Evidence map›Paper›PMID 27539678›Full record

ReviewExpert opinion on therapeutic patents2016

Sphingosine kinase inhibitors: a review of patent literature (2006-2015).

Kevin R Lynch, S Brandon Thorpe, Webster L Santos

Open access · greenAbstract readReview
In one paragraph

Review in Expert opinion on therapeutic patents, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.

0numbers the graph read from it
0cells of the map it votes in
20citing papers in PubMed
1.7field-weighted citation impact, top 15% 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

20 citing papers in PubMed, 27 citations in OpenAlex.

  1. Review
  2. Article
  3. Regulation of cellular and systemic sphingolipid homeostasis.Nature reviews. Molecular cell biology · 2024
    Review
  4. Review
  5. Article
  6. Review
  7. Article
  8. Roles of long non‑coding RNA in osteoarthritis (Review).International journal of molecular medicine · 2021
    Review
  9. Review
  10. Review
  11. Article
  12. Article
  13. Review
  14. Review
  15. Review
  16. A Phase I Study of ABC294640, a First-in-Class Sphingosine Kinase-2 Inhibitor, in Patients with Advanced Solid Tumors.Clinical cancer research : an official journal of the American Association for Cancer Research · 2017
    Article
  17. Article
  18. Review
  19. Article
  20. 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

3 authors at 3 institutions in 1 country.

Kevin R Lyncha Department of Pharmacology , University of Virginia , Charlottesville , VA , USA.
S Brandon Thorpeb SphynKx Therapeutics, LLC ., Charlottesville , VA , USA.
Webster L Santosc Department of Chemistry and Virginia Tech Center for Drug Discovery , Virginia Tech , Blacksburg , VA , USA.
Adenosine Therapeutics (United States) · USUniversity of Virginia · USVirginia Tech · US

Funding

Molecular Pharmacology of Sphingosine 1-PhosphateR01GM067958 · NIGMS · UNIVERSITY OF VIRGINIA CHARLOTTESVILLE · PI LYNCH, KEVIN R. · 2004 to 2014
$3.7M
In Vivo Probes of Sphingosine Kinase FunctionR01GM104366 · NIGMS · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI LYNCH, KEVIN R., SANTOS, WEBSTER L · 2013 to 2015
$1.1M
NIGMS NIH HHS R01 GM067958NIGMS NIH HHS R01 GM104366
6 · The paper itself

Abstract

introductionSphingosine kinase (SphK1 & SphK2) is the sole source of the pleiotropic lipid mediator, sphingosine-1-phosphate (S1P). S1P has been implicated in a variety of diseases such as cancer, Alzheimer's disease, sickle cell disease and fibrosis and thus the biosynthetic route to S1P is a logical target for drug discovery. Areas covered: In this review, the authors consider the SphK inhibitor patent literature from 2006-2016 Q1 with the emphasis on composition of matter utility patents. The Espacenet database was queried with the search term 'sphingosine AND kinase' to identify relevant literature. Expert opinion: Early inhibitor discovery focused on SphK1 with a bias towards oncology indications. Structurally, the reported inhibitors occupy the sphingosine 'J-shaped' binding pocket. The lack of cytotoxicity with improved SphK1 inhibitors raises doubt about the enzyme as an oncology target. SphK2 inhibitors are featured in more recent patent applications. Interestingly, both SphK1 and SphK2 inhibition and gene 'knockout' share opposing effects on circulating S1P levels: SphK1 inhibition/gene ablation decreases, while SphK2 inhibition/gene ablation increases, blood S1P. As understanding of S1P's physiological roles increases and more drug-like SphK inhibitors emerge, inhibiting one or both SphK isotypes could provide unique strategies for treating disease.

Indexed as

Drug DesignAnimalsAntineoplastic AgentsEnzyme InhibitorsHumansNeoplasmsPatents as TopicPhosphotransferases (Alcohol Group Acceptor)Sphingosine KinaseAntineoplastic AgentsEnzyme InhibitorsPhosphotransferases (Alcohol Group Acceptor)Sphingosine Kinasesphingosine kinase 2, humancancer therapeuticskinase inhibitorsphingosine-1-phosphateSphingosine kinasesphingosine kinase 1sphingosine kinase 2

Identifiers

PMID27539678
PMCPMC5773104
OpenAlexW2513686248

What OpenQuestion holds

Textmetadata
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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.