Evidence map›Paper›PMID 31547058›Full record

ArticleMolecules (Basel, Switzerland)2019

Benzoxaboroles-Novel Autotaxin Inhibitors.

Kristina Kraljić, Dubravko Jelić, Dinko Žiher, Adam Cvrtila, Snježana Dragojević, Verona Sinković, Milan Mesić

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 8 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed, 1 pooled it
0.9field-weighted citation impact, top 27% 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

8 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.

  1. Pooled it
  2. Article
  3. Article
  4. Article
  5. Review
  6. Design and Development of Autotaxin Inhibitors.Pharmaceuticals (Basel, Switzerland) · 2021
    Review
  7. Emerging drug delivery strategies for idiopathic pulmonary fibrosis treatment.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2021
    Review
  8. 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

7 authors at 1 institution in 1 country.

Kristina KraljićFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. kristina.kraljic@glpg.com.
Dubravko JelićFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. dubravko.jelic@glpg.com.
Dinko ŽiherFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. dinko.ziher@glpg.com.
Adam CvrtilaFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. adam.cvrtila@glpg.com.
Snježana DragojevićFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. snjezana.dragojevic@glpg.com.
Verona SinkovićFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. verona.sinkovic@glpg.com.
Milan MesićFidelta Ltd., Prilaz baruna Filipovića 29, 10000 Zagreb, Croatia. milan.mesic@glpg.com.
Pliva (Croatia) · HR

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Autotaxin (ATX) is an extracellular enzyme that hydrolyses lysophosphatidylcholine (LPC) to lysophosphatidic acid (LPA), which has a role in the mediation of inflammation, fibrosis and cancer. ATX is a drug target that has been the focus of many research groups during the last ten years. To date, only one molecule, Ziritaxestat (GLPG1690) has entered the clinic; it is currently in Phase 3 clinical trials for idiopathic pulmonary fibrosis. Other small molecules, with different binding modes, have been investigated as ATX inhibitors for cancer including compounds possessing a boronic acid motif such as HA155. In this work, we targeted new, improved inhibitors of ATX that mimic the important interactions of boronic acid using a benzoxaborole motif as the acidic warhead. Furthermore, we aimed to improve the plasma stability of the new compounds by using a more stable core spacer than that embedded in HA155. Compounds were synthesized, evaluated for their ATX inhibitory activity and ADME properties in vitro, culminating in a new benzoxaborole compound, 37, which retains the ATX inhibition activity of HA155 but has improved ADME properties (plasma protein binding, good kinetic solubility and rat/human plasma stability).

Indexed as

AnimalsHumansLysophosphatidylcholinesLysophospholipase DLysophospholipidsNeoplasmsPhosphoric Diester HydrolasesRatsStructure-Activity Relationshiplysophosphatidic acidLysophosphatidylcholinesLysophospholipase DLysophospholipidsPhosphoric Diester HydrolasesAutotaxin (ATX)benzoxaborolescancerlysophosphaditic acid

Identifiers

PMID31547058
PMCPMC6804080
OpenAlexW2973405239

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.