Evidence map›Paper›PMID 40102181›Full record

ArticleJournal of medicinal chemistry2025

From DNA-Encoded Library Screening to

Ian Sarvary, Mikkel Vestergaard, Loris Moretti, Jan Andersson, Jorge Peiró Cadahía, Sanne Cowland, Thomas Flagstad, Thomas Franch, Alex Gouliaev, Gitte Husemoen and 33 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. 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. Review
  3. Article
  4. Article
  5. Review
  6. Review
  7. MTA-cooperative PRMT5 inhibitors from cofactor-directed DNA-encoded library screens.Proceedings of the National Academy of Sciences of the United States of America · 2025
    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

43 authors.

Ian SarvaryAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.ORCID 0009-0006-3722-8510
Mikkel VestergaardAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Loris MorettiAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Jan AnderssonAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.ORCID 0009-0009-3962-4463
Jorge Peiró CadahíaAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.ORCID 0009-0009-5039-7118
Sanne CowlandAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Thomas FlagstadAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Thomas FranchAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Alex GouliaevAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Gitte HusemoenAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Tomas JacsoAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Titi KronborgAmgen Research, Amgen Inc, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
Aleksandra KuropatnickaAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Anna NadaliAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Mads MadsenAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
So Ren NielsenAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.ORCID 0009-0004-7115-5189
David PiiAmgen Research, Amgen Inc, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
So Ren RyborgAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.
Camillia SoedeAmgen Research, Amgen Inc, Fruebjergvej 3, DK-2100 Copenhagen, Denmark.
Jennifer R AllenAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Matthew BourbeauAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Kexue LiAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Qingyian LiuAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Mei-Chu LoAmgen Research, Amgen Inc, 750 Gateway Blvd, South San Francisco, California 94080, United States.
Franck MadouxAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Narbe MardirossianAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.ORCID 0000-0002-1387-0158
Jodi MoriguchiAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Rachel NgoAmgen Research, Amgen Inc, 750 Gateway Blvd, South San Francisco, California 94080, United States.
Chi-Chi PengAmgen Research, Amgen Inc, 750 Gateway Blvd, South San Francisco, California 94080, United States.
Liping PettusAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.ORCID 0000-0002-4427-6602
Nuria TamayoAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.ORCID 0000-0002-0497-5230
Paul WangAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Rajiv KapoorAmgen Research, Syngene-Amgen Research and Development Center, Biocon Park, Bangalore 560099, India.
Brian BelmontesAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Sean CaenepeelAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Paul HughesAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Siyuan LiuAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Katherine K SlemmonsAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.ORCID 0000-0003-3700-5633
Yajing YangAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Fang XieAmgen Research, Amgen Inc, 750 Gateway Blvd, South San Francisco, California 94080, United States.
Sudipa Ghimire-RijalAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Susmith MukundAmgen Research, Amgen Inc, One Amgen Center Drive, Thousand Oaks, California 91320, United States.
Sanne GladAmgen Research, Amgen Inc, Ro̷nnegade 8, DK-2100 Copenhagen, Denmark.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibition of the methyltransferase enzyme PRMT5 by MTA accumulation is a vulnerability of MTAP-deleted cancers. Herein, we report the discovery and optimization of a quinolin-2-amine DEL hit that cooperatively binds PRMT5:MEP50 and MTA to generate a catalytically inhibited ternary complex. X-ray crystallography confirms quinolin-2-amine binding of PRMT5 glutamate-444, while simultaneously exhibiting a hydrophobic interaction with MTA. Lead optimization produced

Indexed as

Enzyme InhibitorsProtein-Arginine N-MethyltransferasesAdministration, OralAnimalsAntineoplastic AgentsCell Line, TumorCrystallography, X-RayDNAFemaleHumansMiceMice, NudeStructure-Activity RelationshipXenograft Model Antitumor AssaysAntineoplastic AgentsDNAEnzyme InhibitorsPRMT5 protein, humanProtein-Arginine N-Methyltransferases

Identifiers

PMID40102181
PMCPMC11956014

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.