Design, synthesis and biological activity of tetrazole-bearing uric acid transporter 1 inhibitors
Sign Up to like & getrecommendations! Published in 2017 at "Chemical Research in Chinese Universities"
DOI: 10.1007/s40242-017-6351-3
Abstract: Systematic structure-activity relationship(SAR) exploration of a moderately active tetrazole-bearing lesinurad-based hit 1f led to the discovery of a potent uric acid transporter 1(URAT1) inhibitor 1i, which possessed a novel molecular skeleton and was 11-fold more… read more here.
Keywords: uric acid; acid transporter; activity; tetrazole bearing ... See more keywords
Molecular characteristics supporting l-Type amino acid transporter 1 (LAT1)-mediated translocation.
Sign Up to like & getrecommendations! Published in 2021 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2021.104921
Abstract: l-Type amino acid transporter 1 (LAT1) is an interesting protein due to its peculiar expression profile. It can be utilized not only as a carrier for improved or targeted drug delivery, e.g., into the brain… read more here.
Keywords: amino acid; transporter lat1; type amino; acid transporter ... See more keywords
The amino acid transporter PAT1 regulates mTORC1 in a nutrient-sensitive manner that requires its transport activity.
Sign Up to like & getrecommendations! Published in 2019 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2018.09.017
Abstract: The proton-coupled amino acid transporter PAT1 has been postulated to regulate the amino acid-stimulated mTORC1 through two different mechanisms, either it activates mTORC1 by sensing and transducing the lysosomal amino acid signal to mTORC1, or… read more here.
Keywords: amino acid; acid transporter; mtorc1; pat1 ... See more keywords
Structural properties for selective and efficient l‐type amino acid transporter 1 (LAT1) mediated cellular uptake
Sign Up to like & getrecommendations! Published in 2018 at "International Journal of Pharmaceutics"
DOI: 10.1016/j.ijpharm.2018.04.025
Abstract: Graphical abstract Figure. No Caption available. Abstract l‐Type amino acid transporter 1 (LAT1) is a sodium‐independent exchanger transporting large neural amino acids and several amino‐acid mimicking drugs across the cell membranes. LAT1 is highly expressed… read more here.
Keywords: amino acid; transporter lat1; type amino; acid transporter ... See more keywords
Dissecting the Conformational Dynamics of the Bile Acid Transporter Homologue ASBTNM.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2020.166764
Abstract: Apical sodium-dependent bile acid transporter (ASBT) catalyses uphill transport of bile acids using the electrochemical gradient of Na+ as the driving force. The crystal structures of two bacterial homologues ASBTNM and ASBTYf have previously been… read more here.
Keywords: bile acid; acid transporter; crystal structures; conformational dynamics ... See more keywords
Molecular features of the L-type amino acid transporter 2 determine different import and export profiles for thyroid hormones and amino acids
Sign Up to like & getrecommendations! Published in 2017 at "Molecular and Cellular Endocrinology"
DOI: 10.1016/j.mce.2017.01.024
Abstract: The L-type amino acid transporter 2 (LAT2) imports amino acids (AA) and also certain thyroid hormones (TH), e.g. 3,3'-T2 and T3, but not rT3 and T4. We utilized LAT2 mutations (Y130A, N133S, F242W) that increase… read more here.
Keywords: export; amino acid; type amino; acid transporter ... See more keywords
Modulatory Effect of Theaflavins on Apical Sodium-Dependent Bile Acid Transporter (ASBT) Activity.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of agricultural and food chemistry"
DOI: 10.1021/acs.jafc.1c03483
Abstract: Inhibiting apical sodium-dependent bile acid transporter (ASBT) has been identified as a potential strategy to reduce plasma cholesterol levels. Thus, in this study, we aimed to identify polyphenols that inhibited ASBT activity and to elucidate… read more here.
Keywords: acid transporter; apical sodium; asbt; bile acid ... See more keywords
Sodium-Dependent Neutral Amino Acid Transporter 2 Can Serve as a Tertiary Carrier for l-Type Amino Acid Transporter 1-Utilizing Prodrugs
Sign Up to like & getrecommendations! Published in 2023 at "Molecular Pharmaceutics"
DOI: 10.1021/acs.molpharmaceut.2c00948
Abstract: Membrane transporters are the key determinants of the homeostasis of endogenous compounds in the cells and their exposure to drugs. However, the substrate specificities of distinct transporters can overlap. In the present study, the interactions… read more here.
Keywords: acid transporter; utilizing prodrugs; amino acid;
Design and Characterization of Novel Small Molecule Activators of Excitatory Amino Acid Transporter 2.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.2c00304
Abstract: Excitotoxicity in the brain is a causal factor in several neurological and neurodegenerative disorders. Excitatory amino acid transporter 2 (EAAT2), an astrocytic glutamate transporter involved in the clearance of >80% of synaptic glutamate, is considered… read more here.
Keywords: transporter; excitatory amino; design characterization; acid transporter ... See more keywords
Optoproteomics elucidates the interactome of L-type amino acid transporter 3 (LAT3).
Sign Up to like & getrecommendations! Published in 2021 at "Chemical communications"
DOI: 10.1039/d0cc08423a
Abstract: Membrane protein interactions are crucial for diverse biological processes. We report the application of genetic code expansion in combination with photo-crosslinking chemistry, as we termed "optoproteomics", to identify proteins interacting with the human L-type membrane… read more here.
Keywords: type; transporter lat3; amino acid; acid transporter ... See more keywords
The 4b-4c loop of excitatory amino acid transporter 1 containing four critical residues essential for substrate transport
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Biomolecular Structure and Dynamics"
DOI: 10.1080/07391102.2019.1664935
Abstract: Abstract In the mammalians, the 4b-4c loop of excitatory amino acid transporters (EAATs) spans more than 50 amino-acid residues that are absent in glutamate transporter homologue of Pyrococcus horikoshii (GltPh). This part of insertion is… read more here.
Keywords: amino acid; acid transporter; transport; excitatory amino ... See more keywords