Five Amino Acids in the Innermost Cavity of the Substrate Binding Cleft of Organic Cation Transporter 1 Interact with Extracellular and Intracellular Corticosterone

2009 ◽  
Vol 76 (2) ◽  
pp. 275-289 ◽  
Author(s):  
Christopher Volk ◽  
Valentin Gorboulev ◽  
Alexander Kotzsch ◽  
Thomas D. Müller ◽  
Hermann Koepsell
Keyword(s):  
Amino Acids ◽  
Organic Cation ◽  
Substrate Binding ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1 ◽  
Binding Cleft

scholarly journals A Substrate Binding Hinge Domain Is Critical for Transport-related Structural Changes of Organic Cation Transporter 1

2012 ◽  
Vol 287 (37) ◽  
pp. 31561-31573 ◽  
Author(s):  
Brigitte Egenberger ◽  
Valentin Gorboulev ◽  
Thorsten Keller ◽  
Dmitry Gorbunov ◽  
Neha Gottlieb ◽  
...  
Keyword(s):  
Structural Changes ◽  
Organic Cation ◽  
Substrate Binding ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1 ◽  
Hinge Domain

L503F variant of carnitine/organic cation transporter 1 efficiently transports metformin and other biguanides

2016 ◽  
Vol 68 (9) ◽  
pp. 1160-1169 ◽  
Author(s):  
Azusa Futatsugi ◽  
Yusuke Masuo ◽  
Shiori Kawabata ◽  
Noritaka Nakamichi ◽  
Yukio Kato
Keyword(s):  
Organic Cation ◽  
Organic Cation Transporter ◽  
Organic Cation Transporter 1

scholarly journals The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC-1 coactivator

2016 ◽  
Vol 173 (10) ◽  
pp. 1703-1715 ◽  
Author(s):  
Lucie Hyrsova ◽  
Tomas Smutny ◽  
Alejandro Carazo ◽  
Stefan Moravcik ◽  
Jana Mandikova ◽  
...  
Keyword(s):  
Organic Cation ◽  
Pregnane X Receptor ◽  
Organic Cation Transporter ◽  
Human Hepatocytes ◽  
Organic Cation Transporter 1

PIII-66Development of an immobilized human organic cation transporter 1 column for use in on-line screening

2006 ◽  
Vol 79 (2) ◽  
pp. P76-P76
Author(s):  
F BIGHI ◽  
R YAMAGUCHI ◽  
S PATEL ◽  
P HO ◽  
I WAINER ◽  
...  
Keyword(s):  
Organic Cation ◽  
Organic Cation Transporter ◽  
On Line ◽  
Organic Cation Transporter 1

Different Affinities of Inhibitors to the Outwardly and Inwardly Directed Substrate Binding Site of Organic Cation Transporter 2

2003 ◽  
Vol 64 (5) ◽  
pp. 1037-1047 ◽  
Author(s):  
Christopher Volk ◽  
Valentin Gorboulev ◽  
Thomas Budiman ◽  
Georg Nagel ◽  
Hermann Koepsell
Keyword(s):  
Binding Site ◽  
Organic Cation ◽  
Substrate Binding ◽  
Organic Cation Transporter ◽  
Substrate Binding Site ◽  
Organic Cation Transporter 2

scholarly journals Regulation Mechanisms of Expression and Function of Organic Cation Transporter 1

2021 ◽  
Vol 11 ◽  
Author(s):  
Giuliano Ciarimboli
Keyword(s):  
Organic Cation ◽  
Basolateral Membrane ◽  
Organic Cation Transporter ◽  
Organic Cations ◽  
Regulatory Processes ◽  
Organic Cation Transporter 1 ◽  
Exogenous Origin ◽  
And Function

The organic cation transporter 1 (OCT1) belongs together with OCT2 and OCT3 to the solute carrier family 22 (SLC22). OCTs are involved in the movement of organic cations through the plasma membrane. In humans, OCT1 is mainly expressed in the sinusoidal membrane of hepatocytes, while in rodents, OCT1 is strongly represented also in the basolateral membrane of renal proximal tubule cells. Considering that organic cations of endogenous origin are important neurotransmitters and that those of exogenous origin are important drugs, these transporters have significant physiological and pharmacological implications. Because of the high expression of OCTs in excretory organs, their activity has the potential to significantly impact not only local but also systemic concentration of their substrates. Even though many aspects governing OCT function, interaction with substrates, and pharmacological role have been extensively investigated, less is known about regulation of OCTs. Possible mechanisms of regulation include genetic and epigenetic modifications, rapid regulation processes induced by kinases, regulation caused by protein–protein interaction, and long-term regulation induced by specific metabolic and pathological situations. In this mini-review, the known regulatory processes of OCT1 expression and function obtained from in vitro and in vivo studies are summarized. Further research should be addressed to integrate this knowledge to known aspects of OCT1 physiology and pharmacology.

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