Evidence map›Paper›PMID 26588064›Full record

ArticleEuropean journal of medicinal chemistry2016

New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.

Ivan B Yanachkov, Hung Chang, Milka I Yanachkova, Edward J Dix, Michelle A Berny-Lang, Thomas Gremmel, Alan D Michelson, George E Wright, Andrew L Frelinger

Open access · greenAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
3.6field-weighted citation impact, top 7% 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

18 citing papers in PubMed, 42 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Review
  5. Review
  6. Article
  7. P2YPurinergic signalling · 2022
    Article
  8. Microglia and Neuroinflammation: What Place for P2RY12?International journal of molecular sciences · 2021
    Review
  9. Review
  10. Update of P2Y receptor pharmacology: IUPHAR Review 27.British journal of pharmacology · 2020
    Review
  11. MiR-34b-3p Represses the Multidrug-Chemoresistance of Bladder Cancer Cells by Regulating the CCND2 and P2RY1 Genes.Medical science monitor : international medical journal of experimental and clinical research · 2019
    Article
  12. Article
  13. GLS-409, an Antagonist of Both P2YScientific reports · 2018
    Article
  14. Article
  15. Novel aspects of antiplatelet therapy in cardiovascular disease.Research and practice in thrombosis and haemostasis · 2018
    Review
  16. Platelet Signaling Pathways and New Inhibitors.Arteriosclerosis, thrombosis, and vascular biology · 2018
    Review
  17. Article
  18. Review
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

9 authors at 3 institutions in 2 countries.

Ivan B YanachkovGLSynthesis, Inc. Worcester, MA, USA. Electronic address: ivan.yanachkov@glsynthesis.com.
Hung ChangCenter for Platelet Function Studies, Department of Pediatrics, University of Massachusetts Medical School, Worcester, MA, USA; Hematology Division, Chang Gung Memorial Hospital, Chang Gung University, Taipei, Taiwan.
Milka I YanachkovaGLSynthesis, Inc. Worcester, MA, USA.
Edward J DixGLSynthesis, Inc. Worcester, MA, USA.
Michelle A Berny-LangCenter for Platelet Research Studies, Division of Hematology/Oncology, Boston Children's Hospital, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.
Thomas GremmelCenter for Platelet Research Studies, Division of Hematology/Oncology, Boston Children's Hospital, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA.
Alan D MichelsonCenter for Platelet Research Studies, Division of Hematology/Oncology, Boston Children's Hospital, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA; Center for Platelet Function Studies, Department of Pediatrics, University of Massachusetts Medical School, Worcester, MA, USA.
George E WrightGLSynthesis, Inc. Worcester, MA, USA.
Andrew L FrelingerCenter for Platelet Research Studies, Division of Hematology/Oncology, Boston Children's Hospital, Dana-Farber Cancer Institute, Harvard Medical School, Boston, MA, USA; Center for Platelet Function Studies, Department of Pediatrics, University of Massachusetts Medical School, Worcester, MA, USA.
Boston Children's Hospital · USGlsynthesis · USUniversity of Massachusetts Chan Medical School · US

Funding

Novel Antithrombotic Diadenosine Tetraphosphate AnalogsR44TR000983 · NCATS · GLSYNTHESIS, INC. · PI YANACHKOV, IVAN B · 2013 to 2015
$3.4M
Novel Antithrombotic Diadenosine Tetraphosphate AnalogsR44HL088828 · NHLBI · GLSYNTHESIS, INC. · PI YANACHKOV, IVAN B · 2009 to 2010
$1.5M
Novel Antithrombotic Diadenosine Tetraphosphate AnalogsR43HL088828 · NHLBI · GLSYNTHESIS, INC. · PI YANACHKOV, IVAN B · 2007 to 2007
$333k
NCATS NIH HHS R44 TR000983NHLBI NIH HHS HL088828NHLBI NIH HHS R43 HL088828NHLBI NIH HHS R44 HL088828
6 · The paper itself

Abstract

Currently approved platelet adenosine diphosphate (ADP) receptor antagonists target only the platelet P2Y12 receptor. Moreover, especially in patients with acute coronary syndromes, there is a strong need for rapidly acting and reversible antiplatelet agents in order to minimize the risk of thrombotic events and bleeding complications. In this study, a series of new P(1),P(4)-di(adenosine-5') tetraphosphate (Ap4A) derivatives with modifications in the base and in the tetraphosphate chain were synthesized and evaluated with respect to their effects on platelet aggregation and function of the platelet P2Y1, P2Y12, and P2X1 receptors. The resulting structure-activity relationships were used to design Ap4A analogs which inhibit human platelet aggregation by simultaneously antagonizing both P2Y1 and P2Y12 platelet receptors. Unlike Ap4A, the analogs do not activate platelet P2X1 receptors. Furthermore, the new compounds exhibit fast onset and offset of action and are significantly more stable than Ap4A to degradation in plasma, thus presenting a new promising class of antiplatelet agents.

Indexed as

AnimalsChemistry Techniques, SyntheticDinucleoside PhosphatesDrug Evaluation, PreclinicalDrug StabilityHumansPlatelet Aggregation InhibitorsPurinergic P2X Receptor AntagonistsPurinergic P2Y Receptor AntagonistsRatsReceptors, Purinergic P2X1Receptors, Purinergic P2Y1Receptors, Purinergic P2Y12Structure-Activity Relationshipdiadenosine tetraphosphateDinucleoside PhosphatesP2RY12 protein, humanPlatelet Aggregation InhibitorsPurinergic P2X Receptor AntagonistsPurinergic P2Y Receptor AntagonistsReceptors, Purinergic P2X1Receptors, Purinergic P2Y1Receptors, Purinergic P2Y12Acute coronary syndromesAdenosine diphosphateAntiplatelet therapyAntithromboticsBis-nucleoside polyphosphatesCardiovascular diseaseDinucleoside polyphosphatesInhibitorsP2X1P2Y(1)P2Y(12)Platelets

Identifiers

PMID26588064
PMCPMC4674339
OpenAlexW2208948204

What Socratic holds

Textmetadata
LicenceTDM
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.