Evidence map›Paper›PMID 37379717›Full record

ReviewCurrent opinion in chemical biology2023

Recent advances in developing degraders & inhibitors of lysine methyltransferases.

Julia Velez, H Ümit Kaniskan, Jian Jin

Abstract readReview
In one paragraph

Review in Current opinion in chemical biology, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing 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

7 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. Chromatin remodellers as therapeutic targets.Nature reviews. Drug discovery · 2024
    Review
  5. Article
  6. Article
  7. 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.

Julia VelezMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States.
H Ümit KaniskanMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States. Electronic address: husnu.kaniskan@mssm.edu.
Jian JinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences, Oncological Sciences and Neuroscience, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, NY 10029, United States. Electronic address: jian.jin@mssm.edu.

Funding

TRAINING PROGRAM IN CANCER THERAPYT32CA078207 · NCI · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI James J Manfredi · 1999 to 2026
$11.6M
Discovery of First-in-class WDR5 PROTACs as a Novel Therapeutic Strategy for MLL-rearranged LeukemiasR01CA268384 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI Jian Jin, G Greg Wang · 2022 to 2026
$3.9M
Dissecting and targeting canonical and non-canonical oncogenic functions of EZH2 in canerR01CA268519 · NCI · UNIV OF NORTH CAROLINA CHAPEL HILL · PI Jian Jin, G Greg Wang · 2022 to 2026
$3.2M
Targeting Lysine Methyltransferases EZH2 and EZH1 for Treating MLL-rearranged LeukemiasR01CA218600 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN, WANG, G GREG · 2017 to 2021
$2.8M
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
$2.5M
(PQ9) Developing EZH2 Degraders for Treating Triple-Negative Breast CancerR01CA230854 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN, PARSONS, RAMON E · 2018 to 2022
$1.5M
NCI NIH HHS R01 CA218600NCI NIH HHS R01 CA230854NCI NIH HHS R01 CA260666NCI NIH HHS R01 CA268384NCI NIH HHS R01 CA268519NCI NIH HHS T32 CA078207
6 · The paper itself

Abstract

Over the last several decades, there has been continued interest in developing novel therapeutic approaches targeting protein lysine methyltransferases (PKMTs). Along with PKMT inhibitors, targeted protein degradation (TPD) has emerged as a promising strategy to attenuate aberrant PKMT activity. Particularly, proteolysis targeting chimeras (PROTACs) effectively eliminate PKMTs of interest, suppressing all enzymatic and non-enzymatic functions. PROTACs and other TPD approaches add new depth to PKMT research and novel therapeutics discovery. This review focuses on recent advances in PKMT degrader and inhibitor development over the last several years.

Indexed as

Histone-Lysine N-MethyltransferaseLysineProteolysisHistone-Lysine N-MethyltransferaseLysineDegradersInhibitorsLysine MethyltransferasesPROTACs

Identifiers

PMID37379717
PMCPMC10527319

What OpenQuestion holds

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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.