Metabolism of [ 3H]leupeptin by rat liver
Tritium-labeled leupeptin was used to study how this tripeptide proteinase inhibitor interacts with the liver, including the mechanism of its transport into the cell, its subcellular distribution after uptake, and its metabolism once in the tissue. Experiments were done in situ and in a perfused liv...
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Veröffentlicht in: | Archives of biochemistry and biophysics 1985-08, Vol.240 (2), p.768-776 |
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description | Tritium-labeled leupeptin was used to study how this tripeptide proteinase inhibitor interacts with the liver, including the mechanism of its transport into the cell, its subcellular distribution after uptake, and its metabolism once in the tissue. Experiments were done
in situ and in a perfused liver. At low concentrations (1 to 10 μ
m) the uptake of radioactive inhibitor was competed by chemically reduced leupeptin. At high concentrations at least up to 400 μ
m the uptake was directly proportional to the external concentration of tripeptide. Entry into the tissue essentially stopped at low temperature ( |
doi_str_mv | 10.1016/0003-9861(85)90085-2 |
format | Article |
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in situ and in a perfused liver. At low concentrations (1 to 10 μ
m) the uptake of radioactive inhibitor was competed by chemically reduced leupeptin. At high concentrations at least up to 400 μ
m the uptake was directly proportional to the external concentration of tripeptide. Entry into the tissue essentially stopped at low temperature (<21 °C). [
3H]Leupeptin initially was located in the soluble fraction of the liver homogenate and by 15 to 30 min became concentrated in the lysosome-rich fraction. During 2 h of perfusion almost 50% of [
3H]leupeptin that had entered the liver was secreted intact into the bile. In addition, a portion of the leupeptin that remained in the liver was degraded during this time period.</description><identifier>ISSN: 0003-9861</identifier><identifier>EISSN: 1096-0384</identifier><identifier>DOI: 10.1016/0003-9861(85)90085-2</identifier><identifier>PMID: 4026303</identifier><identifier>CODEN: ABBIA4</identifier><language>eng</language><publisher>San Diego, CA: Elsevier Inc</publisher><subject>Animals ; Applied sciences ; Binding, Competitive ; Biological Transport, Active ; Chloroquine - pharmacology ; Exact sciences and technology ; Leupeptins - metabolism ; Liver - drug effects ; Liver - metabolism ; Lysosomes - metabolism ; Male ; Oligopeptides - metabolism ; Other techniques and industries ; Perfusion ; Rats ; Rats, Inbred Strains ; Temperature</subject><ispartof>Archives of biochemistry and biophysics, 1985-08, Vol.240 (2), p.768-776</ispartof><rights>1985</rights><rights>1986 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-8f252fba1e54f5860a4a1ebf994ee15630700cc591d89e685cdb8439fd9124da3</citedby><cites>FETCH-LOGICAL-c386t-8f252fba1e54f5860a4a1ebf994ee15630700cc591d89e685cdb8439fd9124da3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/0003-9861(85)90085-2$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=8840276$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/4026303$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Dennis, Patricia A.</creatorcontrib><creatorcontrib>Aronson, Nathan N.</creatorcontrib><title>Metabolism of [ 3H]leupeptin by rat liver</title><title>Archives of biochemistry and biophysics</title><addtitle>Arch Biochem Biophys</addtitle><description>Tritium-labeled leupeptin was used to study how this tripeptide proteinase inhibitor interacts with the liver, including the mechanism of its transport into the cell, its subcellular distribution after uptake, and its metabolism once in the tissue. Experiments were done
in situ and in a perfused liver. At low concentrations (1 to 10 μ
m) the uptake of radioactive inhibitor was competed by chemically reduced leupeptin. At high concentrations at least up to 400 μ
m the uptake was directly proportional to the external concentration of tripeptide. Entry into the tissue essentially stopped at low temperature (<21 °C). [
3H]Leupeptin initially was located in the soluble fraction of the liver homogenate and by 15 to 30 min became concentrated in the lysosome-rich fraction. During 2 h of perfusion almost 50% of [
