Bernard Testa

Summary

Affiliation: Centre Hospitalier Universitaire Vaudois
Country: Switzerland

Publications

  1. doi Drug metabolism for the perplexed medicinal chemist
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 6:2055-70. 2009
  2. ncbi Lessons learned from marketed and investigational prodrugs
    Peter Ettmayer
    Novartis Institute for Biomedical Research, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 47:2393-404. 2004
  3. ncbi Prodrug research: futile or fertile?
    Bernard Testa
    Pharmacy Department, University Hospital Centre, CHUV BH 04, 46 Rue du Bugnon, CH 1011 Lausanne, Switzerland
    Biochem Pharmacol 68:2097-106. 2004
  4. ncbi Musings on ADME predictions and structure-activity relations
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 2:1411-27. 2005
  5. ncbi The biochemistry of drug metabolism--an introduction: part 1. Principles and overview
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 3:1053-101. 2006
  6. doi Simulations in evolution. III. Randomness as a generator of opportunities
    Bernard Testa
    Department of Pharmacy, Lausanne University Hospital, BH04 CHUV, Rue du Bugnon 41, CH 1011 Lausanne, Switzerland
    Chem Biodivers 10:62-72. 2013
  7. doi Reactions and enzymes in the metabolism of drugs and other xenobiotics
    Bernard Testa
    Service of Pharmacy, Lausanne University Hospital, Switzerland
    Drug Discov Today 17:549-60. 2012
  8. ncbi Variation, natural selection, and information content--a simulation
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon 41, CH 1011 Lausanne
    Chem Biodivers 4:2458-72. 2007
  9. ncbi The biochemistry of drug metabolism--an introduction: part 3. Reactions of hydrolysis and their enzymes
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 4:2031-122. 2007
  10. ncbi The biochemistry of drug metabolism--an introduction: Part 2. Redox reactions and their enzymes
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 4:257-405. 2007

