Evidence map›Paper›PMID 38533580›Full record

ArticleJournal of medicinal chemistry2024

Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.

Yan Xiong, Holger Greschik, Catrine Johansson, Ludwig Seifert, Vicki Gamble, Kwang-Su Park, Vincent Fagan, Fengling Li, Irene Chau, Masoud Vedadi and 9 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 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
0.5field-weighted citation impact, top 38% 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

2 citing papers in PubMed, 2 citations in OpenAlex.

  1. Article
  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

19 authors at 8 institutions in 4 countries.

Yan XiongMount 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, New York 10029, United States.
Holger GreschikDepartment of Urology and Center for Clinical Research, University Freiburg Medical Center, Freiburg 79106, Germany.
Catrine JohanssonStructural Genomics Consortium, Botnar Research Center, NIHR Oxford BRU, University of Oxford, Oxford OX3 7LD, U.K.
Ludwig SeifertInstitute of Pharmaceutical Sciences, University of Freiburg, Freiburg 79104, Germany.
Vicki GambleStructural Genomics Consortium, Botnar Research Center, NIHR Oxford BRU, University of Oxford, Oxford OX3 7LD, U.K.
Kwang-Su ParkMount 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, New York 10029, United States.ORCID 0000-0002-1910-3937
Vincent FaganCentre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.; Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.
Fengling LiStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Irene ChauStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Masoud VedadiOntario Institute for Cancer Research, 661 University Avenue, Toronto, Ontario M5G 0A3, Canada.
Cheryl H ArrowsmithStructural Genomics Consortium, University of Toronto, Toronto, Ontario M5G 1L7, Canada.
Paul BrennanCentre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.; Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.
Oleg FedorovCentre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.; Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.
Manfred JungInstitute of Pharmaceutical Sciences, University of Freiburg, Freiburg 79104, Germany.ORCID 0000-0002-6361-7716
Gillian FarnieCentre for Medicines Discovery, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.; Target Discovery Institute, Nuffield Department of Medicine, University of Oxford, Oxford OX3 7FZ, U.K.
Jing LiuMount 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, New York 10029, United States.
Udo OppermannStructural Genomics Consortium, Botnar Research Center, NIHR Oxford BRU, University of Oxford, Oxford OX3 7LD, U.K.
Roland SchüleDepartment of Urology and Center for Clinical Research, University Freiburg Medical Center, Freiburg 79106, Germany.
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, New York 10029, United States.ORCID 0000-0002-2387-3862
Icahn School of Medicine at Mount Sinai · USNuffield Orthopaedic Centre · GBUniversity of Freiburg · DEUniversity of Toronto · CAOxford BioMedica (United Kingdom) · GBOntario Institute for Cancer Research · CAUniversity Medical Center Freiburg · DEUniversity of Oxford · GB

Funding

An AVANCE NEO 400 MHz NMR Spectrometer for Chemical Biology and Drug DiscoveryS10OD028504 · OD · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI ZHOU, MING-MING · 2020 to 2020
$599k
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
Cancer Research UKNIH HHS S10 OD025132NIH HHS S10 OD028504
6 · The paper itself

Abstract

The methyl-lysine reader protein SPIN1 plays important roles in various human diseases. However, targeting methyl-lysine reader proteins has been challenging. Very few cellularly active SPIN1 inhibitors have been developed. We previously reported that our G9a/GLP inhibitor UNC0638 weakly inhibited SPIN1. Here, we present our comprehensive structure-activity relationship study that led to the discovery of compound

Indexed as

LysineTudor DomainAnimalsHumansMiceStructure-Activity RelationshipLysinemethyl-lysine

Identifiers

PMID38533580
PMCPMC11022035
OpenAlexW4393227377

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.