ArticleEuropean journal of medicinal chemistry2024
Exploration of the tunability of BRD4 degradation by DCAF16 trans-labelling covalent glues.
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Article in European journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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22citing papers in PubMed
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Who cites it
22 citing papers in PubMed.
- Dual E3 ligase recruitment by monovalent degraders for tunable SMARCA 2/4 degradation.Nature chemical biology · 2026Article
- A tail of two ligases.Nature chemical biology · 2026Article
- Ubiquitin family as novel protein partners for molecular glues.npj drug discovery · 2026Review
- BromoCatch: a self-labelling tag platform for protein modification and live cell imaging.Nature communications · 2026Article
- An Optimized RNF126-Targeting Covalent Handle for Molecular Glue Degraders.bioRxiv : the preprint server for biology · 2026Article
- Sub-stoichiometric Degradation is Dispensable for Potent PROTACs: A Case Study for Irreversible Covalent BTK Degraders.bioRxiv : the preprint server for biology · 2026Article
- From Serendipity to Strategy: Rationalizing Molecular Glue Discovery and Proximity-Induced Pharmacology through Chemical Biology.Journal of the American Chemical Society · 2026Review
- Discovery of Non-Degradative Covalent Molecular Glues for Transcriptional Reprogramming.bioRxiv : the preprint server for biology · 2025Article
- Mode of action of a DCAF16-recruiting targeted glue that can selectively degrade BRD9.Nature communications · 2025Article
- DCAF16-Based Covalent Degradative Handles for the Modular Design of Degraders.ACS central science · 2025Article
- Targeted protein degradation for cancer therapy.Nature reviews. Cancer · 2025Review
- Linker-free PROTACs efficiently induce the degradation of oncoproteins.Nature communications · 2025Article
- Delineating cysteine-reactive compound modulation of cellular proteostasis processes.Nature chemical biology · 2025Article
- Implications of frequent hitter E3 ligases in targeted protein degradation screens.Nature chemical biology · 2025Review
- Discovery of DCAF16 Binders for Targeted Protein Degradation.ACS chemical biology · 2025Article
- Covalent Proximity Inducers.Chemical reviews · 2025Review
- DCAF16-Based Covalent Handle for the Rational Design of Monovalent Degraders.ACS central science · 2024Article
- Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation.Nature communications · 2024Article
- Applications of protein ubiquitylation and deubiquitylation in drug discovery.The Journal of biological chemistry · 2024Review
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Authors and funding
19 authors.
Muhammad Murtaza HassanDepartment of Chemical and Systems Biology, ChEM-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA; SPARK Translational Research Program, Stanford University School of Medicine, Stanford, CA, USA.
Yen-Der LiDepartment of Molecular and Cellular Biology, Harvard University, Cambridge, MA, USA; Department of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA, USA.
Michelle W MaDepartment of Molecular and Cellular Biology, Harvard University, Cambridge, MA, USA; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Mingxing TengCenter for Drug Discovery, Department of Pathology & Immunology, and Verna and Marrs McLean Department of Biochemistry and Molecular Pharmacology, Baylor College of Medicine, Houston, TX, USA.
Woong Sub ByunDepartment of Chemical and Systems Biology, ChEM-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA.
Kedar PuvarDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Ryan LumpkinDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Brittany SandovalDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA.
Justine C RutterDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA, USA.
Cyrus Y JinDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Michelle Y WangDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.
Shawn XuDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA.
Anna M SchmokerDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Hakyung CheongDepartment of Molecular and Cellular Biology, Harvard University, Cambridge, MA, USA; Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA.
Brian J GroendykeDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.
Jun QiDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA.
Eric S FischerDepartment of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA, USA. Electronic address: eric_fischer@dfci.harvard.edu.
Benjamin L EbertDepartment of Medical Oncology, Dana-Farber Cancer Institute, Boston, MA, USA; Cancer Program, Broad Institute of MIT and Harvard, Cambridge, MA, USA; Howard Hughes Medical Institute, Boston, MA, USA. Electronic address: benjamin_ebert@dfci.harvard.edu.
Nathanael S GrayDepartment of Chemical and Systems Biology, ChEM-H and Stanford Cancer Institute, Stanford School of Medicine, Stanford University, Stanford, CA, USA. Electronic address: nsgray01@stanford.edu.
Funding
TYROSINE KINASE ONCOGENESIS IN MYELOID LEUKEMIAP01CA066996 · NCI · DANA-FARBER CANCER INSTITUTE · PI SCOTT A ARMSTRONG · 1996 to 2026
$52.5MMedical Scientist Training ProgramT32GM144273 · NIGMS · HARVARD MEDICAL SCHOOL · PI David Shumway Jones, Jacqueline A. Lees · 2022 to 2026
$14.7MTargeting SYK Kinase in AMLP50CA206963 · NCI · DANA-FARBER CANCER INST · PI STEGMAIER, KIMBERLY · 2017 to 2021
$10.6MFunctional Genomic Dissection of Refractory AnemiaR01HL082945 · NHLBI · DANA-FARBER CANCER INSTITUTE · PI EBERT, BENJAMIN LEVINE · 2005 to 2022
$6.8MThe role of clonal hematopoiesis in the development and therapy of myeloid malignanciesR35CA253125 · NCI · DANA-FARBER CANCER INST · PI EBERT, BENJAMIN LEVINE · 2020 to 2024
$4.9MCancer Chemical Biology and Metabolism Training ProgramT32CA236754 · NCI · DANA-FARBER CANCER INST · PI Nika N Danial, THOMAS M ROBERTS · 2019 to 2026
$2.6MDevelopment of a generalizable chemo-proteomics screening platform for small molecule degraders applied to HDACsR01CA262188 · NCI · DANA-FARBER CANCER INST · PI FISCHER, ERIC SEBASTIAN · 2022 to 2025
$1.8M500 MHz NMR Spectrometer System with High Sensitivity Cryoprobe and Automated Sample Changer for Biochemical ResearchS10OD028697 · OD · STANFORD UNIVERSITY · PI BURNS, NOAH ZACHARY · 2020 to 2020
$709kNCI NIH HHS P01 CA066996NCI NIH HHS P50 CA206963NCI NIH HHS R01 CA262188NCI NIH HHS R35 CA253125NCI NIH HHS T32 CA236754NHLBI NIH HHS R01 HL082945NIGMS NIH HHS T32 GM144273NIH HHS S10 OD028697
Abstract
Chemically induced proximity modalities such as targeted protein degradation (TPD) hold promise for expanding the number of proteins that can be manipulated pharmacologically. However, current TPD strategies are often limited to proteins with preexisting ligands. Molecular glues (e.g. glutarimide ligands for CUL4
Indexed as
Cell Cycle ProteinsTranscription FactorsAzepinesBromodomain Containing ProteinsDose-Response Relationship, DrugHumansMolecular StructureProteolysisStructure-Activity RelationshipTriazolesAzepinesBRD4 protein, humanBromodomain Containing ProteinsCell Cycle Proteins(+)-JQ1 compoundTranscription FactorsTriazoles
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