| pubmed-article:11120959 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C0019704 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C1524059 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C0031327 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C0033262 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C0018330 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C1999216 | lld:lifeskim |
| pubmed-article:11120959 | lifeskim:mentions | umls-concept:C0060636 | lld:lifeskim |
| pubmed-article:11120959 | pubmed:issue | 1 | lld:pubmed |
| pubmed-article:11120959 | pubmed:dateCreated | 2001-2-5 | lld:pubmed |
| pubmed-article:11120959 | pubmed:abstractText | (-)-beta-D-2,6-Diaminopurine dioxolane (DAPD), is a nucleoside reverse transcriptase (RT) inhibitor with activity against human immunodeficiency virus type 1 (HIV-1). DAPD, which was designed as a water-soluble prodrug, is deaminated by adenosine deaminase to give (-)-beta-D-dioxolane guanine (DXG). By using calf adenosine deaminase a K(m) value of 15 +/- 0.7 microM was determined for DAPD, which was similar to the K(m) value for adenosine. However, the k(cat) for DAPD was 540-fold slower than the k(cat) for adenosine. In CEM cells and peripheral blood mononuclear cells exposed to DAPD or DXG, only the 5'-triphosphate of DXG (DXG-TP) was detected. DXG-TP is a potent alternative substrate inhibitor of HIV-1 RT. Rapid transient kinetic studies show the efficiency of incorporation for DXG-TP to be lower than that measured for the natural substrate, 2'-deoxyguanosine 5'-triphosphate. DXG-TP is a weak inhibitor of human DNA polymerases alpha and beta. Against the large subunit of human DNA polymerase gamma a K(i) value of 4.3 +/- 0.4 microM was determined for DXG-TP. DXG showed little or no cytotoxicity and no mitochondrial toxicity at the concentrations tested. | lld:pubmed |
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| pubmed-article:11120959 | pubmed:language | eng | lld:pubmed |
| pubmed-article:11120959 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:11120959 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:11120959 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:11120959 | pubmed:month | Jan | lld:pubmed |
| pubmed-article:11120959 | pubmed:issn | 0066-4804 | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:ChiC WCW | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:FurmanP APA | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:SchinaziR FRF | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:HillEE | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:AndersonK SKS | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:SommadossiJ... | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:CopelandW CWC | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:LibermanII | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:JeffreyJJ | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:PainterG RGR | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:Borroto-Esoda... | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:FengJ YJY | lld:pubmed |
| pubmed-article:11120959 | pubmed:author | pubmed-author:KieferL LLL | lld:pubmed |
| pubmed-article:11120959 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:11120959 | pubmed:volume | 45 | lld:pubmed |
| pubmed-article:11120959 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:11120959 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:11120959 | pubmed:pagination | 158-65 | lld:pubmed |
| pubmed-article:11120959 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
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| pubmed-article:11120959 | pubmed:year | 2001 | lld:pubmed |
| pubmed-article:11120959 | pubmed:articleTitle | Mechanism of action of 1-beta-D-2,6-diaminopurine dioxolane, a prodrug of the human immunodeficiency virus type 1 inhibitor 1-beta-D-dioxolane guanosine. | lld:pubmed |
| pubmed-article:11120959 | pubmed:affiliation | Triangle Pharmaceuticals, Durham, North Carolina 27707, USA. furmanpa@tripharm.com | lld:pubmed |
| pubmed-article:11120959 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:11120959 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| pubmed-article:11120959 | pubmed:publicationType | Research Support, U.S. Gov't, Non-P.H.S. | lld:pubmed |
| pubmed-article:11120959 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
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