Evidence map›Paper›PMID 36856089›Full record

ArticleeLife2023

Conserved allosteric inhibition mechanism in SLC1 transporters.

Yang Dong, Jiali Wang, Rachel-Ann Garibsingh, Keino Hutchinson, Yueyue Shi, Gilad Eisenberg, Xiaozhen Yu, Avner Schlessinger, Christof Grewer

Open access · goldFull text read
In one paragraph

Article in eLife, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing papers in PubMed
2.9field-weighted citation impact, top 10% 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

9 citing papers in PubMed, 16 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Review
  5. Article
  6. Comprehensive Characterization of LAT1 Cholesterol-Binding Sites.Journal of chemical theory and computation · 2024
    Article
  7. Review
  8. Article
  9. 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

9 authors at 2 institutions in 1 country.

Yang DongDepartment of Chemistry, Binghamton University, Binghamton, United States.
Jiali WangDepartment of Chemistry, Binghamton University, Binghamton, United States.ORCID 0000-0002-9520-8140
Rachel-Ann GaribsinghDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, United States.
Keino HutchinsonDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, United States.
Yueyue ShiDepartment of Chemistry, Binghamton University, Binghamton, United States.
Gilad EisenbergDepartment of Chemistry, Binghamton University, Binghamton, United States.
Xiaozhen YuDepartment of Chemistry, Binghamton University, Binghamton, United States.
Avner SchlessingerDepartment of Pharmacological Sciences, Icahn School of Medicine at Mount Sinai, New York, United States.ORCID 0000-0003-4007-7814
Christof GrewerDepartment of Chemistry, Binghamton University, Binghamton, United States.ORCID 0000-0002-8342-9878
Binghamton University · USIcahn School of Medicine at Mount Sinai · US

Funding

TRAINING PROGRAM IN CANCER THERAPYT32CA078207 · NCI · MOUNT SINAI SCHOOL OF MEDICINE OF NYU · PI James J Manfredi · 1999 to 2026
$11.6M
Substrate Specificity Determinants in Nutrient Solute Carrier TransportersR01GM108911 · NIGMS · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI SCHLESSINGER, AVNER · 2014 to 2022
$3.1M
Substrate Specificity Determinants in Nutrient Solute Carrier TransportersR01CA277794 · NCI · ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI · PI Avner Schlessinger · 2023 to 2026
$1.7M
How to Combat Glutamate Release by Reverse Transport: Mechanistic Studies and Development of Selective Efflux InhibitorsR15GM135843 · NIGMS · STATE UNIVERSITY OF NY,BINGHAMTON · PI GREWER, CHRISTOF THEODOR · 2019 to 2019
$450k
NCI NIH HHS R01 CA277794NIGMS NIH HHS R01 GM108911NIGMS NIH HHS R15 GM135843NIH HHS R01 GM108911NIH HHS R15 GM135843-01NIH HHS T32 CA078207
6 · The paper itself

Abstract

Excitatory amino acid transporter 1 (EAAT1) is a glutamate transporter belonging to the SLC1 family of solute carriers. It plays a key role in the regulation of the extracellular glutamate concentration in the mammalian brain. The structure of EAAT1 was determined in complex with UCPH-101, apotent, non-competitive inhibitor of EAAT1. Alanine serine cysteine transporter 2 (ASCT2) is a neutral amino acid transporter, which regulates pools of amino acids such as glutamine between intracellular and extracellular compartments . ASCT2 also belongs to the SLC1 family and shares 58% sequence similarity with EAAT1. However, allosteric modulation of ASCT2 via non-competitive inhibitors is unknown. Here, we explore the UCPH-101 inhibitory mechanisms of EAAT1 and ASCT2 by using rapid kinetic experiments. Our results show that UCPH-101 slows substrate translocation rather than substrate or Na

Indexed as

Amino AcidsGlutamineAlanineAnimalsBinding SitesExcitatory Amino Acid Transporter 1Glutamic AcidMammalsMinor Histocompatibility AntigensSerineAlanineAmino AcidsExcitatory Amino Acid Transporter 1Glutamic AcidGlutamineMinor Histocompatibility AntigensSerinealanine serine cysteine transporterdockingelectrophysiologyglutamate transporterhumaninhibitionmolecular biophysicsratSLC1structural biology

Identifiers

PMID36856089
PMCPMC10017108
OpenAlexW4322719488

What OpenQuestion holds

Textfull text, public
LicenceCC BY
measurements read58
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.