Biochemical and pharmacological studies with 1-β- d-arabinofuranosylcytosine in man
Cytosine arabinoside, labeled with tritium, was administered to five patients with far-advanced neoplasms. The analog was rapidly deaminated to uracil arabinoside; the latter accounted for between 86 and 96 per cent of the radioactivity excreted in the urine. Incorporation of tritium-labeled cytidin...
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| Veröffentlicht in: | Biochemical pharmacology 1966-10, Vol.15 (10), p.1417-1428 |
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| container_title | Biochemical pharmacology |
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| creator | Creasey, William A. Papac, Rose J. Markiw, Maria E. Calabresi, Paul Welch, Arnold D. |
| description | Cytosine arabinoside, labeled with tritium, was administered to five patients with far-advanced neoplasms. The analog was rapidly deaminated to uracil arabinoside; the latter accounted for between 86 and 96 per cent of the radioactivity excreted in the urine. Incorporation of tritium-labeled cytidine into DNA by suspensions of human leukemic leukocytes was inhibited in the presence of cytosine arabinoside. Although administration of cytosine arabinoside at therapeutic levels depressed the ability of leukemic leukocytes to incorporate cytidine into DNA
in vitro, there was no correlation between the degree and duration of this effect and the clinical response to the drug. Tritium-labeled cytosine arabinoside entered human leukemic leukocytes very rapidly when incubated with the cells
in vitro; there was a small but significant incorporation of the analog into both DNA and RNA. |
| doi_str_mv | 10.1016/0006-2952(66)90186-9 |
| format | Article |
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in vitro, there was no correlation between the degree and duration of this effect and the clinical response to the drug. Tritium-labeled cytosine arabinoside entered human leukemic leukocytes very rapidly when incubated with the cells
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in vitro, there was no correlation between the degree and duration of this effect and the clinical response to the drug. Tritium-labeled cytosine arabinoside entered human leukemic leukocytes very rapidly when incubated with the cells
in vitro; there was a small but significant incorporation of the analog into both DNA and RNA.</description><subject>Adult</subject><subject>Carcinoma, Hepatocellular - drug therapy</subject><subject>Chromatography, Paper</subject><subject>Cytarabine - blood</subject><subject>Cytarabine - metabolism</subject><subject>Cytarabine - therapeutic use</subject><subject>Cytarabine - urine</subject><subject>DNA - metabolism</subject><subject>Female</subject><subject>Humans</subject><subject>Leukemia, Myeloid - drug therapy</subject><subject>Leukocytes - metabolism</subject><subject>Liver Neoplasms</subject><subject>Lymphoma, Large B-Cell, Diffuse - drug therapy</subject><subject>Male</subject><subject>Melanoma - drug therapy</subject><subject>Middle Aged</subject><subject>Nucleosides - metabolism</subject><subject>RNA - metabolism</subject><subject>RNA, Transfer - metabolism</subject><subject>Tritium</subject><subject>Uracil Nucleotides - metabolism</subject><subject>Uridine - metabolism</subject><issn>0006-2952</issn><issn>1873-2968</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1966</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kM9OwzAMxiMEGmPwBiD1hOBQSJY2TS5IMPFPmsRlnKM0cVlQm4ykBe21eBCeiZZNO3KwLNufP8s_hE4JviKYsGuMMUunIp9eMHYpMOEsFXtoTHhB-zbj-2i8kxyioxjfh5IzMkKjbCoIzYsxWtxZr5fQWK3qRDmTrJYqNEr72r_99WLbGQsx-bLtMiHpz3eamFQFVVrnqy4o5-O61uvWR-sgsS5plDtGB5WqI5xs8wS9PtwvZk_p_OXxeXY7T3V_u015xXnJFAhOGAcKpsA0M0KpXPXBC1GRUlOuuTC5LkT_mNBaV1yoUrACV3SCzje-q-A_OoitbGzUUNfKge-i5BmlJKNZL8w2Qh18jAEquQq2UWEtCZYDTDmgkQMpyZj8gylFv3a29e_KBsxuaUuvn99s5tA_-WkhyKgtOA3GBtCtNN7-f-AXNt-FCA</recordid><startdate>196610</startdate><enddate>196610</enddate><creator>Creasey, William A.</creator><creator>Papac, Rose J.