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Synonyms: example 315 [US20090131492A1] | VX-661 | VX661
tezacaftor is an approved drug (EMA & FDA (2018))
Compound class:
Synthetic organic
Comment: Tezacaftor is a small molecule cystic fibrosis transmembrane conductance regulator (CFTR) modulator that was developed by Vertex Pharmaceuticals [4].
![]() 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. Drévillon L, Tanguy G, Hinzpeter A, Arous N, de Becdelièvre A, Aissat A, Tarze A, Goossens M, Fanen P. (2011)
COMMD1-mediated ubiquitination regulates CFTR trafficking. PLoS One, 6 (3): e18334. [PMID:21483833] |
2. Fernández Massó JR, Oliva Argüelles B, Tejeda Y, Astrada S, Garay H, Reyes O, Delgado-Roche L, Bollati-Fogolín M, Vallespí MG. (2013)
The Antitumor Peptide CIGB-552 Increases COMMD1 and Inhibits Growth of Human Lung Cancer Cells. J Amino Acids, 2013: 251398. [PMID:23401744] |
3. Gomez Rodriguez Y, Oliva Arguelles B, Riera-Romo M, Fernandez-De-Cossio J, Garay HE, Fernandez Masso J, Guerra Vallespi M. (2022)
Synergic effect of anticancer peptide CIGB-552 and Cisplatin in lung cancer models. Mol Biol Rep, 49 (4): 3197-3212. [PMID:35094208] |
4. Ruah SSH, Grootenhuis PDJ, Van Goor F, Zhou J, Bear B, Miller MT, McCartney J, Numa MMD. (2009)
Indole derivatives as CFTR modulators. Patent number: US20090131492A1. Assignee: ertex Pharmaceuticals Inc. Priority date: 07/04/2006. Publication date: 21/05/2009. |
5. Tanguy G, Drévillon L, Arous N, Hasnain A, Hinzpeter A, Fritsch J, Goossens M, Fanen P. (2008)
CSN5 binds to misfolded CFTR and promotes its degradation. Biochim Biophys Acta, 1783 (6): 1189-99. [PMID:18267124] |