michigan 49503, United States.
Lihuai QinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, the Mount Sinai Tisch Cancer Center, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Zhefan WangDepartment of Epigenetics, Van Andel Institute, Grand Rapids, Michigan 49503, United States.ORCID 0009-0009-7120-8507 Pengcheng GaoMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, the Mount Sinai Tisch Cancer Center, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0003-4266-0616 Ling XieDepartment of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Yangzhou SuDepartment of Epigenetics, Van Andel Institute, Grand Rapids, Michigan 49503, United States.
Xian ChenDepartment of Biochemistry and Biophysics, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
H Ümit KaniskanMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, the Mount Sinai Tisch Cancer Center, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0001-5327-832X Hong WenDepartment of Epigenetics, Van Andel Institute, Grand Rapids, Michigan 49503, United States.ORCID 0000-0001-8739-4572 Jian JinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Science, Oncological Science and Neuroscience, the Mount Sinai Tisch Cancer Center, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0002-2387-3862 Funding
Development of Novel PROTACs Targeting the ENL YEATS Domain for Treating MLL-rearranged LeukemiasR01CA260666 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN, WEN, HONG · 2021 to 2025
$2.5MDiscovery of small molecules targeting the histone acetylation reader ENLR01CA255506 · NCI · VAN ANDEL RESEARCH INSTITUTE · PI WEN, HONG · 2021 to 2024
$1.7MAn AVANCE NEO 400 MHz NMR Spectrometer for Chemical Biology and Drug DiscoveryS10OD028504 · OD · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZHOU, MING-MING · 2020 to 2020
$599kAn AVANCE NEO 600 MHz NMR Spectrometer System for Structural and Chemical BiologyS10OD025132 · OD · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZHOU, MING-MING · 2019 to 2019
$535kNCI NIH HHS R01 CA255506NCI NIH HHS R01 CA260666NIH HHS S10 OD025132NIH HHS S10 OD028504
6 · The paper itselfAbstract
The eleven-nineteen leukemia protein (ENL), a YEATS domain-containing acyl-lysine reader, represents a critical dependency in acute myeloid leukemia (AML). We previously reported our first-generation ENL proteolysis-targeting chimera (PROTAC) degrader, MS41. Here, via a comprehensive structure-activity relationship (SAR) study, we discovered MS108 (compound
Indexed as
Antineoplastic AgentsDrug DiscoveryAnimalsCell Line, TumorCell ProliferationHumansLeukemia, Myeloid, AcuteProteolysisProteolysis Targeting ChimeraStructure-Activity RelationshipVon Hippel-Lindau Tumor Suppressor ProteinAntineoplastic AgentsProteolysis Targeting ChimeraVon Hippel-Lindau Tumor Suppressor Protein
Identifiers
PMID42025203
PMCPMC13143349
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