Evidence map›Paper›PMID 27689866›Full record

ArticleJournal of the American Chemical Society2016

Chemical Proteomic Profiling of Human Methyltransferases.

Benjamin D Horning, Radu M Suciu, Darian A Ghadiri, Olesya A Ulanovskaya, Megan L Matthews, Kenneth M Lum, Keriann M Backus, Steven J Brown, Hugh Rosen, Benjamin F Cravatt

Abstract read
In one paragraph

Article in Journal of the American Chemical Society, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.

0numbers the graph read from it
0cells of the map it votes in
49citing papers in PubMed
6.1field-weighted citation impact, top 3% 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

49 citing papers in PubMed, 96 citations in OpenAlex.

  1. Article
  2. Article
  3. Efficacious Anti-Cancer Drugs Targeting NicotinamidePharmaceuticals (Basel, Switzerland) · 2026
    Article
  4. Article
  5. Review
  6. Phenomics-Based Discovery of Novel Orthosteric Choline Kinase Inhibitors.Angewandte Chemie (International ed. in English) · 2025
    Article
  7. Review
  8. Review
  9. Article
  10. Review
  11. Article
  12. Article
  13. Review
  14. Article
  15. Article
  16. Review
  17. Functionalised Cofactor Mimics for Interactome Discovery and Beyond.Angewandte Chemie (International ed. in English) · 2022
    Review
  18. Article
  19. Review
  20. 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

10 authors at 1 institution in 1 country.

Benjamin D HorningDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Radu M SuciuDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Darian A GhadiriDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Olesya A UlanovskayaDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Megan L MatthewsDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Kenneth M LumDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Keriann M BackusDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Steven J BrownDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Hugh RosenDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Benjamin F CravattDepartments of Chemical Physiology, The Scripps Research Institute , La Jolla, California 92307, United States.
Scripps Research Institute · US

Funding

Chemical Probes for Metabolic Pathway Discovery in Human DiseaseR01CA132630 · NCI · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F · 2007 to 2018
$5.1M
Chemoproteomic methods to profile and inhibit methyltransferasesF32CA186587 · NCI · SCRIPPS RESEARCH INSTITUTE, THE · PI HORNING, BENJAMIN · 2014 to 2015
$109k
NCI NIH HHS F32 CA186587NCI NIH HHS R01 CA132630
6 · The paper itself

Abstract

Methylation is a fundamental mechanism used in Nature to modify the structure and function of biomolecules, including proteins, DNA, RNA, and metabolites. Methyl groups are predominantly installed into biomolecules by a large and diverse class of S-adenosyl methionine (SAM)-dependent methyltransferases (MTs), of which there are ∼200 known or putative members in the human proteome. Deregulated MT activity contributes to numerous diseases, including cancer, and several MT inhibitors are in clinical development. Nonetheless, a large fraction of the human MT family remains poorly characterized, underscoring the need for new technologies to characterize MTs and their inhibitors in native biological systems. Here, we describe a suite of S-adenosyl homocysteine (SAH) photoreactive probes and their application in chemical proteomic experiments to profile and enrich a large number of MTs (>50) from human cancer cell lysates with remarkable specificity over other classes of proteins. We further demonstrate that the SAH probes can enrich MT-associated proteins and be used to screen for and assess the selectivity of MT inhibitors, leading to the discovery of a covalent inhibitor of nicotinamide N-methyltransferase (NNMT), an enzyme implicated in cancer and metabolic disorders. The chemical proteomics probes and methods for their utilization reported herein should prove of value for the functional characterization of MTs, MT complexes, and MT inhibitors in mammalian biology and disease.

Indexed as

ProteomicsCell Line, TumorEnzyme ActivationHumansMethyltransferasesMolecular ProbesS-AdenosylhomocysteineUltraviolet RaysMethyltransferasesMolecular ProbesS-Adenosylhomocysteine

Identifiers

PMID27689866
PMCPMC5072128
OpenAlexW2526407243

What OpenQuestion holds

Textmetadata
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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.