Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P61278 (somatostatin)
 22,083 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The uptake of the cyclopeptide c(Phe-Thr-Lys-Trp-Phe-D-Pro) (008), an analog of somatostatin with retro sequence, was studied in isolated hepatocytes. 008 is taken up by hepatocytes in a concentration-, time-, energy- and temperature- dependent manner. Since 008 is hydrophobic, it binds rapidly to liver cells. This is evident by the positive intercept at the gamma-axis in the uptake curves. At higher concentrations, a minor part of the transport occurs by diffusion at a rate of 8.307.10(-6) cm/s. This part of diffusion is measured at 4 degrees C and can be subtracted from the uptake at 37 degrees C resulting in the carrier mediated part of uptake which is saturable. Kinetic parameters for the saturable part of uptake are Km 1.5 microM and Vmax 40.0 pmol/mg per min. The transport is decreased in the absence of oxygen and in the presence of metabolic inhibitors. Uptake is accelerated at temperatures above 20 degrees C. The activation energy was determined to be 30.77 kJ/mol. The membrane potential and not a sodium gradient is the main driving force for 008 transport. Cholate (a typical substrate of the multispecific bile acid transporter) and taurocholate are mutual competitive inhibitors of 008 uptake. Phalloidin, antamanide and iodipamide, typical foreign substrates of the transporter, interfere with the uptake of 008. AS 30D ascites hepatoma cells, known to be unable to transport bile acids, phalloidin and iodipamide, are also unfit to transport 008. Interestingly, sulfobromophthalein (BSP) but not rifampicin, both foreign substrates of the bilirubin carrier, inhibits the transport of 008 in a competitive manner.
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PMID:Hepatocellular transport of cyclosomatostatins: evidence for a carrier system related to the multispecific bile acid transporter. 170 41

Increased choleresis of up to 4950 ml per day was observed after positioning of a PTCD in a patient with complete biliary obstruction due to a malignant tumor. Bile secretion could be temporarily reduced to 15% of the initial flow rate by intravenous administration of somatostatin. Simultaneously, the concentration of bile acids increased from 1.2 to 6.2 mmol/l, whereas the concentrations of electrolytes remained constant. Cholic acid had no influence on bile secretion. To safeguard the patient from excessive loss of fluid and electrolytes, the drained bile was reinfused into the duodenum via a PEG.
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PMID:[Post-cholestatic hypercholeresis in a patient with malignant obstruction of the bile ducts]. 834 4