Evidence map›Paper›PMID 34143170›Full record

ReviewChemical Society reviews2021

Chemoproteomic methods for covalent drug discovery.

Wai Cheung Chan, Shabnam Sharifzadeh, Sara J Buhrlage, Jarrod A Marto

Abstract readReview
In one paragraph

Review in Chemical Society reviews, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 29 papers.

0numbers the graph read from it
0cells of the map it votes in
29citing 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

29 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
  4. Article
  5. Article
  6. Review
  7. Review
  8. Article
  9. Article
  10. Article
  11. Review
  12. Target Engagement Assays in Early Drug Discovery.Journal of medicinal chemistry · 2025
    Review
  13. Chemoproteomic Profiling ofJournal of medicinal chemistry · 2025
    Article
  14. Article
  15. Article
  16. Review
  17. Chemoproteomic Profiling ofbioRxiv : the preprint server for biology · 2025
    Article
  18. Review
  19. Article
  20. 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

4 authors.

Wai Cheung ChanDepartment of Cancer Biology and the Linde Program in Cancer Chemical Biology, Dana-Farber Cancer Institute, Boston, MA, USA. SaraJ_Buhrlage@dfci.harvard.edu jarrod_marto@dfci.harvard.edu and Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.ORCID http://orcid.org/0000-0001-8413-5401
Shabnam SharifzadehDepartment of Cancer Biology and the Linde Program in Cancer Chemical Biology, Dana-Farber Cancer Institute, Boston, MA, USA. SaraJ_Buhrlage@dfci.harvard.edu jarrod_marto@dfci.harvard.edu and Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA.
Sara J BuhrlageDepartment of Cancer Biology and the Linde Program in Cancer Chemical Biology, Dana-Farber Cancer Institute, Boston, MA, USA. SaraJ_Buhrlage@dfci.harvard.edu jarrod_marto@dfci.harvard.edu and Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Jarrod A MartoDepartment of Cancer Biology and the Linde Program in Cancer Chemical Biology, Dana-Farber Cancer Institute, Boston, MA, USA. SaraJ_Buhrlage@dfci.harvard.edu jarrod_marto@dfci.harvard.edu and Department of Pathology, Brigham and Women's Hospital and Harvard Medical School, Boston, MA, USA and Blais Proteomics Center, Dana-Farber Cancer Institute, Boston, MA, USA.ORCID http://orcid.org/0000-0003-2086-1134

Funding

Novel Screening Platform for Discovery of DUB Targeting ProbesR01CA233800 · NCI · DANA-FARBER CANCER INST · PI BUHRLAGE, SARA J, MARTO, JARROD A. · 2019 to 2022
$2.5M
Tools for DUB Drug DiscoveryR21CA247671 · NCI · DANA-FARBER CANCER INST · PI BUHRLAGE, SARA J, MARTO, JARROD A. · 2020 to 2021
$648k
Tools for the understudied kinase PNK3R03CA250020 · NCI · DANA-FARBER CANCER INST · PI MARTO, JARROD A. · 2019 to 2019
$178k
NCI NIH HHS R01 CA233800NCI NIH HHS R03 CA250020NCI NIH HHS R21 CA247671
6 · The paper itself

Abstract

Covalent drugs constitute cornerstones of modern medicine. The past decade has witnessed growing enthusiasm for development of covalent inhibitors, fueled by clinical successes as well as advances in analytical techniques associated with the drug discovery pipeline. Among these, mass spectrometry-based chemoproteomic methods stand out due to their broad applicability from focused analysis of electrophile-containing compounds to surveying proteome-wide inhibitor targets. Here, we review applications of both foundational and cutting-edge chemoproteomic techniques across target identification, hit discovery, and lead characterization/optimization in covalent drug discovery. We focus on the practical aspects necessary for the general drug discovery scientist to design, interpret, and evaluate chemoproteomic experiments. We also present three case studies on clinical stage molecules to further showcase the real world significance and future opportunities of these methodologies.

Indexed as

Mass SpectrometryProteomicsDrug DesignDrug DiscoveryHumansProteomeProteome

Identifiers

PMID34143170
PMCPMC8328943

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.