</creator><creator>Markiw, Maria E.</creator><creator>Calabresi, Paul</creator><creator>Welch, Arnold D.</creator><general>Elsevier Inc</general><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>196610</creationdate><title>Biochemical and pharmacological studies with 1-β- d-arabinofuranosylcytosine in man</title><author>Creasey, William A. ; Papac, Rose J. ; Markiw, Maria E. ; Calabresi, Paul ; Welch, Arnold D.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c357t-8f88b6ae98168e3ed7034d9aa5aaa5879f1bc38c89d5c791879cccf89ab9670f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1966</creationdate><topic>Adult</topic><topic>Carcinoma, Hepatocellular - drug therapy</topic><topic>Chromatography, Paper</topic><topic>Cytarabine - blood</topic><topic>Cytarabine - metabolism</topic><topic>Cytarabine - therapeutic use</topic><topic>Cytarabine - urine</topic><topic>DNA - metabolism</topic><topic>Female</topic><topic>Humans</topic><topic>Leukemia, Myeloid - drug therapy</topic><topic>Leukocytes - metabolism</topic><topic>Liver Neoplasms</topic><topic>Lymphoma, Large B-Cell, Diffuse - drug therapy</topic><topic>Male</topic><topic>Melanoma - drug therapy</topic><topic>Middle Aged</topic><topic>Nucleosides - metabolism</topic><topic>RNA - metabolism</topic><topic>RNA, Transfer - metabolism</topic><topic>Tritium</topic><topic>Uracil Nucleotides - metabolism</topic><topic>Uridine - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Creasey, William A.</creatorcontrib><creatorcontrib>Papac, Rose J.</creatorcontrib><creatorcontrib>Markiw, Maria E.</creatorcontrib><creatorcontrib>Calabresi, Paul</creatorcontrib><creatorcontrib>Welch, Arnold D.</creatorcontrib><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>Biochemical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Creasey, William A.</au><au>Papac, Rose J.</au><au>Markiw, Maria E.</au><au>Calabresi, Paul</au><au>Welch, Arnold D.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Biochemical and pharmacological studies with 1-β- d-arabinofuranosylcytosine in man</atitle><jtitle>Biochemical pharmacology</jtitle><addtitle>Biochem Pharmacol</addtitle><date>1966-10</date><risdate>1966</risdate><volume>15</volume><issue>10</issue><spage>1417</spage><epage>1428</epage><pages>1417-1428</pages><issn>0006-2952</issn><eissn>1873-2968</eissn><abstract>Cytosine arabinoside, labeled with tritium, was administered to five patients with far-advanced neoplasms. The analog was rapidly deaminated to uracil arabinoside; the latter accounted for between 86 and 96 per cent of the radioactivity excreted in the urine. Incorporation of tritium-labeled cytidine into DNA by suspensions of human leukemic leukocytes was inhibited in the presence of cytosine arabinoside. Although administration of cytosine arabinoside at therapeutic levels depressed the ability of leukemic leukocytes to incorporate cytidine into DNA
in vitro, there was no correlation between the degree and duration of this effect and the clinical response to the drug. Tritium-labeled cytosine arabinoside entered human leukemic leukocytes very rapidly when incubated with the cells
in vitro; there was a small but significant incorporation of the analog into both DNA and RNA.</abstract><cop>England</cop><pub>Elsevier Inc</pub><pmid>4291357</pmid><doi>10.1016/0006-2952(66)90186-9</doi><tpages>12</tpages></addata></record> |
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| subjects | Adult Carcinoma, Hepatocellular - drug therapy Chromatography, Paper Cytarabine - blood Cytarabine - metabolism Cytarabine - therapeutic use Cytarabine - urine DNA - metabolism Female Humans Leukemia, Myeloid - drug therapy Leukocytes - metabolism Liver Neoplasms Lymphoma, Large B-Cell, Diffuse - drug therapy Male Melanoma - drug therapy Middle Aged Nucleosides - metabolism RNA - metabolism RNA, Transfer - metabolism Tritium Uracil Nucleotides - metabolism Uridine - metabolism |
| title | Biochemical and pharmacological studies with 1-β- d-arabinofuranosylcytosine in man |
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