Evidence map›Paper›PMID 33276504›Full record

ArticleMolecules (Basel, Switzerland)2020

Antiangiogenic Activity and in Silico Cereblon Binding Analysis of Novel Thalidomide Analogs.

Megan L Peach, Shaunna L Beedie, Cindy H Chau, Matthew K Collins, Suzana Markolovic, Weiming Luo, David Tweedie, Christian Steinebach, Nigel H Greig, Michael Gütschow and 3 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.0field-weighted citation impact, top 25% 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

14 citing papers in PubMed, 20 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

13 authors at 5 institutions in 3 countries.

Megan L PeachBasic Science Program, Chemical Biology Laboratory, Frederick National Laboratory for Cancer Research, National Cancer Institute, Frederick, MD 21701, USA.ORCID 0000-0002-4290-5268
Shaunna L BeedieMolecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
Cindy H ChauMolecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
Matthew K CollinsMolecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.ORCID 0000-0002-9305-3560
Suzana MarkolovicMolecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.
Weiming LuoDrug Design & Development Section, Translational Gerontology Branch, National Institute on Aging, NIH, Baltimore, MD 21224, USA.
David TweedieDrug Design & Development Section, Translational Gerontology Branch, National Institute on Aging, NIH, Baltimore, MD 21224, USA.
Christian SteinebachPharmaceutical Institute, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0001-5638-1955
Nigel H GreigDrug Design & Development Section, Translational Gerontology Branch, National Institute on Aging, NIH, Baltimore, MD 21224, USA.
Michael GütschowPharmaceutical Institute, University of Bonn, 53121 Bonn, Germany.ORCID 0000-0002-9376-7897
Neil VargessonSchool of Medicine, Medical Sciences & Nutrition, Institute of Medical Sciences, University of Aberdeen, Aberdeen AB25 2ZD, UK.ORCID 0000-0001-8027-114X
Marc C NicklausChemical Biology Laboratory, Center for Cancer Research, National Cancer Institute, NIH, Frederick, MD 21701, USA.
William D FiggMolecular Pharmacology Section, Genitourinary Malignancies Branch, Center for Cancer Research, National Cancer Institute, NIH, Bethesda, MD 20892, USA.ORCID 0000-0003-2428-5613
National Cancer Institute · USNational Institute on Aging · USUniversity of Aberdeen · GBUniversity of Bonn · DEFrederick National Laboratory for Cancer Research · US

Funding

Development of Anticancer AgentsZIASC006538 · NCI · DIVISION OF CLINICAL SCIENCES - NCI · PI FIGG, WILLIAM DOUGLAS · 2009 to 2025
$8.6M
NCI NIH HHS HHSN261200800001ENCI NIH HHS ZIA SC006538Wellcome Trust 098252/Z/12/Z
6 · The paper itself

Abstract

Due to its antiangiogenic and anti-immunomodulatory activity, thalidomide continues to be of clinical interest despite its teratogenic actions, and efforts to synthesize safer, clinically active thalidomide analogs are continually underway. In this study, a cohort of 27 chemically diverse thalidomide analogs was evaluated for antiangiogenic activity in an ex vivo rat aorta ring assay. The protein cereblon has been identified as the target for thalidomide, and in silico pharmacophore analysis and molecular docking with a crystal structure of human cereblon were used to investigate the cereblon binding abilities of the thalidomide analogs. The results suggest that not all antiangiogenic thalidomide analogs can bind cereblon, and multiple targets and mechanisms of action may be involved.

Indexed as

Molecular Docking SimulationAdaptor Proteins, Signal TransducingAngiogenesis InhibitorsAnimalsAortaComputer SimulationHumansMaleNeovascularization, PhysiologicRatsRats, Sprague-DawleyThalidomideUbiquitin-Protein LigasesAdaptor Proteins, Signal TransducingAngiogenesis InhibitorsCRBN protein, humanThalidomideUbiquitin-Protein Ligasesangiogenesiscereblondockingstructure–activity relationshipsthalidomide

Identifiers

PMID33276504
PMCPMC7730988
OpenAlexW3108823767

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.