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Synonyms: OMP-52M51 | OMP52M51
Compound class: Antibody
Comment: Brontictuzumab (OMP-52M51) is a fully human anti-NOTCH1 monoclonal antibody [4-5]. It was developed by OncoMed Pharmaceuticals. Peptide sequence analysis reveals that the heavy and light chains that make up brontictuzumab are claimed in Oncomed patent US20140011271A1 . The heavy chain is SEQ ID NO:22 (52M51-H4), and the light chain is SEQ ID NO:26 (2M51L3), making the brontictuzumab structure 52M51H4L3.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Ferrarotto R, Eckhardt G, Patnaik A, LoRusso P, Faoro L, Heymach JV, Kapoun AM, Xu L, Munster P. (2018)
A phase I dose-escalation and dose-expansion study of brontictuzumab in subjects with selected solid tumors.
Ann Oncol, 29 (7): 1561-1568. [PMID:29726923]
2. Ferrarotto R, Mitani Y, Diao L, Guijarro I, Wang J, Zweidler-McKay P, Bell D, William Jr WN, Glisson BS, Wick MJ et al.. (2017)
Activating NOTCH1 Mutations Define a Distinct Subgroup of Patients With Adenoid Cystic Carcinoma Who Have Poor Prognosis, Propensity to Bone and Liver Metastasis, and Potential Responsiveness to Notch1 Inhibitors.
J Clin Oncol, 35 (3): 352-360. [PMID:27870570]
3. Gurney Al, Hoey TC, Bruhns MF, Axelrod FT. (2014)
Notch1 receptor binding agents and methods of use thereof.
Patent number: US20140011271A1. Assignee: Oncomed Pharmaceuticals. Priority date: 08/07/2008. Publication date: 09/01/2014.
4. López-Guerra M, Xargay-Torrent S, Fuentes P, Roldán J, González-Farré B, Rosich L, Silkenstedt E, García-León MJ, Lee-Vergés E, Giménez N et al.. (2020)
Specific NOTCH1 antibody targets DLL4-induced proliferation, migration, and angiogenesis in NOTCH1-mutated CLL cells.
Oncogene, 39 (6): 1185-1197. [PMID:31616059]
5. Silkenstedt E, Arenas F, Colom-Sanmartí B, Xargay-Torrent S, Higashi M, Giró A, Rodriguez V, Fuentes P, Aulitzky WE, van der Kuip H et al.. (2019)
Notch1 signaling in NOTCH1-mutated mantle cell lymphoma depends on Delta-Like ligand 4 and is a potential target for specific antibody therapy.
J Exp Clin Cancer Res, 38 (1): 446. [PMID:31676012]