Evidence map›Paper›PMID 30390553›Full record

ArticleBioorganic chemistry2019

Synthesis and evaluation of an AZD2461 [

Sean W Reilly, Laura N Puentes, Alexander Schmitz, Chia-Ju Hsieh, Chi-Chang Weng, Catherine Hou, Shihong Li, Yin-Ming Kuo, Prashanth Padakanti, Hsiaoju Lee and 3 more

Abstract read
In one paragraph

Article in Bioorganic chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
0.5field-weighted citation impact, top 31% 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

12 citing papers in PubMed, 22 citations in OpenAlex.

  1. Review
  2. [Journal of clinical medicine · 2024
    Review
  3. PET imaging of PARP expression usingEuropean journal of nuclear medicine and molecular imaging · 2023
    Article
  4. Article
  5. Design and synthesis of benzodiazepines as brain penetrating PARP-1 inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2022
    Article
  6. Review
  7. Review
  8. Review
  9. Review
  10. Novel Tracers and Radionuclides in PET Imaging.Radiologic clinics of North America · 2021
    Review
  11. [Molecular imaging and biology · 2020
    Article
  12. 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

13 authors at 1 institution in 1 country.

Sean W ReillyDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Laura N PuentesDepartment of Systems Pharmacology and Translational Therapeutics, University of Pennsylvania, 421 Curie Boulevard, Philadelphia, PA 19104, USA.
Alexander SchmitzDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Chia-Ju HsiehDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Chi-Chang WengDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Catherine HouDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Shihong LiDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Yin-Ming KuoDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Prashanth PadakantiDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Hsiaoju LeeDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Aladdin A RiadDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA.
Mehran MakvandiDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA. Electronic address: makvandi@pennmedicine.upenn.edu.
Robert H MachDepartment of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA. Electronic address: rmach@mail.med.upenn.edu.
University of Pennsylvania · US

Funding

PREDOCTORAL TRAINING PROGRAM IN PHARMACOLOGYT32GM008076 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI BLENDY, JULIE A · 1985 to 2023
$10.8M
T32 Translational Addiction Research Fellowship ProgramT32DA028874 · NIDA · UNIVERSITY OF PENNSYLVANIA · PI Julie A Blendy, Anna Rose Childress · 2010 to 2026
$5.0M
NEUROBIOLOGY OF COCAINE-INDUCED BEHVRL SENSITIZATIONF32DA005589 · NIDA · WASHINGTON STATE UNIVERSITY · PI PIERCE, ROBERT CHRISTOPHER · 1993 to 1995
–
NIDA NIH HHS F32 DA005589NIDA NIH HHS T32 DA028874NIGMS NIH HHS T32 GM008076
6 · The paper itself

Abstract

Poly(ADP-ribose)polymerase-1 inhibitor (PARPi) AZD2461 was designed to be a weak P-glycoprotein (P-gp) analogue of FDA approved olaparib. With this chemical property in mind, we utilized the AZD2461 ligand architecture to develop a CNS penetrant and PARP-1 selective imaging probe, in order to investigate PARP-1 mediated neuroinflammation and neurodegenerative diseases, such as Alzheimer's and Parkinson's. Our work led to the identification of several high-affinity PARPi, including AZD2461 congener 9e (PARP-1 IC

Indexed as

AnimalsATP Binding Cassette Transporter, Subfamily B, Member 1Blood-Brain BarrierCell Line, TumorFluorine RadioisotopesHumansMacaca mulattaMaleMice, Inbred BALB CPhthalazinesPiperidinesPoly (ADP-Ribose) Polymerase-1ATP Binding Cassette Transporter, Subfamily B, Member 1AZD2461Fluorine RadioisotopesPARP1 protein, humanPhthalazinesPiperidinesPoly (ADP-Ribose) Polymerase-1AZD2461Blood-brain barrierMicroPET imagingPARP-1 inhibitorP-glycoprotein

Identifiers

PMID30390553
PMCPMC6378121
OpenAlexW2896801746

What OpenQuestion 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 OpenQuestion graph.