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Identification of a Unique Inhibitor-Binding Site on Choline Kinase α.
Kall SL, Delikatny EJ, Lavie A. Kall SL, et al. Biochemistry. 2018 Feb 27;57(8):1316-1325. doi: 10.1021/acs.biochem.7b01257. Epub 2018 Feb 8. Biochemistry. 2018. PMID: 29389115
Here we detail the 2.35 A structure of ChoKalpha in complex with TCD-717. Examination of this structure in conjunction with kinetic assays reveals that TCD-717 does not bind directly in the choline pocket as do previously characterized ChoKalpha inhibi …
Here we detail the 2.35 A structure of ChoKalpha in complex with TCD-717. Examination of this structure in conjunction with ki …
Combined 5-FU and ChoKα inhibitors as a new alternative therapy of colorectal cancer: evidence in human tumor-derived cell lines and mouse xenografts.
de la Cueva A, Ramírez de Molina A, Alvarez-Ayerza N, Ramos MA, Cebrián A, Del Pulgar TG, Lacal JC. de la Cueva A, et al. PLoS One. 2013 Jun 10;8(6):e64961. doi: 10.1371/journal.pone.0064961. Print 2013. PLoS One. 2013. PMID: 23762272 Free PMC article.
METHODOLOGY/PRINCIPAL FINDINGS: ChoKalpha specific inhibitors, MN58b and TCD-717, have demonstrated a potent antitumoral activity both in vitro and in vivo against several tumor-derived cell line xenografts including CRC-derived cell lines. ...The clinical relevance …
METHODOLOGY/PRINCIPAL FINDINGS: ChoKalpha specific inhibitors, MN58b and TCD-717, have demonstrated a potent antitumoral activ …