Abstract:
:Glutamine and tyrosine-based amino acid conjugates of monocarboxylate transporter types 1 and 2 inhibitors (MCT1/2) were designed, synthesized and evaluated for their potency in blocking the proliferation of a human B lymphoma cell line that expresses the transporters Asct2, LAT1 and MCT1. Appropriate placement of an amino acid transporter recognition element was shown to augment anti-tumour efficacy vs. Raji cells. Amino acid conjugation also improves the pharmacodynamic properties of experimental MCT1/2 inhibitors.
journal_name
Medchemcommjournal_title
MedChemCommauthors
Nair RN,Mishra JK,Li F,Tortosa M,Yang C,Doherty JR,Cameron M,Cleveland JL,Roush WR,Bannister TDdoi
10.1039/C5MD00579Esubject
Has Abstractpub_date
2016-05-01 00:00:00pages
900-905issue
5eissn
2040-2503issn
2040-2511journal_volume
7pub_type
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