Evidence map›Paper›PMID 33062178›Full record

ArticleACS medicinal chemistry letters2020

Mechanism-Based Design of 3-Amino-4-Halocyclopentenecarboxylic Acids as Inactivators of GABA Aminotransferase.

Sida Shen, Peter F Doubleday, Pathum M Weerawarna, Wei Zhu, Neil L Kelleher, Richard B Silverman

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing papers in PubMed
0.5field-weighted citation impact, top 38% 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

10 citing papers in PubMed, 11 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Synthesis of (2The Journal of organic chemistry · 2024
    Article
  5. Information-Rich, Dual-FunctionJournal of the American Chemical Society · 2023
    Article
  6. Article
  7. Rational Design, Synthesis, and Mechanism of (3Journal of the American Chemical Society · 2022
    Article
  8. Turnover and Inactivation Mechanisms for (Journal of the American Chemical Society · 2021
    Article
  9. Remarkable and Unexpected Mechanism for (Journal of the American Chemical Society · 2021
    Article
  10. 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 at 1 institution in 1 country.

Sida ShenDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Peter F DoubledayDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Pathum M WeerawarnaDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Wei ZhuDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Neil L KelleherDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Richard B SilvermanDepartment of Chemistry, Chemistry of Life Processes Institute, Center for Molecular Innovation and Drug Discovery, and Center for Developmental Therapeutics and Department of Molecular Biosciences, Northwestern University, Evanston, Illinois 60208, United States.
Northwestern University · US

Funding

The UIUC Neuroproteomics Center on Cell-Cell SignalingP30DA018310 · NIDA · UNIVERSITY OF ILLINOIS URBANA-CHAMPAIGN · PI Elena V Romanova · 2004 to 2026
$24.9M
New Inactivators of GABA Aminotransferase for Addiction and EpilepsyR01DA030604 · NIDA · NORTHWESTERN UNIVERSITY · PI SILVERMAN, RICHARD B · 2011 to 2020
$4.0M
NIDA NIH HHS P30 DA018310NIDA NIH HHS R01 DA030604
6 · The paper itself

Abstract

Aminotransferases are pyridoxal 5'-phosphate-dependent enzymes that catalyze reversible transamination reactions between an amino acid and an α-keto acid, playing a critical role in cellular nitrogen metabolism. It is evident that γ-aminobutyric acid aminotransferase (GABA-AT), which balances the levels of inhibitory and excitatory neurotransmitters, has emerged as a promising therapeutic target for epilepsy and cocaine addiction based on mechanism-based inactivators (MBIs). In this work, we established an integrated approach using computational simulation, organic synthesis, biochemical evaluation, and mass spectrometry to facilitate our design and mechanistic studies of MBIs, which led to the identification of a new cyclopentene-based analogue (

Identifiers

PMID33062178
PMCPMC7549257
OpenAlexW3007341318

What OpenQuestion holds

Textmetadata
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.