Faculty Opinions recommendation of Discovery of a highly potent, nonabsorbable apical sodium-dependent bile acid transporter inhibitor (GSK2330672) for treatment of type 2 diabetes.

2013 ◽  
Author(s):  
Meenakshisundaram Ananthanarayanan
Keyword(s):  
Type 2 Diabetes ◽  
Bile Acid ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

Discovery of a Highly Potent, Nonabsorbable Apical Sodium-Dependent Bile Acid Transporter Inhibitor (GSK2330672) for Treatment of Type 2 Diabetes

2013 ◽  
Vol 56 (12) ◽  
pp. 5094-5114 ◽  
Author(s):  
Yulin Wu ◽  
Christopher J. Aquino ◽  
David J. Cowan ◽  
Don L. Anderson ◽  
Jeff L. Ambroso ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Bile Acid ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

scholarly journals The inhibitors of the apical sodium-dependent bile acid transporter (ASBT) as promising drugs

2020 ◽  
Vol 66 (3) ◽  
pp. 185-195
Author(s):  
E.E. Saveleva ◽  
E.S. Tyutrina ◽  
T. Nakanishi ◽  
I. Tamai ◽  
A.B. Salmina
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Enterohepatic Circulation ◽  
Alcoholic Fatty Liver ◽  
Good Tolerance ◽  
Current Trends ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

Inhibition of the apical sodium-dependent bile acid transporter (ASBT, also known as IBAT — ileal bile acid transporter, SLC10A2) leads to disruption of the enterohepatic circulation of bile acids and their excretion with fecal masses. This is accompanied by cholesterol utilization for synthesis of new bile acids. ASBT inhibitors are promising drugs for the treatment of such diseases as non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, type 2 diabetes mellitus, necrotic enterocolitis, chronic constipation, atherosclerosis. To date the most known chemically synthesized inhibitors are: A3309, SHP626, A4250, 264W94, GSK2330672, SC-435. All of them are at different stages of clinical trials, which confirm the high efficacy and good tolerance of these inhibitors. Current trends in this field also include directed chemical synthesis of ASBT inhibitors, as well as their search among substances of plant origin.

Induction of sodium-dependent bile acid transporter messenger RNA, protein, and activity in rat ileum by cholic acid

1997 ◽  
Vol 113 (5) ◽  
pp. 1599-1608 ◽  
Author(s):  
RT Stravitz ◽  
AJ Sanyal ◽  
WM Pandak ◽  
ZR Vlahcevic ◽  
JW Beets ◽  
...  
Keyword(s):  
Bile Acid ◽  
Cholic Acid ◽  
Messenger Rna ◽  
Rat Ileum ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

Comparative analysis of the ontogeny of a sodium-dependent bile acid transporter in rat kidney and ileum

1996 ◽  
Vol 271 (2) ◽  
pp. G377-G385 ◽  
Author(s):  
D. M. Christie ◽  
P. A. Dawson ◽  
S. Thevananther ◽  
B. L. Shneider
Keyword(s):  
Bile Acid ◽  
Rat Kidney ◽  
Membrane Vesicles ◽  
Mrna Levels ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Old Rats ◽  
Acid Transporter ◽  
The Difference ◽  
And Function

An apical sodium-dependent bile acid transporter (ASBT) has recently been cloned and characterized in the rat ileum. Northern and Western blotting revealed both the ASBT mRNA and protein in rat kidney. The coding sequence of the kidney transcript was found to be identical to the previously cloned ileal ASBT. Indirect immunofluorescence studies localized the ASBT protein to the apical membrane of the renal proximal convoluted tubule. Kinetic analysis of sodium-dependent taurocholate uptake using membrane vesicles revealed a similar Michaelis-Menten constant value for taurocholate in the kidney and intestine. ASBT protein and function were present in the kidney but not the ileum from 7-day-old rats. On postnatal day 7, there was a sevenfold increase in ASBT steady-state mRNA levels in the kidney relative to the ileum, yet nuclear run-on assays revealed that the nascent transcription rates at this age were virtually the same. This suggests that the difference in the neonatal expression of the ASBT gene in the kidney and ileum may be in part due to differences in mRNA stability.

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