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View article: Biochemical characterization of a GDP-mannose transporter from Chaetomium thermophilum
Biochemical characterization of a GDP-mannose transporter from Chaetomium thermophilum Open
Nucleotide Sugar Transporters (NSTs) belong to the SLC35 family (human solute carrier) of membrane transport proteins and are crucial components of the glycosylation machinery. NSTs are localized in the ER and Golgi apparatus membranes, wh…
View article: Figure S5 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S5 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Assessment of lapatinib or trametinib as OATP1B1 substrates. (A) Percent uptake of 3H-lapatinib (1 µM) in OATP1B1 overexpressing HEK293 cells relative to uptake in HEK293 cells transfected with a vector control (VC) (n=3, from a single exp…
View article: Table S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Table S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Cellular viability and uptake of 8FcA by OATP1B1 following reverse transfection with 25 nM siRNA for various protein kinases. Percent uptake was determined relative to OATP1B1 uptake with control siRNA.
View article: Figure S4 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S4 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Assessment of LYN kinase expression, and function in the presence of various TKIs. (A) Detection of LYN protein expression in human hepatocyte and spleen lysates as determined by Western blot analysis. Prior to analysis, spleen (1:10) and …
View article: Figure S4 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S4 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Assessment of LYN kinase expression, and function in the presence of various TKIs. (A) Detection of LYN protein expression in human hepatocyte and spleen lysates as determined by Western blot analysis. Prior to analysis, spleen (1:10) and …
View article: Figure S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Influence of TKIs on OATP1B1-dependent uptake or substrate disposition. (A) Uptake of 3H-EβG (2 µM, 2 min) in OATP1B1 overexpressing HEK293 cells in the presence or absence of select individual FDA approved TKIs (10 μM) identified as posit…
View article: Figure S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Percent of total tyrosine-phosphorylated spectral counts for all OATP1B1 tyrosine residues after exposure to DMSO (vehicle) or nilotinib (10 μM). Three concentrated OATP1B1 protein extracts were purified by immunoprecipitation and analyzed…
View article: Figure S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Percent of total tyrosine-phosphorylated spectral counts for all OATP1B1 tyrosine residues after exposure to DMSO (vehicle) or nilotinib (10 μM). Three concentrated OATP1B1 protein extracts were purified by immunoprecipitation and analyzed…
View article: Figure S3 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S3 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
A structural model of OATP1B1. The model was generated by Phyre2 and presented as a cartoon. Y640 and Y645 are highlighted in blue and the image was produced with PyMOL.
View article: Table S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Table S2 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Cellular viability and uptake of 8FcA by OATP1B1 following reverse transfection with 25 nM siRNA for various protein kinases. Percent uptake was determined relative to OATP1B1 uptake with control siRNA.
View article: Figure S3 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S3 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
A structural model of OATP1B1. The model was generated by Phyre2 and presented as a cartoon. Y640 and Y645 are highlighted in blue and the image was produced with PyMOL.
View article: Table S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Table S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Mean {plus minus} SEM change of 8FcA uptake (Mean difference) in OATP1B1 overexpressing HEK293 cells between vehicle (DMSO) and exposure to FDA approved TKIs. Statistical significance was measured by ANOVA and Fisher's LSD test.
View article: Table S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Table S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Mean {plus minus} SEM change of 8FcA uptake (Mean difference) in OATP1B1 overexpressing HEK293 cells between vehicle (DMSO) and exposure to FDA approved TKIs. Statistical significance was measured by ANOVA and Fisher's LSD test.
View article: Figure S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S1 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Influence of TKIs on OATP1B1-dependent uptake or substrate disposition. (A) Uptake of 3H-EβG (2 µM, 2 min) in OATP1B1 overexpressing HEK293 cells in the presence or absence of select individual FDA approved TKIs (10 μM) identified as posit…
View article: Figure S5 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Figure S5 from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Assessment of lapatinib or trametinib as OATP1B1 substrates. (A) Percent uptake of 3H-lapatinib (1 µM) in OATP1B1 overexpressing HEK293 cells relative to uptake in HEK293 cells transfected with a vector control (VC) (n=3, from a single exp…
View article: Data from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Data from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Purpose:OATP1B1 (SLCO1B1) is the most abundant and pharmacologically relevant uptake transporter in the liver and a key mediator of xenobiotic clearance. However, the regulatory mechanisms that determine OATP1B1 activity remain uncertain, …
View article: Data from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Data from Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Purpose:OATP1B1 (SLCO1B1) is the most abundant and pharmacologically relevant uptake transporter in the liver and a key mediator of xenobiotic clearance. However, the regulatory mechanisms that determine OATP1B1 activity remain uncertain, …
View article: Biochemical characterization of a GDP-mannose transporter from<i>Chaetomium thermophilum</i>
Biochemical characterization of a GDP-mannose transporter from<i>Chaetomium thermophilum</i> Open
Nucleotide Sugar Transporters (NSTs) belong to the SLC35 family (human solute carrier) of membrane transport proteins and are crucial components of the glycosylation machinery. NSTs are localized in the ER and Golgi apparatus membranes, wh…
View article: Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation
Regulation of OATP1B1 Function by Tyrosine Kinase–mediated Phosphorylation Open
Purpose: OATP1B1 (SLCO1B1) is the most abundant and pharmacologically relevant uptake transporter in the liver and a key mediator of xenobiotic clearance. However, the regulatory mechanisms that determine OATP1B1 activity remain uncertain,…
View article: Conformational transitions of the sodium-dependent sugar transporter, vSGLT
Conformational transitions of the sodium-dependent sugar transporter, vSGLT Open
Significance Transporters isomerize between conformations to shuttle cargo across membranes, but the mechanism is not understood. Double electron–electron resonance measurements on the sodium-dependent sugar transporter (vSGLT) were used t…
View article: Active site voltage clamp fluorometry of the sodium glucose cotransporter hSGLT1
Active site voltage clamp fluorometry of the sodium glucose cotransporter hSGLT1 Open
Significance Site-directed fluorometry was used to understand conformational changes of the Na + /glucose symporter. SGLT1 functions by a mechanism where the substrate-binding site alternates between the two faces of the membrane, but litt…
View article: <b> A large Rab GTPase encoded by <i>CRACR2A</i> </b> <b>is a component of subsynaptic vesicles that transmit T cell activation signals</b>
<b> A large Rab GTPase encoded by <i>CRACR2A</i> </b> <b>is a component of subsynaptic vesicles that transmit T cell activation signals</b> Open
Recruitment of intracellular vesicles containing the large GTPase CRACR2A to the immunological synapse mediates T cell receptor signaling.
View article: Identification of a second substrate-binding site in solute-sodium symporters.
Identification of a second substrate-binding site in solute-sodium symporters. Open
Identification of a Second Substrate-binding Site in Solute-Sodium SymportersJournal of Biological ChemistryVol. 290Issue 1PreviewThe structure of the sodium/galactose transporter (vSGLT), a solute-sodium symporter (SSS) from Vibrio paraha…