Evidence map›Paper›PMID 36719862›Full record

ArticleJournal of medicinal chemistry2023

Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening.

Ram K Modukuri, Diana Monsivais, Feng Li, Murugesan Palaniappan, Kurt M Bohren, Zhi Tan, Angela F Ku, Yong Wang, Chandrashekhar Madasu, Jian-Yuan Li and 5 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
–field-weighted citation impact
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

16 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. Article
  5. Review
  6. Discovery of highly potent and ALK2/ALK1 selective kinase inhibitors using DNA-encoded chemistry technology.Proceedings of the National Academy of Sciences of the United States of America · 2024
    Article
  7. Review
  8. Article
  9. Identification of potent pan-ephrin receptor kinase inhibitors using DNA-encoded chemistry technology.Proceedings of the National Academy of Sciences of the United States of America · 2024
    Article
  10. Review
  11. Article
  12. Review
  13. Article
  14. Article
  15. Article
  16. 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

15 authors.

Ram K ModukuriCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.ORCID 0000-0002-5849-4088
Diana MonsivaisCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Feng LiCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Murugesan PalaniappanCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Kurt M BohrenCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Zhi TanCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Angela F KuCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Yong WangCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Chandrashekhar MadasuCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Jian-Yuan LiCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Suni TangCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Gabriella MiklossyCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Stephen S PalmerCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Damian W YoungCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.
Martin M MatzukCenter for Drug Discovery, Department of Pathology & Immunology, Baylor College of Medicine, Houston, Texas77030, United States.ORCID 0000-0002-1445-8632

Funding

Transforming growth factor β family signaling pathways in ovarian and uterine biologyR01HD032067 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI MARTIN M. MATZUK · 1994 to 2026
$9.9M
Kinases as Therapeutic Targets for EndometriosisR01HD110038 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI MARTIN M. MATZUK · 2022 to 2026
$3.4M
Targeting the endometrial stem cell niche inendometriosisR01HD105800 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI Diana Monsivais · 2022 to 2026
$2.5M
Mechanisms of Liver Toxicity of Anit-Depressant DuloxetineR01DK121970 · NIDDK · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2020 to 2023
$1.8M
Elucidating Chemical Features that Block or Facilitate Passage across the Blood-Testis and/or Blood-Epidydimal Barriers in MiceR33HD099995 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2022 to 2024
$1.7M
Elucidating Chemical Features that Block or Facilitate Passage across the Blood-Testis and/or Blood-Epidydimal Barriers in MiceR61HD099995 · NICHD · BAYLOR COLLEGE OF MEDICINE · PI LI, FENG · 2020 to 2021
$862k
Development of a Precision Drug to target Y537S Mutant Estrogen Receptor in Metastatic Breast CancerR03CA259664 · NCI · BAYLOR COLLEGE OF MEDICINE · PI PALANIAPPAN, MURUGESAN · 2022 to 2023
$160k
NCI NIH HHS R03 CA259664NICHD NIH HHS R01 HD032067NICHD NIH HHS R01 HD105800NICHD NIH HHS R01 HD110038NICHD NIH HHS R33 HD099995NICHD NIH HHS R61 HD099995NIDDK NIH HHS R01 DK121970
6 · The paper itself

Abstract

The discovery of monokinase-selective inhibitors for patients is challenging because the 500+ kinases encoded by the human genome share highly conserved catalytic domains. Until now, no selective inhibitors unique for a single transforming growth factor β (TGFβ) family transmembrane receptor kinase, including bone morphogenetic protein receptor type 2 (BMPR2), have been reported. This dearth of receptor-specific kinase inhibitors hinders therapeutic options for skeletal defects and cancer as a result of an overactivated BMP signaling pathway. By screening 4.17 billion "unbiased" and "kinase-biased" DNA-encoded chemical library molecules, we identified hits

Indexed as

DNASignal TransductionBone Morphogenetic Protein Receptors, Type IIGene LibraryHumansBMPR2 protein, humanBone Morphogenetic Protein Receptors, Type IIDNA

Identifiers

PMID36719862
PMCPMC9924264

What OpenQuestion holds

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Registered trials

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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.