Evidence map›Paper›PMID 34807584›Full record

ArticleJournal of medicinal chemistry2022

Inhibitors of the Hippo Pathway Kinases STK3/MST2 and STK4/MST1 Have Utility for the Treatment of Acute Myeloid Leukemia.

Nicole Bata, Apirat Chaikuad, Nicole A Bakas, Allison S Limpert, Lester J Lambert, Douglas J Sheffler, Lena M Berger, Guoxiong Liu, Cunxiang Yuan, Li Wang and 6 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
2.8field-weighted citation impact, top 9% 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

14 citing papers in PubMed, 33 citations in OpenAlex.

  1. Article
  2. Review
  3. Article
  4. Article
  5. Article
  6. Article
  7. Review
  8. Article
  9. Review
  10. Article
  11. Review
  12. Review
  13. Review
  14. 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

16 authors at 3 institutions in 3 countries.

Nicole BataCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.
Apirat ChaikuadBuchmann Institute for Molecular Life Sciences, Structural Genomics Consortium, Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany.ORCID 0000-0003-1120-2209
Nicole A BakasCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.ORCID 0000-0002-9413-205X
Allison S LimpertCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.
Lester J LambertCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.ORCID 0000-0002-6274-1811
Douglas J ShefflerCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.
Lena M BergerBuchmann Institute for Molecular Life Sciences, Structural Genomics Consortium, Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany.ORCID 0000-0002-7835-8067
Guoxiong LiuChemistry Department, Viva Biotech Ltd., 581 Shen Kuo Road, Shanghai 201203, China.
Cunxiang YuanChemistry Department, Viva Biotech Ltd., 581 Shen Kuo Road, Shanghai 201203, China.
Li WangChemistry Department, Viva Biotech Ltd., 581 Shen Kuo Road, Shanghai 201203, China.
Yi PengChemistry Department, Viva Biotech Ltd., 581 Shen Kuo Road, Shanghai 201203, China.
Jing DongChemistry Department, Viva Biotech Ltd., 581 Shen Kuo Road, Shanghai 201203, China.
Maria CeleridadCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.
Fabiana LayngCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.
Stefan KnappBuchmann Institute for Molecular Life Sciences, Structural Genomics Consortium, Johann Wolfgang Goethe-University, D-60438 Frankfurt am Main, Germany.
Nicholas D P CosfordCell and Molecular Biology of Cancer Program, NCI-Designated Cancer Center, Sanford Burnham Prebys Medical Discovery Institute, 10901 North Torrey Pines Road, La Jolla, California 92037, United States.ORCID 0000-0001-7228-4709
Sanford Burnham Prebys Medical Discovery Institute · USViva Biotech (China) · CNGoethe University Frankfurt · DE

Funding

Tumor Microenvironment and Cancer ImmunologyP30CA030199 · NCI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI ELENA B PASQUALE · 1985 to 2026
$107.2M
Cancer Targets and Drug DiscoveryT32CA211036 · NCI · SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE · PI COSFORD, NICHOLAS DAVID · 2018 to 2022
$1.2M
NCI NIH HHS P30 CA030199NCI NIH HHS T32 CA211036Wellcome Trust
6 · The paper itself

Abstract

Serine/threonine-protein kinases 3 and 4 (STK3 and STK4, respectively) are key components of the Hippo signaling pathway, which regulates cell proliferation and death and provides a potential therapeutic target for acute myeloid leukemia (AML). Herein, we report the structure-based design of a series of pyrrolopyrimidine derivatives as STK3 and STK4 inhibitors. In an initial screen, the compounds exhibited low nanomolar potency against both STK3 and STK4. Crystallization of compound

Indexed as

AnimalsFemaleHippo KinasesHippo Signaling PathwayHumansIntracellular Signaling Peptides and ProteinsLeukemia, Myeloid, AcuteMiceMice, Inbred C57BLProtein Kinase InhibitorsProtein Serine-Threonine KinasesSerine-Threonine Kinase 3Hippo KinasesIntracellular Signaling Peptides and ProteinsProtein Kinase InhibitorsProtein Serine-Threonine KinasesSerine-Threonine Kinase 3STK3 protein, humanSTK4 protein, human

Identifiers

PMID34807584
PMCPMC10149138
OpenAlexW3215431779

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.