NDLI: 2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport

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2-Amino-4-bis(aryloxybenzyl)aminobutanoic acids: A novel scaffold for inhibition of ASCT2-mediated glutamine transport

Content Provider	Scilit
Author	Schulte, Michael L. Khodadadi, Alexandra B. Cuthbertson, Madison L. Smith, Jarrod A. Manning, H. Charles
Copyright Year	2016
Description	Journal: Bioorganic & medicinal chemistry letters Herein, we report the discovery of 2-amino-4-bis(aryloxybenzyl)aminobutanoic acids as novel inhibitors of ASCT2(SLC1A5)-mediated glutamine accumulation in mammalian cells. Focused library development led to two novel ASCT2 inhibitors that exhibit significantly improved potency compared with prior art in C6 (rat) and HEK293 (human) cells. The potency of leads reported here represents a 40-fold improvement over our most potent, previously reported inhibitor and represents, to our knowledge, the most potent pharmacological inhibitors of ASCT2-mediated glutamine accumulation in live cells. These and other compounds in this novel series exhibit tractable chemical properties for further development as potential therapeutic leads.
Related Links	http://europepmc.org/articles/pmc4727990?pdf=render https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4727990/pdf
Ending Page	1047
Page Count	4
Starting Page	1044
ISSN	0960894X
DOI	10.1016/j.bmcl.2015.12.031
Journal	Bioorganic & medicinal chemistry letters
Issue Number	3
Volume Number	26
Language	English
Publisher	Elsevier BV
Publisher Date	2016-02-01
Access Restriction	Open
Subject Keyword	Journal: Bioorganic & medicinal chemistry letters Medicinal Chemistry
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Drug Discovery Biochemistry Molecular Biology Clinical Biochemistry Molecular Medicine Pharmaceutical Science

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