Evidence map›Paper›PMID 36680947›Full record

ArticleBioorganic & medicinal chemistry2023

Development of fluorophore labeled or biotinylated anticancer small molecule NSC243928.

Rahul Prakash, Dustin W Goodlett, Sheelu Varghese, Justyna Andrys, Fahidat A Gbadamosi, Ricardo H Arriaza, Megha Patel, Purushottam B Tiwari, Tomasz Borowski, Maksymilian Chruszcz and 2 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it
0cells of the map it votes in
0citing papers in PubMed
0.3field-weighted citation impact, top 50% 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

0 citing papers in PubMed, 2 citations in OpenAlex.

No citing paper in PubMed yet.

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 at 4 institutions in 2 countries.

Rahul PrakashDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Dustin W GoodlettDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Sheelu VargheseHenry M. Jackson Foundation, Bethesda, MD, USA; Department of Pathology, Uniformed Services University, Bethesda, MD, USA.
Justyna AndrysJerzy Haber Institute of Catalysis and Surface Chemistry, Polish Academy of Science, Niezapominajek 8, Krakow 30-239, Poland.
Fahidat A GbadamosiDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Ricardo H ArriazaDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Megha PatelDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Purushottam B TiwariDepartment of Oncology, Georgetown University Medical Center, Washington, DC, USA.
Tomasz BorowskiJerzy Haber Institute of Catalysis and Surface Chemistry, Polish Academy of Science, Niezapominajek 8, Krakow 30-239, Poland.
Maksymilian ChruszczDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Linda S ShimizuDepartment of Chemistry and Biochemistry, University of South Carolina, Columbia, SC 29208, USA.
Geeta UpadhyayJohn P. Murtha Cancer Center, Bethesda, MD, USA; Department of Pathology, Uniformed Services University, Bethesda, MD, USA; Department of Oncology, Georgetown University Medical Center, Washington, DC, USA. Electronic address: geeta.upadhyay@usuhs.edu.
University of South Carolina · USGeorgetown University Medical Center · USJerzy Haber Institute of Catalysis and Surface Chemistry, Polish Academy of Sciences · PLHenry M. Jackson Foundation · US

Funding

Tissue Culture Shared ResourceP30CA051008 · NCI · GEORGETOWN UNIVERSITY · PI Louis M Weiner · 1990 to 2026
$71.5M
Role of Ly6K in TGF-beta and immune escape pathways of triple negative breast cancerR01CA227694 · NCI · HENRY M. JACKSON FDN FOR THE ADV MIL/MED · PI Geeta Upadhyay · 2018 to 2026
$2.4M
Use of Ly6K specific CAR T-cells to treat primary and metastatic triple negative breast cancerR21CA256424 · NCI · HENRY M. JACKSON FDN FOR THE ADV MIL/MED · PI UPADHYAY, GEETA · 2021 to 2022
$389k
NCI NIH HHS P30 CA051008NCI NIH HHS R01 CA227694NCI NIH HHS R21 CA256424
6 · The paper itself

Abstract

Small molecule NSC243928 binds with LY6K, a potential target for the treatment of triple-negative breast cancer, and induces cancer cell death with an unclear mechanism. We have developed chemical tools to identify the molecular mechanisms of NSC243928-LY6K interaction. Herein, we report on the development and synthesis of biotinylated and fluorophore-tethered derivatives of NSC243928 guided by docking studies and molecular dynamics. Surface plasmon resonance assay indicates that these derivatives retained a direct binding with LY6K protein. Confocal analysis revealed that nitrobenzoxadiazole (NBD) fluorophore tagged NSC243928 is retained in LY6K expressing cancer cells. These novel modified compounds will be employed in future in vitro and in vivo studies to understand the molecular mechanisms of NSC243928 mediated cancer cell death. These studies will pave the path for developing novel targeted therapeutics and understanding any potential side-effects of these treatments for hard-to-treat cancers such as triple-negative breast cancer or other cancers with high expression of LY6K.

Indexed as

Triple Negative Breast NeoplasmsAcridinesCell Line, TumorHumansSulfonamidesAcridinesNSC243928SulfonamidesLY6KNSC243928Triple negative breast cancer

Identifiers

PMID36680947
PMCPMC9892358
OpenAlexW4315977465

What OpenQuestion holds

Textmetadata
LicenceTDM
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.