Collaborators

Detail Information

Publications30

  1. doi Drug metabolism for the perplexed medicinal chemist
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 6:2055-70. 2009
    ..The conclusion is that oxidoreductases are the main enzymes responsible for the formation of toxic or active metabolites, whereas transferases play the major role in producing inactive and nontoxic metabolites...
  2. ncbi Lessons learned from marketed and investigational prodrugs
    Peter Ettmayer
    Novartis Institute for Biomedical Research, Brunnerstrasse 59, A 1235 Vienna, Austria
    J Med Chem 47:2393-404. 2004
  3. ncbi Prodrug research: futile or fertile?
    Bernard Testa
    Pharmacy Department, University Hospital Centre, CHUV BH 04, 46 Rue du Bugnon, CH 1011 Lausanne, Switzerland
    Biochem Pharmacol 68:2097-106. 2004
    ..We conclude that prodrugs offer a viable strategy to disentangle pharmacodynamic and pharmacokinetic optimization...
  4. ncbi Musings on ADME predictions and structure-activity relations
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 2:1411-27. 2005
    ..Most significantly in an ADME perspective, the molecule is able, within the limits of its property space, to adapt to the medium. This is equivalent to saying that the medium constrains the molecule to resemble it as much as feasible...
  5. ncbi The biochemistry of drug metabolism--an introduction: part 1. Principles and overview
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 3:1053-101. 2006
  6. doi Simulations in evolution. III. Randomness as a generator of opportunities
    Bernard Testa
    Department of Pharmacy, Lausanne University Hospital, BH04 CHUV, Rue du Bugnon 41, CH 1011 Lausanne, Switzerland
    Chem Biodivers 10:62-72. 2013
    ..This increase in information content is interpreted as facilitated adaptability of the population...
  7. doi Reactions and enzymes in the metabolism of drugs and other xenobiotics
    Bernard Testa
    Service of Pharmacy, Lausanne University Hospital, Switzerland
    Drug Discov Today 17:549-60. 2012
    ..Thus, there is a need for several drug discovery scientists to better grasp the variety of drug metabolism reactions and enzymes and their consequences...
  8. ncbi Variation, natural selection, and information content--a simulation
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon 41, CH 1011 Lausanne
    Chem Biodivers 4:2458-72. 2007
    ..In other words, variation acting alone progressively decreased the information content of a population. When both factors, F and Y, were applied simultaneously, their relative weight determined the progressive change in SE...
  9. ncbi The biochemistry of drug metabolism--an introduction: part 3. Reactions of hydrolysis and their enzymes
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 4:2031-122. 2007
  10. ncbi The biochemistry of drug metabolism--an introduction: Part 2. Redox reactions and their enzymes
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 4:257-405. 2007
    ..g., flavin-containing monooxygenases, amine oxidases, molybdenum hydroxylases, peroxidases, and the innumerable dehydrogenases/reductases...
  11. doi Prodrugs: bridging pharmacodynamic/pharmacokinetic gaps
    Bernard Testa
    Pharmacy Department, University Hospital Centre, CHUV BH 04, 46 Rue du Bugnon, CH 1011 Lausanne, Switzerland
    Curr Opin Chem Biol 13:338-44. 2009
    ..New antimicrobial agents are also in the pipeline. In addition, biooxidative bioprecursors offer a promising strategy in specific cases, as illustrated by the successful antiaggregating agent clopidogrel...
  12. ncbi Predicting drug metabolism--an evaluation of the expert system METEOR
    Bernard Testa
    Institute of Medicinal Chemistry, University of Lausanne, CH 1015 Lausanne
    Chem Biodivers 2:872-85. 2005
    ..The predictions for four representative substrates are presented in detail (Figs. 1-4), illustrating the interest of such an evaluation in identifying where and how predictive rules can be improved...
  13. doi The biochemistry of drug metabolism--an introduction: part 5. Metabolism and bioactivity
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, Lausanne
    Chem Biodivers 6:591-684. 2009
    ..But, far from being concerned only with individual cases, the review is based on broad classifications, global rationalizations, and synthetic hypotheses...
  14. doi The biochemistry of drug metabolism--an introduction: part 4. reactions of conjugation and their enzymes
    Bernard Testa
    Department of Pharmacy, University Hospital Centre CHUV, Rue du Bugnon, CH 1011 Lausanne
    Chem Biodivers 5:2171-336. 2008
    ..Nonenzymatic reactions, mainly of glutathione conjugation, also receive due attention. A number of medicinally, environmentally, and toxicologically relevant examples are presented and discussed...
  15. doi Atomic diversity, molecular diversity, and chemical diversity: the concept of chemodiversity
    Bernard Testa
    Department of Pharmacy, University Hospital Center CHUV, Lausanne
    Chem Biodivers 6:1145-51. 2009
    ..In other words, chemodiversity is the material condition for life to emerge and exist. Increasing our knowledge of chemodiversity is thus a condition for a better understanding of life as a process...
  16. ncbi Development of an in vitro rat intestine segmental perfusion model to investigate permeability and predict oral fraction absorbed
    Marc Etienne Castella
    LCT Pharmacochemistry, School of Pharmaceutical Sciences, EPGL, University of Geneva, University of Lausanne, 30, Quai Ernest Ansermet, CH 1211, Geneva 4, Switzerland
    Pharm Res 23:1543-53. 2006
    ..The aims of the study are to develop and evaluate an in vitro rat intestine segmental perfusion model for the prediction of the oral fraction absorbed of compounds and to assess the ability of the model to study intestinal metabolism...
  17. doi Lack of enantioselectivity in the SULT1A3-catalyzed sulfoconjugation of normetanephrine enantiomers: an in vitro and computational study
