Evidence map›Paper›PMID 31810327›Full record

ArticleMolecules (Basel, Switzerland)2019

Synthesis and Biological Evaluation of BODIPY-PF-543.

Jitendra Shrestha, Gil Tae Hwang, Taeho Lee, Seon Woong Kim, Yoon Sin Oh, Yongseok Kwon, Seung Woo Hong, Sanghee Kim, Hong Seop Moon, Dong Jae Baek and 1 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Targeting the Sphingolipid Rheostat in Gliomas.International journal of molecular sciences · 2022
    Review
  3. Article
  4. Article
  5. 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

11 authors at 4 institutions in 1 country.

Jitendra ShresthaCollege of Pharmacy, Mokpo National University, Jeonnam 58554, Korea.
Gil Tae HwangDepartment of Chemistry, Kyungpook National University, Daegu 41566, Korea.ORCID 0000-0001-7107-9244
Taeho LeeCollege of Pharmacy, Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea.
Seon Woong KimCollege of Pharmacy, Mokpo National University, Jeonnam 58554, Korea.
Yoon Sin OhDepartment of Food and Nutrition, Eulji University, Seongnam 13135, Korea.ORCID 0000-0003-3995-4429
Yongseok KwonDepartment of Chemistry, Sogang University, Seoul 04107, Korea.
Seung Woo HongDepartment of Chemistry, Kyungpook National University, Daegu 41566, Korea.
Sanghee KimCollege of Pharmacy, Seoul National University, Seoul 08826, Korea.ORCID 0000-0001-9125-9541
Hong Seop MoonCollege of Pharmacy, Mokpo National University, Jeonnam 58554, Korea.
Dong Jae BaekCollege of Pharmacy, Mokpo National University, Jeonnam 58554, Korea.ORCID 0000-0001-6100-488X
Eun-Young ParkCollege of Pharmacy, Mokpo National University, Jeonnam 58554, Korea.
Mokpo National University · KRKyungpook National University · KREulji University · KRSogang University · KR

Funding

This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning 2018R1C1B6001892 and 2017R1D1A1B03032529
6 · The paper itself

Abstract

Sphingosine-1-phosphate (S1P) regulates the proliferation of various cells and promotes the growth of cancer cells. Sphingosine kinase (SK), which transforms sphingosine into S1P, has two isotypes: SK1 and SK2. To date, both isotypes are known to be involved in the proliferation of cancer cells. PF-543, an SK1 inhibitor developed by Pfizer, strongly inhibits SK1. However, despite its strong SK1 inhibitory effect, PF-543 shows low anticancer activity in vitro. Therefore, additional biological evidence on the anticancer activity of SK1 inhibitor is required. The present study aimed to investigate the intracellular localization of PF-543 and identify its association with anticancer activity by introducing a fluoroprobe into PF-543. Boron-dipyrromethene (BODIPY)-introduced PF-543 has a similar SK1 inhibitory effect as PF-543. These results indicate that the introduction of BODIPY does not significantly affect the inhibitory effect of SK1. In confocal microscopy after BODIPY-PF-543 treatment, the compound was mainly located in the cytosol of the cells. This study demonstrated the possibility of introducing fluorescent material into an SK inhibitor and designing a synthesized compound that is permeable to cells while maintaining the SK inhibitory effect.

Indexed as

Chemistry Techniques, SyntheticBoron CompoundsEnzyme InhibitorsMethanolMolecular StructurePhosphotransferases (Alcohol Group Acceptor)PyrrolidinesSpectrum AnalysisSphingosine KinaseStructure-Activity RelationshipSulfones4,4-difluoro-4-bora-3a,4a-diaza-s-indaceneBoron CompoundsEnzyme InhibitorsMethanolPF-543Phosphotransferases (Alcohol Group Acceptor)PyrrolidinesSphingosine KinaseSulfonesBODIPYconfocal microscopyinhibitorPF-543sphingosine kinase

Identifiers

PMID31810327
PMCPMC6930633
OpenAlexW2989696383

What OpenQuestion 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 OpenQuestion graph.