Evidence map›Paper›PMID 27774134›Full record

ArticleACS medicinal chemistry letters2016

Discovery of 8-Membered Ring Sulfonamides as Inhibitors of Oncogenic Mutant Isocitrate Dehydrogenase 1.

Jason M Law, Sebastian C Stark, Ke Liu, Norah E Liang, Mahmud M Hussain, Matthias Leiendecker, Daisuke Ito, Oscar Verho, Andrew M Stern, Stephen E Johnston and 4 more

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing 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

11 citing papers in PubMed.

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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

14 authors.

Jason M LawCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States.
Sebastian C StarkCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Ke LiuCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Norah E LiangCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States.
Mahmud M HussainCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States; Howard Hughes Medical Institute, Cambridge, Massachusetts 02138, United States.
Matthias LeiendeckerCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States.
Daisuke ItoCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Oscar VerhoCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States.
Andrew M SternCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Stephen E JohnstonCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Yan-Ling ZhangCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Gavin P DunnDepartment of Neurological Surgery, Washington Univeristy School of Medicine , St. Louis, Missouri 63110, United States.
Alykhan F ShamjiCenter for the Science of Therapeutics, Broad Institute , Cambridge, Massachusetts 02142, United States.
Stuart L SchreiberCenter for the Science of Therapeutics, Broad Institute, Cambridge, Massachusetts 02142, United States; Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, United States; Howard Hughes Medical Institute, Cambridge, Massachusetts 02138, United States.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Evidence suggests that specific mutations of isocitrate dehydrogenases 1 and 2 (IDH1/2) are critical for the initiation and maintenance of certain tumor types and that inhibiting these mutant enzymes with small molecules may be therapeutically beneficial. In order to discover mutant allele-selective IDH1 inhibitors with chemical features distinct from existing probes, we screened a collection of small molecules derived from diversity-oriented synthesis. The assay identified compounds that inhibit the IDH1-R132H mutant allele commonly found in glioma. Here, we report the discovery of a potent (IC

Indexed as

2-hydroxyglutarateallele-selective probeAMLBRD2879cancerdiversity-oriented synthesisgliomahigh-throughput screeningisocitrate dehydrogenasesmall-molecule probe

Identifiers

PMID27774134
PMCPMC5066158

What OpenQuestion holds

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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.