3H]leupeptin that had entered the liver was secreted intact into the bile. In addition, a portion of the leupeptin that remained in the liver was degraded during this time period.</description><subject>Animals</subject><subject>Applied sciences</subject><subject>Binding, Competitive</subject><subject>Biological Transport, Active</subject><subject>Chloroquine - pharmacology</subject><subject>Exact sciences and technology</subject><subject>Leupeptins - metabolism</subject><subject>Liver - drug effects</subject><subject>Liver - metabolism</subject><subject>Lysosomes - metabolism</subject><subject>Male</subject><subject>Oligopeptides - metabolism</subject><subject>Other techniques and industries</subject><subject>Perfusion</subject><subject>Rats</subject><subject>Rats, Inbred Strains</subject><subject>Temperature</subject><issn>0003-9861</issn><issn>1096-0384</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1985</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE9LAzEQxYMotVa_gcIeRPSwOtn8aXIRpKgVKl70JBKy2QlEtt2a7Bb67d3a0qOnGXi_eTPzCDmncEuByjsAYLlWkl4rcaMBlMiLAzKkoGUOTPFDMtwjx-QkpW8ASrksBmTAoZAM2JDcvGJry6YOaZ41PvvM2PSrxm6JyzYssnKdRdtmdVhhPCVH3tYJz3Z1RD6eHt8n03z29vwyeZjljinZ5soXovClpSi4F0qC5X1feq05IhX91jGAc0LTSmmUSriqVJxpX2la8MqyEbna-i5j89Nhas08JId1bRfYdMmMZcHZWLAe5FvQxSaliN4sY5jbuDYUzCYhs3nfbN43Spi_hEzRj13s_LtyjtV-aBdJr1_udJucrX20CxfSHlOqB8eyx-63GPZZrAJGk1zAhcMqRHStqZrw_x2_a05_Vw</recordid><startdate>19850801</startdate><enddate>19850801</enddate><creator>Dennis, Patricia A.</creator><creator>Aronson, Nathan N.</creator><general>Elsevier Inc</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19850801</creationdate><title>Metabolism of [ 3H]leupeptin by rat liver</title><author>Dennis, Patricia A. ; Aronson, Nathan N.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-8f252fba1e54f5860a4a1ebf994ee15630700cc591d89e685cdb8439fd9124da3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1985</creationdate><topic>Animals</topic><topic>Applied sciences</topic><topic>Binding, Competitive</topic><topic>Biological Transport, Active</topic><topic>Chloroquine - pharmacology</topic><topic>Exact sciences and technology</topic><topic>Leupeptins - metabolism</topic><topic>Liver - drug effects</topic><topic>Liver - metabolism</topic><topic>Lysosomes - metabolism</topic><topic>Male</topic><topic>Oligopeptides - metabolism</topic><topic>Other techniques and industries</topic><topic>Perfusion</topic><topic>Rats</topic><topic>Rats, Inbred Strains</topic><topic>Temperature</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Dennis, Patricia A.</creatorcontrib><creatorcontrib>Aronson, Nathan N.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Archives of biochemistry and biophysics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Dennis, Patricia A.</au><au>Aronson, Nathan N.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Metabolism of [ 3H]leupeptin by rat liver</atitle><jtitle>Archives of biochemistry and biophysics</jtitle><addtitle>Arch Biochem Biophys</addtitle><date>1985-08-01</date><risdate>1985</risdate><volume>240</volume><issue>2</issue><spage>768</spage><epage>776</epage><pages>768-776</pages><issn>0003-9861</issn><eissn>1096-0384</eissn><coden>ABBIA4</coden><abstract>Tritium-labeled leupeptin was used to study how this tripeptide proteinase inhibitor interacts with the liver, including the mechanism of its transport into the cell, its subcellular distribution after uptake, and its metabolism once in the tissue. Experiments were done
in situ and in a perfused liver. At low concentrations (1 to 10 μ
m) the uptake of radioactive inhibitor was competed by chemically reduced leupeptin. At high concentrations at least up to 400 μ
m the uptake was directly proportional to the external concentration of tripeptide. Entry into the tissue essentially stopped at low temperature (<21 °C). [
3H]Leupeptin initially was located in the soluble fraction of the liver homogenate and by 15 to 30 min became concentrated in the lysosome-rich fraction. During 2 h of perfusion almost 50% of [
3H]leupeptin that had entered the liver was secreted intact into the bile. In addition, a portion of the leupeptin that remained in the liver was degraded during this time period.</abstract><cop>San Diego, CA</cop><pub>Elsevier Inc</pub><pmid>4026303</pmid><doi>10.1016/0003-9861(85)90085-2</doi><tpages>9</tpages></addata></record> |
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subjects | Animals Applied sciences Binding, Competitive Biological Transport, Active Chloroquine - pharmacology Exact sciences and technology Leupeptins - metabolism Liver - drug effects Liver - metabolism Lysosomes - metabolism Male Oligopeptides - metabolism Other techniques and industries Perfusion Rats Rats, Inbred Strains Temperature |
title | Metabolism of [ 3H]leupeptin by rat liver |
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