    Eric Grouzmann
    Service de biomédecine, Lausanne University Hospital, Lausanne, Switzerland
    Chirality 25:28-34. 2013
    ..In conclusion, SULT1A3 is not substrate-enantioselective toward normetanephrine, an unexpected finding explainable by a mutual adaptability between the ligands and SULT1A3 through an "induced-fit model" in the catalytic pocket...
  18. doi Simulations in evolution. II. Relative fitness and the propagation of mutants
    Bernard Testa
    Department of Pharmacy, University of Lausanne, Hospital Centre, Rue du Bugnon 41, Lausanne
    Chem Biodivers 6:356-68. 2009
    ..The results of these simulations illustrate, in a graphically didactic manner, the influence of natural selection, operating through relative fitness, in the emergence and dominance of a fitter mutant...
  19. ncbi Liposome/water lipophilicity: methods, information content, and pharmaceutical applications
    Georgette Plemper van Balen
    Institut de chimie thérapeutique, Section de Pharmacie, Universite de Lausanne, CH 1015 Lausanne, Switzerland
    Med Res Rev 24:299-324. 2004
    ..In the conclusion, we summarize the interests and limitations of this technology and point to promising developments...
  20. ncbi Quantitative structure-permeation relationships (QSPeRs) to predict skin permeation: a critical evaluation
    Sandrine Geinoz
    Institute of Medicinal Chemistry, BEP, University of Lausanne, CH 1015 Lausanne, Switzerland
    Pharm Res 21:83-92. 2004
    ..Development of reliable mathematical models to predict skin permeability remains a challenging objective. This article examines some of the existing algorithms and critically evaluates their statistical relevance...
  21. ncbi Studies of ligand diffusion pathways over a protein surface
    Lemont B Kier
    Institute of Medicinal Chemistry, University of Lausanne, CH 1015 Lausanne, Switzerland
    J Chem Inf Comput Sci 43:255-8. 2003
    ..These findings have relevance to observations about the mechanism of action of nonspecific anesthetic agents...
  22. ncbi Quantitative structure-permeation relationships for solute transport across silicone membranes
    Sandrine Geinoz
    Institut de chimie thérapeutique, BEP, Université de Lausanne CH 1015, Lausanne, Switzerland
    Pharm Res 19:1622-9. 2002
    ..The purpose of this work was to assess the molecular properties that influence solute permeation across siliconemembranes and to compare the results with transport across human skin...
  23. ncbi Predicting the oxidative metabolism of statins: an application of the MetaSite algorithm
    Giulia Caron
    Dipartimento di Scienza e Tecnologia del Farmaco, Via Giuria 9, 10125 Torino, Italy
    Pharm Res 24:480-501. 2007
    ..This study was undertaken to examine the MetaSite algorithm by comparing its predictions with experimentally characterized metabolites of statins produced by cytochromes P450 (CYPs)...
  24. doi Assessing drug-likeness--what are we missing?
    Giulio Vistoli
    Istituto di Chimica Farmaceutica Pietro Pratesi, Facolta di Farmacia, Universita di Milano, Via Mangiagalli 25, I 20133 Milano, Italy
    Drug Discov Today 13:285-94. 2008
    ..Molecular sensitivity (namely, how much a given computable physicochemical property varies as a function of flexibility) appears as a promising descriptor to encode some of the information contained in molecular property spaces...
  25. ncbi The conformational and property space of acetylcholine bound to muscarinic receptors: an entropy component accounts for the subtype selectivity of acetylcholine
    Giulio Vistoli
    Istituto di Chimica Farmaceutica Pietro Pratesi, Facolta di Farmacia, Universita di Milano, Viale Abruzzi 42, I 20131 Milano, Italy
    Arch Biochem Biophys 464:112-21. 2007
    ..This finding suggests that the selectivity profile of acetylcholine for the M(2) receptor is largely entropy-driven, a fact that might explain the intrinsic difficulty to design subtype-selective muscarinic agonists...
  26. ncbi Homology modeling of human serum carnosinase, a potential medicinal target, and MD simulations of its allosteric activation by citrate
    Giulio Vistoli
    Istituto di Chimica Farmaceutica, Facolta di Farmacia, Universita di Milano, Viale Abruzzi 42, I 20131 Milano, Italy
    J Med Chem 49:3269-77. 2006
    ..e., binding score) of carnosine to the catalytic site. This is one of the first reports documenting the molecular mechanism of an allosteric enzyme activator using MD simulations...
  27. ncbi Solvent constraints on the property space of acetylcholine. I. Isotropic solvents
    Giulio Vistoli
    Istituto di Chimica Farmaceutica, Facolta di Farmacia, Universita di Milano, Viale Abruzzi 42, I 20131 Milano, Italy
    J Med Chem 48:1759-67. 2005
    ..Solvent constraints on the property space clearly indicate that a polar medium tends to favor polar conformers, whereas the opposite is true for a solvent of low polarity...
  28. ncbi Theoretical and experimental exploration of the lipophilicity of zwitterionic drugs in the 1,2-dichloroethane/water system
    Géraldine Bouchard
    Institut de chimie thérapeutique, Universite de Lausanne, Switzerland
    Pharm Res 19:1150-9. 2002
    ..This work examines the lipophilic behavior of various zwitterions and shows how distribution profiles in biphasic systems and ionic partition diagrams may improve our understanding of pH-absorption profiles of drugs...
  29. ncbi Lipophilicity and solvation of anionic drugs
    Géraldine Bouchard
    Institut de Chimie Thérapeutique Université de Lausanne, BEP, 1015 Lausanne, Switzerland
    Chemistry 8:3478-84. 2002
    ....
  30. ncbi The relative partitioning of neutral and ionised compounds in sodium dodecyl sulfate micelles measured by micellar electrokinetic capillary chromatography
    Agnes Taillardat-Bertschinger
    Institut de chimie thérapeutique, Section de Pharmacié Universitéde Lausanne, CH 1015 Lausanne, Switzerland
    Eur J Pharm Sci 15:225-34. 2002
    ....