Evidence map›Paper›PMID 31223445›Full record

ArticleACS medicinal chemistry letters2019

Computer-Aided Selective Optimization of Side Activities of Talinolol.

Kerstin Hiesinger, Jan S Kramer, Janosch Achenbach, Daniel Moser, Julia Weber, Sandra K Wittmann, Christophe Morisseau, Carlo Angioni, Gerd Geisslinger, Astrid S Kahnt and 7 more

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
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

4 citing papers in PubMed, 5 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. 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

17 authors at 1 institution in 1 country.

Kerstin HiesingerInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Jan S KramerInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Janosch AchenbachInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Daniel MoserInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Julia WeberInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Sandra K WittmannInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Christophe MorisseauDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center, University of California Davis, One Shields Avenue, Davis, California 95616, United States.
Carlo AngioniInstitute of Clinical Pharmacology, Pharmazentrum Frankfurt, ZAFES, Theodor-Stern-Kai 7, D-60590 Frankfurt am Main, Germany.
Gerd GeisslingerInstitute of Clinical Pharmacology, Pharmazentrum Frankfurt, ZAFES, Theodor-Stern-Kai 7, D-60590 Frankfurt am Main, Germany.
Astrid S KahntInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Astrid KaiserInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Anna ProschakInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Dieter SteinhilberInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Denys PogoryelovInstitute of Biochemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Karen WagnerDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center, University of California Davis, One Shields Avenue, Davis, California 95616, United States.
Bruce D HammockDepartment of Entomology and Nematology and UC Davis Comprehensive Cancer Center, University of California Davis, One Shields Avenue, Davis, California 95616, United States.
Ewgenij ProschakInstitute of Pharmaceutical Chemistry, Goethe-University of Frankfurt, Max-von-Laue Strasse 9, D-60438 Frankfurt am Main, Germany.
Goethe University Frankfurt · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Selective optimization of side activities is a valuable source of novel lead structures in drug discovery. In this study, a computer-aided approach was used to deorphanize the pleiotropic cholesterol-lowering effects of the beta-blocker talinolol, which result from the inhibition of the enzyme soluble epoxide hydrolase (sEH). X-ray structure analysis of the sEH in complex with talinolol enables a straightforward optimization of inhibitory potency. The resulting lead structure exhibited

Identifiers

PMID31223445
PMCPMC6580380
OpenAlexW2946984863

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.