Evidence map›Paper›PMID 33915015›Full record

ArticleAngewandte Chemie (International ed. in English)2021

Discovery of a Potent Degrader for Fibroblast Growth Factor Receptor 1/2.

Guangyan Du, Jie Jiang, Qibiao Wu, Nathaniel J Henning, Katherine A Donovan, Hong Yue, Jianwei Che, Wenchao Lu, Eric S Fischer, Nabeel Bardeesy and 2 more

Open access · greenAbstract read
In one paragraph

Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.

0numbers the graph read from it
0cells of the map it votes in
22citing papers in PubMed
3.2field-weighted citation impact, top 7% 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

22 citing papers in PubMed, 55 citations in OpenAlex.

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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

12 authors at 3 institutions in 1 country.

Guangyan DuDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Jie JiangDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Qibiao WuCancer Center, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA.
Nathaniel J HenningDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Katherine A DonovanDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Hong YueDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Jianwei CheDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Wenchao LuDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Eric S FischerDepartment of Cancer Biology, Dana Farber Cancer Institute, 360 Longwood Ave, Boston, MA, 02215, USA.
Nabeel BardeesyCancer Center, Massachusetts General Hospital, Harvard Medical School, Boston, MA, USA.
Tinghu ZhangDepartment of Chemical and Systems Biology, Chem-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA.
Nathanael S GrayDepartment of Chemical and Systems Biology, Chem-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA.ORCID 0000-0001-5354-7403
Harvard University · USBroad Institute · USStanford University · US

Funding

Tissue and Pathology ResourcesP50CA127003 · NCI · DANA-FARBER CANCER INST · PI BASS, ADAM JOEL · 2007 to 2023
$33.2M
ATP-Dependent Chromatin Remodeling in Human MalignancyR01CA163915 · NCI · STANFORD UNIVERSITY · PI Gerald R. Crabtree · 2012 to 2026
$5.4M
Degrading therapeutically important kinases using small moleculesR01CA218278 · NCI · STANFORD UNIVERSITY · PI Eric Sebastian Fischer, NATHANAEL Schiander GRAY · 2019 to 2026
$4.6M
HIJACKING CANCER DRIVERS TO ACTIVATE PROAPOPTOTIC GENES IN DLBCLR01CA276167 · NCI · STANFORD UNIVERSITY · PI Gerald R. Crabtree, NATHANAEL Schiander GRAY · 2023 to 2026
$2.2M
NCI NIH HHS P50 CA127003NCI NIH HHS R01 CA163915NCI NIH HHS R01 CA218278NCI NIH HHS R01 CA276167NIH HHS NIH 5 R01 CA218278-02NIH HHS NIH P50 CA127003
6 · The paper itself

Abstract

Aberrant activation of FGFR signaling occurs in many cancers, and ATP-competitive FGFR inhibitors have received regulatory approval. Despite demonstrating clinical efficacy, these inhibitors exhibit dose-limiting toxicity, potentially due to a lack of selectivity amongst the FGFR family and are poorly tolerated. Here, we report the discovery and characterization of DGY-09-192, a bivalent degrader that couples the pan-FGFR inhibitor BGJ398 to a CRL2

Indexed as

Receptor, Fibroblast Growth Factor, Type 1Receptor, Fibroblast Growth Factor, Type 2AnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationDrug DiscoveryHumansMicePhenylurea CompoundsProtein Kinase InhibitorsPyrimidinesAntineoplastic AgentsFGFR1 protein, humanFGFR2 protein, humaninfigratinibPhenylurea CompoundsProtein Kinase InhibitorsPyrimidinesReceptor, Fibroblast Growth Factor, Type 1Receptor, Fibroblast Growth Factor, Type 2cholangiocarcinomadegraderFGFR1FGFR2protein degradation

Identifiers

PMID33915015
PMCPMC8324087
OpenAlexW3157161277

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.