Synthesis and Inhibitory Studies of Phosphonic Acid Analogues of Homophenylalanine and Phenylalanine towards Alanyl Aminopeptidases.

Weronika Wanat, Michał Talma, Błażej Dziuk, Paweł Kafarski

Open access · goldAbstract read

In one paragraph

Article in Biomolecules, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

0numbers the graph read from it

0cells of the map it votes in

0citing papers in PubMed

0.1field-weighted citation impact, top 54% 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

0 citing papers in PubMed, 4 citations in OpenAlex.

No citing paper in PubMed yet.

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

4 authors at 1 institution in 1 country.

Weronika WanatDepartment of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.ORCID 0000-0002-8633-6335

Michał TalmaDepartment of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.ORCID 0000-0001-8902-097X

Błażej DziukFaculty of Chemistry, University of Opole, Oleska 48, 45-052 Opole, Poland.

Paweł KafarskiDepartment of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.ORCID 0000-0001-8019-4797

Wrocław University of Science and Technology · PL

Funding

National Science Center of Poland 017/26/M/ST5/00437

6 · The paper itself

Abstract

A library of novel phosphonic acid analogues of homophenylalanine and phenylalanine, containing fluorine and bromine atoms in the phenyl ring, have been synthesized. Their inhibitory properties against two important alanine aminopeptidases, of human (hAPN, CD13) and porcine (pAPN) origin, were evaluated. Enzymatic studies and comparison with literature data indicated the higher inhibitory potential of the homophenylalanine over phenylalanine derivatives towards both enzymes. Their inhibition constants were in the submicromolar range for hAPN and the micromolar range for pAPN, with 1-amino-3-(3-fluorophenyl) propylphosphonic acid (compound

Indexed as

AminobutyratesAnimalsBinding SitesBromineCD13 AntigensEnzyme InhibitorsFluorineHumansIsoenzymesKineticsModels, MolecularPhenylalaninePhosphorous AcidsProtein BindingProtein Conformation, alpha-HelicalProtein Conformation, beta-Strand2-amino-4-phenylbutyric acidAminobutyratesBromineCD13 AntigensEnzyme InhibitorsFluorineIsoenzymesPhenylalaninephosphonic acidPhosphorous AcidsSmall Molecule Librariescomputer-aided simulationsfluorine and bromine substitutionhuman and porcine alanine aminopeptidasephosphonic acid inhibitors

Identifiers

PMID32938014

DOI10.3390/biom10091319

PMCPMC7565091

OpenAlexW3085585497

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.