Evidence map›Paper›PMID 38742921›Full record

ArticleBiochemistry2024

Anticancer Drugs of Lysine Specific Histone Demethylase-1 (LSD1) Display Variable Inhibition on Nucleosome Substrates.

Dulmi Senanayaka, Danyun Zeng, Emre Deniz, Indunil K Priyankara, Joceline Helmbreck, Owen Schneider, Aashay Mardikar, Aykut Uren, Nicholas J Reiter

Abstract read
In one paragraph

Article in Biochemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–field-weighted citation impact
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

2 citing papers in PubMed.

  1. Review
  2. Article
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

9 authors.

Dulmi SenanayakaDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Danyun ZengDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Emre DenizDepartment of Oncology, Georgetown University Medical Center, Georgetown University, Washington, D.C. 20007, United States.ORCID 0000-0002-9635-983X
Indunil K PriyankaraDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Joceline HelmbreckDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Owen SchneiderDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Aashay MardikarDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.
Aykut UrenDepartment of Oncology, Georgetown University Medical Center, Georgetown University, Washington, D.C. 20007, United States.
Nicholas J ReiterDepartment of Chemistry, Marquette University, Milwaukee, Wisconsin 53233. United States.ORCID 0000-0002-6095-6528

Funding

Supplement to Existing Grant for the acquisition of a circular dichroism spectrometer at Marquette University's Chemistry DepartmentR01GM120572 · NIGMS · VANDERBILT UNIVERSITY · PI Nicholas J Reiter · 2017 to 2026
$3.2M
NIGMS NIH HHS R01 GM120572
6 · The paper itself

Abstract

Lysine specific demethylase-1 (LSD1) serves as a regulator of transcription and represents a promising epigenetic target for anticancer treatment. LSD1 inhibitors are in clinical trials for the treatment of Ewing's sarcoma (EWS), acute myeloid leukemia, and small cell lung cancer, and the development of robust inhibitors requires accurate methods for probing demethylation, potency, and selectivity. Here, the inhibition kinetics on the H3K4me2 peptide and nucleosome substrates was examined, comparing the rates of demethylation in the presence of reversible [CC-90011 (PD) and SP-2577 (SD)] and irreversible [ORY-1001 (ID) and tranylcypromine (TCP)] inhibitors. Inhibitors were also subject to viability studies in three human cell lines and Western blot assays to monitor H3K4me2 nucleosome levels in EWS (TC-32) cells, enabling a correlation of drug potency, inhibition

Indexed as

Antineoplastic AgentsHistone DemethylasesNucleosomesCell Line, TumorEnzyme InhibitorsHistonesHumansKineticsSubstrate SpecificityTranylcypromineAntineoplastic AgentsEnzyme InhibitorsHistone DemethylasesHistonesKDM1A protein, humanNucleosomesTranylcypromine

Identifiers

PMID38742921
PMCPMC12129301

What Socratic holds

Textmetadata
LicenceTDM
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 Socratic graph.