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  1. No Access

    Article

    Carrier Mechanisms Involved in the Transepithelial Transport of bis(POM)-PMEA and Its Metabolites Across Caco-2 Monolayers

    Purpose. To investigate the role of carrier mechanisms in: [1] the polarized transport of the bis(pivaloyloxymethyl)- [bis(POM)-] ester prodrug of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] a...

    P. Annaert, J. Van Gelder, L. Naesens, E. De Clercq… in Pharmaceutical Research (1998)

  2. No Access

    Article

    Comparison of the Disposition of Ester Prodrugs of the Antiviral Agent 9-(2-phosphonylmethoxyethyl)adenine [PMEA] in Caco-2 Monolayers

    Purpose. To evaluate the potential of several bis-ester prodrugs of the antiviral agent 9-(2-phosphonylmethoxyethyl)adenine (PMEA, adefovir) to enhance the oral absorption of PMEA.

    P. Annaert, G. Gosselin, A. Pompon, S. Benzaria, G. Valette… in Pharmaceutical Research (1998)

  3. No Access

    Chapter

    Metabolism of Eicar (5-Ethynyl-1-β-D- Ribofuranosylimidazole-4-Carboxamide),A Potent Inhibitor of Inosinate Dehydrogenase

    The cytostatic agent 5-ethynyl-l-β-D-ribofuranosylimidazole-4-carboxamide (EICAR) causes a rapid and marked inhibition of inosinate (IMP) dehydrogenase activity in intact tumor cells. [3H]EICAR is metabolised in ...

    J. Balzarini, L. Stet, A. Matsuda, L. Wiebe… in Purine and Pyrimidine Metabolism in Man IX (1998)

  4. No Access

    Chapter

    Metabolism and Anti-HIV Activity of Phosphoramidate Derivatives of D4T-MP with Variations in the Amino Acid Moiety

    The metabolism of different phosphoramidate prodrugs of d4T-MP, in which the phosphate group is linked to a phenyl group and the alkyl ester of an amino acid was studied in crude CEM cell extracts. Significant...

    L. Naesens, D. Cahard, A. Salgado, L. Bidois… in Purine and Pyrimidine Metabolism in Man IX (1998)

  5. No Access

    Chapter

    In Vitro and in Vivo Inhibitory Activity of the Differentiation-Inducing Agent 9-(2-Phosphonylmethoxyethyl)Adenine (Pmea) Against Rat Choriocarcinoma

    The acyclic nucleoside phosphonate 9-(2-phosphonylmethoxyethyl)adenine (PMEA) has previously been shown to be a strong inducer of differentiation in several tumor cell lines. We have now investigated the in vitro

    S. Hatse, L. Naesens, B. Degrève… in Purine and Pyrimidine Metabolism in Man IX (1998)

  6. No Access

    Chapter and Conference Paper

    Anti-HIV Agents Interfering with the Viral gp120-Cellular CD4 Interaction

    The high affinity interaction of the viral envelope glycoprotein gp120 with the cellular CD4 receptor accounts for the tropism of human immunodeficiency virus (HIV) for CD4+ cells [1] and represents an important ...

    D. Schols, E. De Clercq in Molecular Aspects of Chemotherapy (1992)

  7. No Access

    Chapter

    Conversion of Acyclic Nucleoside Phosphonates to Their Diphosphate Derivatives by 5-Phosphoribosyl-1-Pyrophosphate (PRPP) Synthetase

    Recently, we discovered a group of acyclic nucleoside phosphonate derivatives with potent and selective activity against a broad spectrum of DNA viruses (1,2). The prototype compound of this new class of compo...

    J. Balzarini, E. de Clercq in Purine and Pyrimidine Metabolism in Man VII (1991)

  8. No Access

    Article

    Alopecia in laboratory animals induced by a polyampholyte, polyethylene alanine

    Polyethylene alanine, a polyaminoacid, was found to induce a characteristic alopecia when administered topically or systemically to suckling mice, or newborn guinea-pigs or rabbits.

    E. De Clercq, J. Descamps, P. De Somer, C. Samyn, G. Smets in Experientia (1980)