Evidence map›Paper›PMID 32369358›Full record

ArticleJournal of medicinal chemistry2020

Targeting ALK2: An Open Science Approach to Developing Therapeutics for the Treatment of Diffuse Intrinsic Pontine Glioma.

Deeba Ensan, David Smil, Carlos A Zepeda-Velázquez, Dimitrios Panagopoulos, Jong Fu Wong, Eleanor P Williams, Roslin Adamson, Alex N Bullock, Taira Kiyota, Ahmed Aman and 5 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing 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

13 citing papers in PubMed, 28 citations in OpenAlex.

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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

15 authors at 4 institutions in 3 countries.

Deeba EnsanDepartment of Pharmacology and Toxicology, University of Toronto, Medical Sciences Building, Room 4207, 1 King's College Circle, Toronto, Ontario M5S 1A8, Canada.ORCID 0000-0002-3251-1521
David SmilDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.ORCID 0000-0002-6232-6087
Carlos A Zepeda-VelázquezDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.ORCID 0000-0002-8130-2232
Dimitrios PanagopoulosDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.
Jong Fu WongStructural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, U.K.
Eleanor P WilliamsStructural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, U.K.
Roslin AdamsonStructural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, U.K.
Alex N BullockStructural Genomics Consortium, University of Oxford, Old Road Campus, Roosevelt Drive, Oxford OX3 7DQ, U.K.
Taira KiyotaDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.
Ahmed AmanDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.
Owen G RobertsM4K Pharma Inc., 101 College Street, MaRS Centre, South Tower, Toronto, Ontario M5G 1L7, Canada.
Aled M EdwardsStructural Genomics Consortium, University of Toronto, 101 College Street, MaRS Centre, South Tower, Toronto, Ontario M5G 1L7, Canada.
Jeff A O'MearaDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.
Methvin B IsaacDrug Discovery Program, Ontario Institute for Cancer Research, 661 University Avenue, MaRS Centre, West Tower, Toronto, Ontario M5G 0A3, Canada.
Rima Al-AwarDepartment of Pharmacology and Toxicology, University of Toronto, Medical Sciences Building, Room 4207, 1 King's College Circle, Toronto, Ontario M5S 1A8, Canada.ORCID 0000-0002-4185-055X
Ontario Institute for Cancer Research · CAGenomics (United Kingdom) · GBUniversity of New Brunswick · CAUniversity of Toronto · CA

Funding

Wellcome TrustWellcome Trust 106169/ZZ14/Z
6 · The paper itself

Abstract

Diffuse intrinsic pontine glioma is an aggressive pediatric cancer for which no effective chemotherapeutic drugs exist. Analysis of the genomic landscape of this disease has led to the identification of the serine/threonine kinase ALK2 as a potential target for therapeutic intervention. In this work, we adopted an open science approach to develop a series of potent type I inhibitors of ALK2 which are orally bio-available and brain-penetrant. Initial efforts resulted in the discovery of

Indexed as

Activin Receptors, Type IAnimalsBenzamidesCaco-2 CellsCell Membrane PermeabilityDiffuse Intrinsic Pontine GliomaFemaleHEK293 CellsHumansMaleMice, SCIDMicrosomes, LiverMolecular StructureMutationPiperazinesProtein Kinase InhibitorsActivin Receptors, Type IACVR1 protein, humanBenzamidesPiperazinesProtein Kinase InhibitorsPyridines

Identifiers

PMID32369358
PMCPMC8213057
OpenAlexW3023922707

What OpenQuestion holds

Textmetadata
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.