Synonyms: MK0752
Compound class:
Synthetic organic
Comment: MK-0752 is a γ-secretase [1] and Notch pathway inhibitor that was originally intended for the treatment of Alzheimer's disease, but was later redeployed for anti-tumour potential.
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
1. Cook JJ, Wildsmith KR, Gilberto DB, Holahan MA, Kinney GG, Mathers PD, Michener MS, Price EA, Shearman MS, Simon AJ et al.. (2010)
Acute gamma-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-beta production to alternative APP fragments without amyloid-beta rebound. J Neurosci, 30 (19): 6743-50. [PMID:20463236] |
2. Cook N, Basu B, Smith DM, Gopinathan A, Evans J, Steward WP, Palmer D, Propper D, Venugopal B, Hategan M et al.. (2018)
A phase I trial of the γ-secretase inhibitor MK-0752 in combination with gemcitabine in patients with pancreatic ductal adenocarcinoma. Br J Cancer, 118 (6): 793-801. [PMID:29438372] |
3. Hoffman LM, Fouladi M, Olson J, Daryani VM, Stewart CF, Wetmore C, Kocak M, Onar-Thomas A, Wagner L, Gururangan S et al.. (2015)
Phase I trial of weekly MK-0752 in children with refractory central nervous system malignancies: a pediatric brain tumor consortium study. Childs Nerv Syst, 31 (8): 1283-9. [PMID:25930724] |
4. Kumar D, Ganeshpurkar A, Kumar D, Modi G, Gupta SK, Singh SK. (2018)
Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead. Eur J Med Chem, 148: 436-452. [PMID:29477076] |