Evidence map›Paper›PMID 33007395›Full record

ArticleBioorganic & medicinal chemistry letters2020

Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness.

Aparna Sundaram, Chun Chen, Nilgun Isik Reed, Sean Liu, Seul Ki Yeon, Joel McIntosh, You-Zhi Tang, Hyunjun Yang, Marc Adler, Richard Beresis and 4 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. The integrin receptor betaRespiratory research · 2024
    Article
  4. Review
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

14 authors.

Aparna SundaramSchool of Medicine, University of California San Francisco, San Francisco, CA 94158, USA.
Chun ChenPliant Therapeutics, 260 Littlefield Ave, South San Francisco, CA 94080, USA.
Nilgun Isik ReedSchool of Medicine, University of California San Francisco, San Francisco, CA 94158, USA.
Sean LiuLung Biology Center, Department of Medicine, University of California San Francisco, San Francisco, CA 94158, USA.
Seul Ki YeonDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
Joel McIntoshDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
You-Zhi TangDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
Hyunjun YangDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
Marc AdlerChemPartner, 280 Utah Avenue, South San Francisco, CA 94080, USA.
Richard BeresisChemPartner, 280 Utah Avenue, South San Francisco, CA 94080, USA.
Ian B SeipleDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
Dean SheppardSchool of Medicine, University of California San Francisco, San Francisco, CA 94158, USA.
William F DeGradoDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA.
Hyunil JoDepartment of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA 94158, USA. Electronic address: Hyunil.Jo@ucsf.edu.

Funding

UC BRAID Center for Accelerated Innovation COVID-19 diagnostic project developmentU54HL119893 · NHLBI · UNIVERSITY OF CALIFORNIA LOS ANGELES · PI PALAZZOLO, MICHAEL J · 2013 to 2020
$18.3M
Deciphering the relationship between structure, dynamics and function in helical bundle proteinsR35GM122603 · NIGMS · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI WILLIAM DEGRADO · 2017 to 2026
$7.1M
Treatment of pulmonary fibrosis with inhibitors of integrin alphavbeta1.UH2HL123423 · NHLBI · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI DEGRADO, WILLIAM, SHEPPARD, DEAN · 2014 to 2015
$2.2M
NHLBI NIH HHS U54 HL119893NHLBI NIH HHS UH2 HL123423NIGMS NIH HHS R35 GM122603
6 · The paper itself

Abstract

Inhibition of integrin α5β1 emerges as a novel therapeutic option to block transmission of contractile forces during asthma attack. We designed and synthesized novel inhibitors of integrin α5β1 by backbone replacement of known αvβ1 integrin inhibitors. These integrin α5β1 inhibitors also retain the nanomolar potency against αvβ1 integrin, which shows promise for developing dual integrin α5β1/αvβ1 inhibitor. Introduction of hydrophobic adamantane group significantly boosted the potency as well as selectivity over integrin αvβ3. We also demonstrated one of the inhibitors (11) reduced airway hyperresponsiveness in ex vivo mouse tracheal ring assay. Results from this study will help guide further development of integrin α5β1 inhibitors as potential novel asthma therapeutics.

Indexed as

AdamantaneAnimalsDose-Response Relationship, DrugIntegrin alpha5beta1MiceMolecular StructureReceptors, VitronectinRespiratory HypersensitivityStructure-Activity RelationshipAdamantaneIntegrin alpha5beta1integrin alphavbeta1Receptors, VitronectinAsthmaIntegrin inhibitorIntegrin α5β1Integrin αvβ1RGD integrin

Identifiers

PMID33007395
PMCPMC7700746

What OpenQuestion holds

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Registered trials

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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.