Evidence map›Paper›PMID 33591753›Full record

ArticleJournal of medicinal chemistry2021

A First-in-Class, Highly Selective and Cell-Active Allosteric Inhibitor of Protein Arginine Methyltransferase 6.

Yudao Shen, Fengling Li, Magdalena M Szewczyk, Levon Halabelian, Irene Chau, Mohammad S Eram, Carlo Dela Seña, Kwang-Su Park, Fanye Meng, He Chen and 17 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.8field-weighted citation impact, top 15% 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

11 citing papers in PubMed, 26 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
  5. Article
  6. Review
  7. Protein arginine methylation in viral infection and antiviral immunity.International journal of biological sciences · 2023
    Review
  8. Review
  9. The Emerging Role of PRMT6 in Cancer.Frontiers in oncology · 2022
    Review
  10. Review
  11. Review
4 · The record

Corrections and comments

5 · Who and what money

Authors and funding

27 authors at 4 institutions in 2 countries.

Yudao ShenMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Fengling LiStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Magdalena M SzewczykStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Levon HalabelianStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.ORCID 0000-0003-4361-3619
Irene ChauStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Mohammad S EramStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Carlo Dela SeñaStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Kwang-Su ParkMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Fanye MengMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
He ChenMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
Hong ZengStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Aiping DongStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Hong WuStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Viacheslav V TrushStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
David McLeodOntario Institute for Cancer Research, Toronto, Ontario M5G 0A3, Canada.
Carlos A Zepeda-VelázquezOntario Institute for Cancer Research, Toronto, Ontario M5G 0A3, Canada.
Robert M CampbellEli Lilly and Company, Lilly Research Laboratories, Indianapolis, Indiana 46225, United States.
Mary M MaderEli Lilly and Company, Lilly Research Laboratories, Indianapolis, Indiana 46225, United States.
Brian M WatsonEli Lilly and Company, Lilly Research Laboratories, Indianapolis, Indiana 46225, United States.
Matthieu SchapiraStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.ORCID 0000-0002-1047-3309
Cheryl H ArrowsmithStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.ORCID 0000-0002-4971-3250
Rima Al-AwarOntario Institute for Cancer Research, Toronto, Ontario M5G 0A3, Canada.
Dalia Barsyte-LovejoyStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
H Ümit KaniskanMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.ORCID 0000-0001-5327-832X
Peter J BrownStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Masoud VedadiStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Jian JinMount Sinai Center for Therapeutics Discovery, Departments of Pharmacological Sciences and Oncological Sciences, Tisch Cancer Institute, Icahn School of Medicine at Mount Sinai, New York, New York 10029, United States.
University of Toronto · CAIcahn School of Medicine at Mount Sinai · USEli Lilly (United States) · USOntario Institute for Cancer Research · CA

Funding

THE TISCH CANCER INSTITUTE - CANCER CENTER SUPPORT GRANTP30CA196521 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI Ramon E Parsons · 2015 to 2026
$35.4M
Discovery of Selective Inhibitors for Histone MethyltransferasesR01GM122749 · NIGMS · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI JIN, JIAN · 2017 to 2020
$1.3M
An 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
$535k
NCI NIH HHS P30 CA196521NIGMS NIH HHS R01 GM122749NIH HHS S10 OD025132Wellcome TrustWellcome Trust 106169/ZZ14/Z
6 · The paper itself

Abstract

Protein arginine methyltransferase 6 (PRMT6) catalyzes monomethylation and asymmetric dimethylation of arginine residues in various proteins, plays important roles in biological processes, and is associated with multiple cancers. To date, a highly selective PRMT6 inhibitor has not been reported. Here we report the discovery and characterization of a first-in-class, highly selective allosteric inhibitor of PRMT6,

Indexed as

Allosteric RegulationAllosteric SiteBenzodiazepinonesCrystallography, X-RayEnzyme InhibitorsHEK293 CellsHumansNuclear ProteinsProtein-Arginine N-MethyltransferasesProtein BindingStereoisomerismBenzodiazepinonesEnzyme InhibitorsNuclear ProteinsPRMT6 protein, humanProtein-Arginine N-Methyltransferases

Identifiers

PMID33591753
PMCPMC8035306
OpenAlexW3131552156

What OpenQuestion 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 OpenQuestion graph.