OTX008 [Neurosurgery Wiki]

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=====OTX008=====
Calix[4]arene compound 0118 is an angiostatic agent that inhibits tumor growth in mice. Although 0118 is a topomimetic of [[galectin-1]]-targeting angiostatic amphipathic peptide Anginex, we had yet to prove that 0118 targets galectin-1. 

(15)N-(1)H HSQC NMR spectroscopy demonstrates that 0118 indeed targets galectin-1 at a site away from the [[lectin]]'s carbohydrate binding site and thereby attenuates lactose binding to the lectin. Flow cytometry and agglutination assays show that 0118 attenuates binding of galectin-1 to cell surface glycans, and the inhibition of cell proliferation by 0118 is found to be correlated with the cellular expression of the lectin. In general,0118 targets galectin-1 as an allosteric inhibitor of glycan/carbohydrate binding
((Dings RP, Miller MC, Nesmelova I, Astorgues-Xerri L, Kumar N, Serova M, Chen
X, Raymond E, Hoye TR, Mayo KH. Antitumor agent calixarene 0118 targets human
galectin-1 as an allosteric inhibitor of carbohydrate binding. J Med Chem. 2012
Jun 14;55(11):5121-9. doi: 10.1021/jm300014q. Epub 2012 May 30. PubMed PMID:
22575017.
)).

OTX008 is a [[galectin-1]]-targeting compound, currently undergoing a phase I clinical trial. This study aimed at investigating OTX008 pharmacokinetics (PK) and antineoplastic activity.