Evidence map›Paper›PMID 32338903›Full record

ArticleJournal of medicinal chemistry2020

Discovery of M-808 as a Highly Potent, Covalent, Small-Molecule Inhibitor of the Menin-MLL Interaction with Strong

Shilin Xu, Angelo Aguilar, Liyue Huang, Tianfeng Xu, Ke Zheng, Donna McEachern, Sally Przybranowski, Caroline Foster, Kaitlin Zawacki, Zhaomin Liu and 3 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.

0numbers the graph read from it
0cells of the map it votes in
15citing papers in PubMed
1.7field-weighted citation impact, top 16% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

15 citing papers in PubMed, 39 citations in OpenAlex.

  1. Review
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  4. Distinct Responses to Menin Inhibition and Synergy with DOT1L Inhibition inInternational journal of molecular sciences · 2024
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors at 1 institution in 1 country.

Angelo Aguilar
Liyue Huang
Tianfeng Xu
Donna McEachern
Sally Przybranowski
Caroline Foster
Kaitlin Zawacki
Zhaomin Liu
Krishnapriya Chinnaswamy
Jeanne Stuckey
University of Michigan · US

Funding

XenograftP30CA046592 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI THEODORE S LAWRENCE · 1988 to 2026
$178.2M
Targeting the menin-MLL1 complex for new therapeuticsR01CA208267 · NCI · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI WANG, SHAOMENG · 2018 to 2022
$3.2M
NCI NIH HHS P30 CA046592NCI NIH HHS R01 CA208267
6 · The paper itself

Abstract

Targeting the menin-MLL protein-protein interaction is a new therapeutic strategy for the treatment of acute leukemia carrying MLL fusion (MLL leukemia). We describe herein the structure-based optimization of a class of covalent menin inhibitors, which led to the discovery of M-808 (

Indexed as

AnimalsAntineoplastic AgentsAzetidinesCell Line, TumorCrystallography, X-RayDrug Screening Assays, AntitumorFemaleHistone-Lysine N-MethyltransferaseHumansLeukemia, Myeloid, AcuteMice, SCIDMolecular StructureMyeloid-Lymphoid Leukemia ProteinProtein BindingProto-Oncogene ProteinsXenograft Model Antitumor AssaysAntineoplastic AgentsAzetidinesHistone-Lysine N-MethyltransferaseKMT2A protein, humanMEN1 protein, humanMyeloid-Lymphoid Leukemia ProteinProto-Oncogene Proteins

Identifiers

PMID32338903
PMCPMC7981784
OpenAlexW3018968521

What OpenQuestion holds

Textmetadata
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Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.