Evidence map›Paper›PMID 33534953›Full record

ReviewChemMedChem2021

A Box of Chemistry to Inhibit the MEN1 Tumor Suppressor Gene Promoting Leukemia.

Ezgi Ozyerli-Goknar, Sheikh Nizamuddin, H T Marc Timmers

Open access · hybridAbstract readReview
In one paragraph

Review in ChemMedChem, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
1.9field-weighted citation impact, top 14% 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

9 citing papers in PubMed, 23 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Clinically Defined Mutations inCancer research communications · 2023
    Article
  5. Article
  6. Review
  7. Article
  8. Review
  9. Review
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

3 authors at 1 institution in 1 country.

Ezgi Ozyerli-GoknarGerman Cancer Consortium (DKTK) partner site Freiburg German Cancer Research Center (DKFZ) Medical Center-University of Freiburg, Department of Urology, Breisacherstrasse 66, 79016, Freiburg, Germany.ORCID 0000-0003-0202-8165
Sheikh NizamuddinGerman Cancer Consortium (DKTK) partner site Freiburg German Cancer Research Center (DKFZ) Medical Center-University of Freiburg, Department of Urology, Breisacherstrasse 66, 79016, Freiburg, Germany.
H T Marc TimmersGerman Cancer Consortium (DKTK) partner site Freiburg German Cancer Research Center (DKFZ) Medical Center-University of Freiburg, Department of Urology, Breisacherstrasse 66, 79016, Freiburg, Germany.ORCID 0000-0001-7062-1417
University of Freiburg · DE

Funding

Deutsche Forschungsgemeinschaft 192904750-SFB 992Deutsche Forschungsgemeinschaft TI688/1-1
6 · The paper itself

Abstract

Targeting protein-protein interactions (PPIs) with small-molecule inhibitors has become a hotbed of modern drug development. In this review, we describe a new class of PPI inhibitors that block menin from binding to MLL proteins. Menin is encoded by the MEN1 tumor suppressor, but acts as an essential cofactor for MLL/KMT2A-rearranged leukemias. The most promising menin-MLL inhibitors belong to the thienopyrimidine class and have recently entered phase I/II clinical trials for treating acute leukemias characterized by MLL/KMT2A translocations or NPM1 mutations. As single agents, thienopyrimidine compounds eradicate leukemia in a xenograft models of primary leukemic cells belonging to the MLL-rearranged or NPM1-mutant subtypes. These compounds are well tolerated with few or no side effects, which is remarkable given the tumor-suppressor function of menin. The menin-MLL inhibitors highlight how leukemia patients could benefit from a targeted epigenetic therapy with novel PPI inhibitors obtained by directed chemical evolution.

Indexed as

AnimalsAntineoplastic AgentsHistone-Lysine N-MethyltransferaseHumansLeukemiaMyeloid-Lymphoid Leukemia ProteinNucleophosminPeptidomimeticsProtein Interaction MapsProto-Oncogene ProteinsPyrimidinesAntineoplastic AgentsHistone-Lysine N-MethyltransferaseKMT2A protein, humanMEN1 protein, humanMyeloid-Lymphoid Leukemia ProteinNPM1 protein, humanNucleophosminPeptidomimeticsProto-Oncogene ProteinsPyrimidinesacute leukemiaschromatin regulationmeninMLLthienopyrimidines

Identifiers

PMID33534953
PMCPMC8252030
OpenAlexW3127239358

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.