Evidence map›Paper›PMID 33290061›Full record

ArticleJournal of medicinal chemistry2020

Design, Synthesis, and Biological Evaluation of a Series of Oxazolone Carboxamides as a Novel Class of Acid Ceramidase Inhibitors.

Samantha Caputo, Simona Di Martino, Vincenzo Cilibrasi, Piero Tardia, Marco Mazzonna, Debora Russo, Ilaria Penna, Maria Summa, Sine Mandrup Bertozzi, Natalia Realini and 10 more

Open access · hybridAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing papers in PubMed
1.1field-weighted citation impact, top 23% 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

7 citing papers in PubMed, 21 citations in OpenAlex.

  1. Article
  2. Beware ofMolecules (Basel, Switzerland) · 2024
    Article
  3. Review
  4. Regulation of cellular and systemic sphingolipid homeostasis.Nature reviews. Molecular cell biology · 2024
    Review
  5. Article
  6. Article
  7. 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

20 authors at 2 institutions in 2 countries.

Samantha CaputoFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Simona Di MartinoFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.ORCID 0000-0001-5817-751X
Vincenzo CilibrasiFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Piero TardiaFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Marco MazzonnaFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Debora RussoFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Ilaria PennaFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Maria SummaFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Sine Mandrup BertozziFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Natalia RealiniFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Natasha MargaroliFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Marco MiglioreFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Giuliana OttonelloFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Min LiuLysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Peter LansburyLysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Andrea ArmirottiFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.ORCID 0000-0002-3766-8755
Rosalia BertorelliFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.
Soumya S RayLysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Renato SkerljLysosomal Therapeutics Inc., 19 Blackstone Street, Cambridge, Massachusetts 02139, United States.
Rita ScarpelliFondazione Istituto Italiano di Tecnologia, Via Morego 30, I-16163 Genova, Italy.ORCID 0000-0002-2623-306X
Italian Institute of Technology · ITBlackstone (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Acid ceramidase (AC) is a cysteine hydrolase that plays a crucial role in the metabolism of lysosomal ceramides, important members of the sphingolipid family, a diversified class of bioactive molecules that mediate many biological processes ranging from cell structural integrity, signaling, and cell proliferation to cell death. In the effort to expand the structural diversity of the existing collection of AC inhibitors, a novel class of substituted oxazol-2-one-3-carboxamides were designed and synthesized. Herein, we present the chemical optimization of our initial hits, 2-oxo-4-phenyl-

Indexed as

Drug DesignAcid CeramidaseAdministration, OralAnimalsBinding SitesCell Line, TumorEnzyme InhibitorsHalf-LifeHumansInhibitory Concentration 50KineticsMaleMiceMice, Inbred C57BLMicrosomesMolecular Docking SimulationAcid CeramidaseEnzyme InhibitorsOxazolone

Identifiers

PMID33290061
PMCPMC7770833
OpenAlexW3111080083

What OpenQuestion holds

Textmetadata
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.