Evidence map›Paper›PMID 22072993›Full record

ArticleMarine drugs2011

Design of new α-conotoxins: from computer modeling to synthesis of potent cholinergic compounds.

Igor E Kasheverov, Maxim N Zhmak, Alexey Y Khruschov, Victor I Tsetlin

Open access · goldAbstract read
In one paragraph

Article in Marine drugs, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
0.5field-weighted citation impact, top 35% 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

18 citing papers in PubMed, 27 citations in OpenAlex.

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  18. Computational exploration of a protein receptor binding space with student proposed peptide ligands.Biochemistry and molecular biology education : a bimonthly publication of the International Union of Biochemistry and Molecular Biology
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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

4 authors at 1 institution in 1 country.

Igor E KasheverovShemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya Street, 16/10 Moscow 117997, Russia.
Maxim N ZhmakShemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya Street, 16/10 Moscow 117997, Russia.
Alexey Y KhruschovShemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya Street, 16/10 Moscow 117997, Russia.
Victor I TsetlinShemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya Street, 16/10 Moscow 117997, Russia.
Institute of Bioorganic Chemistry · RU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

A series of 14 new analogs of α-conotoxin PnIA Conus pennaceus was synthesized and tested for binding to the human α7 nicotinic acetylcholine receptor (nAChR) and acetylcholine-binding proteins (AChBP) Lymnaea stagnalis and Aplysia californica. Based on computer modeling and the X-ray structure of the A. californica AChBP complex with the PnIA[A10L, D14K] analog, single and multiple amino acid substitutions were introduced in α-conotoxin PnIA aimed at compounds of higher affinity and selectivity. Three analogs, PnIA[L5H], PnIA[A10L, D14K] and PnIA[L5R, A10L, D14R], have high affinities for AChBPs or α7 nAChR, as found in competition with radioiodinated α-bungarotoxin. That is why we prepared radioiodinated derivatives of these α-conotoxins, demonstrated their specific binding and found that among the tested synthetic analogs, most had almost 10-fold higher affinity in competition with radioactive α-conotoxins as compared to competition with radioactive α-bungarotoxin. Thus, radioiodinated α-conotoxins are a more sensitive tool for checking the activity of novel α-conotoxins and other compounds quickly dissociating from the receptor complexes.

Indexed as

Computer-Aided DesignDrug Designalpha7 Nicotinic Acetylcholine ReceptorAnimalsAplysiaBinding, CompetitiveBungarotoxinsCarrier ProteinsConotoxinsHalogenationHumansLymnaeaProtein BindingRadioligand AssayReceptors, NicotinicStructure-Activity RelationshipAChBP protein, Lymnaeaalpha7 Nicotinic Acetylcholine ReceptorBungarotoxinsCarrier ProteinsChrna7 protein, humanConotoxinsReceptors, Nicotinicacetylcholine-binding proteinscomputer modelingnicotinic acetylcholine receptorsradioligand analysisα-conotoxin analogs

Identifiers

PMID22072993
PMCPMC3210602
OpenAlexW1997901145

What OpenQuestion holds

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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.