Evidence map›Paper›PMID 33435264›Full record

ArticleMolecules (Basel, Switzerland)2021

In Search for Multi-Target Ligands as Potential Agents for Diabetes Mellitus and Its Complications-A Structure-Activity Relationship Study on Inhibitors of Aldose Reductase and Protein Tyrosine Phosphatase 1B.

Rosaria Ottanà, Paolo Paoli, Mario Cappiello, Trung Ngoc Nguyen, Ilenia Adornato, Antonella Del Corso, Massimo Genovese, Ilaria Nesi, Roberta Moschini, Alexandra Naß and 2 more

Open access · goldAbstract read
In one paragraph

Article in Molecules (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
2.2field-weighted citation impact, top 13% 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

11 citing papers in PubMed, 27 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Article
  5. A pre-clinical study to investigate the anti-diabetic potential ofJournal of diabetes and metabolic disorders · 2023
    Article
  6. Review
  7. Article
  8. Article
  9. Article
  10. Article
  11. Dual-Target Compounds against Type 2Pharmaceuticals (Basel, Switzerland) · 2021
    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

12 authors at 4 institutions in 2 countries.

Rosaria OttanàDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.ORCID 0000-0002-5950-3230
Paolo PaoliDepartment of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.ORCID 0000-0001-6448-7266
Mario CappielloDepartment of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.ORCID 0000-0002-8864-5043
Trung Ngoc NguyenMolecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Ilenia AdornatoDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.
Antonella Del CorsoDepartment of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.ORCID 0000-0003-3165-6128
Massimo GenoveseDepartment of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.ORCID 0000-0002-3732-3124
Ilaria NesiDepartment of Scienze Biomediche Sperimentali e Cliniche, Sezione di Scienze Biochimiche, University of Firenze, Viale Morgagni 50, 50134 Firenze, Italy.ORCID 0000-0002-8060-2700
Roberta MoschiniDepartment of Biology, Biochemistry Unit, University of Pisa, Via S. Zeno, 51, 56123 Pisa, Italy.ORCID 0000-0001-5227-2348
Alexandra NaßMolecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Gerhard WolberMolecular Design Lab, Institute of Pharmacy, Freie Universität Berlin, Königin-Luisestr. 2 + 4, 14195 Berlin, Germany.
Rosanna MaccariDepartment of Chemical, Biological, Pharmaceutical and Environmental Sciences, University of Messina, Viale Palatucci, Polo Universitario Annunziata, 98168 Messina, Italy.ORCID 0000-0001-7561-737X
Freie Universität Berlin · DEUniversity of Florence · ITUniversity of Messina · ITUniversity of Pisa · IT

Funding

Università degli Studi di Messina FFABR_ATENEO_PA_2019
6 · The paper itself

Abstract

Diabetes mellitus (DM) is a complex disease which currently affects more than 460 million people and is one of the leading cause of death worldwide. Its development implies numerous metabolic dysfunctions and the onset of hyperglycaemia-induced chronic complications. Multiple ligands can be rationally designed for the treatment of multifactorial diseases, such as DM, with the precise aim of simultaneously controlling multiple pathogenic mechanisms related to the disease and providing a more effective and safer therapeutic treatment compared to combinations of selective drugs. Starting from our previous findings that highlighted the possibility to target both aldose reductase (AR) and protein tyrosine phosphatase 1B (PTP1B), two enzymes strictly implicated in the development of DM and its complications, we synthesised 3-(5-arylidene-4-oxothiazolidin-3-yl)propanoic acids and analogous 2-butenoic acid derivatives, with the aim of balancing the effectiveness of dual AR/PTP1B inhibitors which we had identified as designed multiple ligands (DMLs). Out of the tested compounds,

Indexed as

Enzyme InhibitorsHypoglycemic AgentsAldehyde ReductaseAnimalsDiabetes MellitusDrug Evaluation, PreclinicalHep G2 CellsHumansLigandsMiceProtein Tyrosine Phosphatase, Non-Receptor Type 1Structure-Activity RelationshipAldehyde ReductaseEnzyme InhibitorsHypoglycemic AgentsLigandsProtein Tyrosine Phosphatase, Non-Receptor Type 1PTPN1 protein, human4-thiazolidinonesaldose reductasediabetes mellitusmolecular dockingmulti-target ligandsprotein tyrosine phosphatase 1B

Identifiers

PMID33435264
PMCPMC7828111
OpenAlexW3118933001

What Socratic 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 Socratic graph.