Evidence map›Paper›PMID 36297668›Full record

ArticlePharmaceutics2022

Optimization of a Novel Mandelamide-Derived Pyrrolopyrimidine Series of PERK Inhibitors.

Michael E Stokes, Matthew D Surman, Veronica Calvo, David Surguladze, An-Hu Li, Jennifer Gasparek, Matthew Betzenhauser, Guangyu Zhu, Hongwen Du, Alan C Rigby and 1 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.9field-weighted citation impact, top 30% 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

5 citing papers in PubMed, 8 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. A PERK-Specific Inhibitor Blocks Metastatic Progression by Limiting Integrated Stress Response-Dependent Survival of Quiescent Cancer Cells.Clinical cancer research : an official journal of the American Association for Cancer Research · 2023
    Article
  5. PERK Inhibition by HC-5404 Sensitizes Renal Cell Carcinoma Tumor Models to Antiangiogenic Tyrosine Kinase Inhibitors.Clinical cancer research : an official journal of the American Association for Cancer Research · 2023
    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

11 authors at 1 institution in 1 country.

Michael E StokesHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
Matthew D SurmanCuria, 26 Corporate Circle, Albany, NY 12203, USA.
Veronica CalvoHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
David SurguladzeHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
An-Hu LiHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
Jennifer GasparekCuria, 1001 Main Street, Buffalo, NY 14203, USA.
Matthew BetzenhauserCuria, 1001 Main Street, Buffalo, NY 14203, USA.
Guangyu ZhuCuria, 1001 Main Street, Buffalo, NY 14203, USA.ORCID 0000-0003-4228-135X
Hongwen DuPharmaron Beijing Co., Ltd., No. 6, TaiHe Road, BDA, Beijing 100176, China.
Alan C RigbyHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
Mark J MulvihillHiberCell Inc., 619 West 54th Street, New York, NY 10019, USA.
FuelCell Energy (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) is one of three endoplasmic reticulum (ER) transmembrane sensors of the unfolded protein response (UPR) responsible for regulating protein synthesis and alleviating ER stress. PERK has been implicated in tumorigenesis, cancer cell survival as well metabolic diseases such as diabetes. The structure-based design and optimization of a novel mandelamide-derived pyrrolopyrimidine series of PERK inhibitors as described herein, resulted in the identification of compound

Indexed as

cancerdiabetesER stressinhibitorkinasePERKsmall moleculestructure–activity-relationship (SAR)UPR

Identifiers

PMID36297668
PMCPMC9611727
OpenAlexW4306835700

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.