Evidence map›Paper›PMID 39425769›Full record

ArticleACS chemical neuroscience2024

Rational Search for Betaine/GABA Transporter 1 Inhibitors─

Kamil Łątka, Stefanie Kickinger, Zuzanna Rzepka, Paula Zaręba, Gniewomir Latacz, Agata Siwek, Małgorzata Wolak, Dorota Stary, Monika Marcinkowska, Petrine Wellendorph and 2 more

Abstract read
In one paragraph

Article in ACS chemical neuroscience, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. 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

12 authors.

Kamil ŁątkaDepartment of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Stefanie KickingerDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.
Zuzanna RzepkaDepartment of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, Poland.
Paula ZarębaDepartment of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.ORCID 0000-0002-5037-6183
Gniewomir LataczDepartment of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Agata SiwekDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Małgorzata WolakDepartment of Pharmacobiology, Faculty of Pharmacy, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Dorota StaryDepartment of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.
Monika MarcinkowskaDepartment of Medicinal Chemistry, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.ORCID 0000-0002-4948-6617
Petrine WellendorphDepartment of Drug Design and Pharmacology, Faculty of Health and Medical Sciences, University of Copenhagen, 2100 Copenhagen, Denmark.ORCID 0000-0002-5455-8013
Dorota WrześniokDepartment of Pharmaceutical Chemistry, Faculty of Pharmaceutical Sciences in Sosnowiec, Medical University of Silesia, Jagiellońska 4, 41-200 Sosnowiec, Poland.
Marek BajdaDepartment of Physicochemical Drug Analysis, Jagiellonian University Medical College, Medyczna 9, 30-688 Kraków, Poland.ORCID 0000-0001-6032-0354

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Inhibitory neurotransmission mediated by γ-aminobutyric acid (GABA) plays an important role in maintaining body homeostasis. Disturbances in GABA signaling are implicated in a multitude of neurologic and psychiatric conditions, including epilepsy, ischemia, anxiety, depression, insomnia, and mood disorders. Clinically relevant increases in GABA neurotransmitter level can be achieved by inhibition of its uptake into presynaptic neurons and surrounding glial cells, driven by GABA transporters (GAT1, BGT1, GAT2, and GAT3). Herein, we focused on the search for inhibitors of the BGT1 transporter which is understudied and for which the therapeutic potential of its inhibition is partly unknown. We applied multilevel virtual screening to identify compounds with inhibitory properties. Among selected hits, compound

Indexed as

GABA Plasma Membrane Transport ProteinsAstrocytesGABA Uptake InhibitorsHEK293 CellsHumansbetaine plasma membrane transport proteinsGABA Plasma Membrane Transport ProteinsGABA Uptake InhibitorsSLC6A1 protein, humanbetaine/GABA transporter 1biological evaluationinhibitorrigid GABA analoguevirtual screening

Identifiers

PMID39425769
PMCPMC11587516

What Socratic 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 Socratic graph.