Evidence map›Paper›PMID 33416017›Full record

ArticleChannels (Austin, Tex.)2021

Comparison of quinazoline and benzoylpyrazoline chemotypes targeting the CaVα-β interaction as antagonists of the N-type CaV2.2 channel.

Dongzhi Ran, Kimberly Gomez, Aubin Moutal, Marcel Patek, Samantha Perez-Miller, Rajesh Khanna

Abstract readComparative Study
In one paragraph

Article in Channels (Austin, Tex.), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing 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

6 citing papers in PubMed.

  1. Review
  2. Review
  3. A peptidomimetic modulator of the CaProceedings of the National Academy of Sciences of the United States of America · 2023
    Article
  4. Review
  5. Review
  6. R and S enantiomers of CBD3063, a CaNeurobiology of pain (Cambridge, Mass.)
    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

6 authors.

Dongzhi RanDepartment of Pharmacology, College of Medicine, The University of Arizona , Tucson, AZ, USA.ORCID 0000-0002-5862-7805
Kimberly GomezDepartment of Pharmacology, College of Medicine, The University of Arizona , Tucson, AZ, USA.ORCID 0000-0003-1867-5041
Aubin MoutalDepartment of Pharmacology, College of Medicine, The University of Arizona , Tucson, AZ, USA.ORCID 0000-0003-4268-1206
Marcel PatekBright Rock Path Consulting, LLC , Tucson, AZ, USA.
Samantha Perez-MillerDepartment of Pharmacology, College of Medicine, The University of Arizona , Tucson, AZ, USA.ORCID 0000-0002-9034-3693
Rajesh KhannaDepartment of Pharmacology, College of Medicine, The University of Arizona , Tucson, AZ, USA.ORCID 0000-0002-9066-2969

Funding

CRMP2, mitochondria, and Huntington’s diseaseR01NS098772 · NINDS · INDIANA UNIVERSITY INDIANAPOLIS · PI BRUSTOVETSKY, NICKOLAY, KHANNA, RAJESH · 2017 to 2021
$2.8M
Sentrin proteases, CRMP2 deSUMOylation, and Chronic PainR01NS120663 · NINDS · UNIVERSITY OF FLORIDA · PI KHANNA, RAJESH · 2020 to 2021
$2.6M
Exploring CRMP5 as a novel target for Alzheimers diseaseR01NS119263 · NINDS · UNIVERSITY OF ARIZONA · PI Aubin Moutal · 2021 to 2026
$2.2M
CRMP2, Nav1.7 sodium channel, and chronic painR01DA042852 · NIDA · UNIVERSITY OF ARIZONA · PI KHANNA, RAJESH · 2017 to 2021
$1.9M
NIDA NIH HHS R01 DA042852NINDS NIH HHS R01 NS098772NINDS NIH HHS R01 NS119263NINDS NIH HHS R01 NS120663
6 · The paper itself

Abstract

Structural studies with an α subunit fragment of voltage-gated calcium (CaV) channels in complex with the CaVβ subunits revealed a high homology between the various CaVα-β subunits, predicting that targeting of this interface would result in nonselective compounds. Despite this likelihood, my laboratory initiated a rational structure-based screening campaign focusing on "hot spots" on the alpha interacting domain (AID) of the CaVβ2a subunits and identified the small molecule 2-(3,5-dimethylisoxazol-4-yl)-N-((4-((3-phenylpropyl)amino)quinazolin-2-yl)methyl)acetamide (

Indexed as

Calcium Channels, N-TypeQuinazolinesAnimalsCalcium Channel BlockersHumansPyrazolesRatsCalcium Channel BlockersCalcium Channels, N-TypePyrazolesQuinazolinesCaV alpha-beta interactionchronic painN-type/CaV2.2 antagonistsPPIs

Identifiers

PMID33416017
PMCPMC7808423

What OpenQuestion holds

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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.