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See detailQuantitative Relationship between Sensitivity to Beta-Lactam Antibiotics and Beta-Lactamase Production in Gram-Negative Bacteria--II. Non-Steady-State Treatment and Progress Curves
Frère, Jean-Marie ULg; Joris, Bernard ULg; Crine, Michel ULg et al

in Biochemical Pharmacology (1989), 38(9), 1427-33

A non-steady-state model is discussed for the study of the interplay between beta-lactamase activity and outer membrane permeability with slowly hydrolysed beta-lactams. The analysis shows: (1) that the ... [more ▼]

A non-steady-state model is discussed for the study of the interplay between beta-lactamase activity and outer membrane permeability with slowly hydrolysed beta-lactams. The analysis shows: (1) that the simple, steady-state model presented in the accompanying paper remains valid as long as kcat (i.e. k3 with chromosome-encoded class C beta-lactamases) is larger than 10(-3)/sec (generation time = 20 min or more); (2) that among the beta-lactam antibiotics studied here, the complete, non-steady-state model needs only be used in the case of aztreonam; (3) that the term "trapping" should be replaced by "formation of a covalent acyl-enzyme" and that such a phenomenon only contributes significantly to the resistance when penetration and hydrolysis are very slow and the periplasmic beta-lactamase concentration is very high. Aztreonam seems to be the only compound which fulfils the first two conditions. [less ▲]

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See detailStructure-Activity Relationships in the Beta-Lactam Family: An Impossible Dream
Frère, Jean-Marie ULg; Joris, Bernard ULg; Varetto, Louis ULg et al

in Biochemical Pharmacology (1988), 37(1), 125-32

The difficulty of establishing structure-activity relationships in the beta-lactam family of antibiotics stems from the fact that: (1) The targets in various bacteria exhibit widely different ... [more ▼]

The difficulty of establishing structure-activity relationships in the beta-lactam family of antibiotics stems from the fact that: (1) The targets in various bacteria exhibit widely different sensitivities. (2) Some bacteria produce beta-lactamases, enzymes capable of destroying the antibiotics. The rates of the reactions with the beta-lactamases and the target enzymes are not necessarily related. (3) In Gram-negative bacteria, the diffusion rate through the outer membrane varies independently from the two other factors. [less ▲]

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See detailAutomated analysis of enzyme inactivation phenomena. Application to beta-lactamases and DD-peptidases.
De Meester, Fabien; Joris, Bernard ULg; Reckinger, Georges et al

in Biochemical Pharmacology (1987), 36

In the presence of a reporter substrate, the progressive inactivation of an enzyme was easily studied by directly transmitting absorbance readings to a microcomputer. Pseudo-first order rate constants as ... [more ▼]

In the presence of a reporter substrate, the progressive inactivation of an enzyme was easily studied by directly transmitting absorbance readings to a microcomputer. Pseudo-first order rate constants as high as 0.3 sec-1 were rapidly and accurately measured. When utilization of the reporter substrate did not exceed 10%, the rate of the reaction (vt) could be considered as proportional to the active enzyme concentration at any time during the analysis and the decrease of vt was first order with time. This simple method was used to follow the inactivation of beta-lactamases (EC 3.5.2.6) by various physical and chemical agents. When a large proportion (30-80%) of reporter substrate was destroyed, a correction was introduced to account for the corresponding decrease of its rate of utilization. This enabled experiments to be performed with a DD-peptidase and a substrate exhibiting a low delta epsilon upon hydrolysis. For the first time, the inactivation of a penicillin-sensitive enzyme by a beta-lactam could be continuously and directly observed. Finally, the method was extended to the study of hysteresis phenomena. [less ▲]

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See detailIn vitro degradation of the four isomers of Soman in human serum
De Bisschop, H. C.; Mainil, Jacques ULg; Willems, J. L.

in Biochemical Pharmacology (1985), 34

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See detailConformational analysis of the calcium-antagonist gallopamil.
Brasseur, Robert ULg; Deleers, M.; Malaisse, W. J.

in Biochemical Pharmacology (1983), 32(3), 437-40

Conformational analysis of gallopamil was performed in order to gain insight into the molecular determinant of its calcium-antagonistic property. Whereas the neutral form of gallopamil was characterized ... [more ▼]

Conformational analysis of gallopamil was performed in order to gain insight into the molecular determinant of its calcium-antagonistic property. Whereas the neutral form of gallopamil was characterized by a single, largely predominant configuration, the protonated form of the drugs yielded several conformers, some of which were characterized by a readily accessible ionized site. The capacity of gallopamil to inhibit ionophore-mediated calcium translocation in a two-phase bulk system was inversely related to the pH of the aqueous phase. These findings indicate that the capacity of gallopamil to interfere with the transport of cations is critically dependent on the availability of a protonated configuration of the drug. [less ▲]

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See detailMode of action of cis-dichloro-diammine platinum(II) on mouse Ehrlich ascites tumour cells.
Heinen, Ernst ULg; Bassleer, R.

in Biochemical Pharmacology (1976), 25(16), 1871-5

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See detailEffects of procaine and d-tubocurarine on the activity of membrane bound acetylcholinesterase
Foidart, Jean-Michel ULg; Gridelet, J.

in Biochemical Pharmacology (1974), 23

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See detailComparative study of the effects of ethidium bromide and DNA-ethidium bromide complex on normal and cancer cells.
Heinen, Ernst ULg; Bassleer, R.; Calberg-Bacq, C. M. et al

in Biochemical Pharmacology (1974), 23(10), 1549-51

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See detailEffet de la mescaline, du lsd 25 et de dérivés de l'adrenochrome sur la décarboxlyase glutamique du cerveau
Deltour, G. H.; Ghuysen, Jean-Marie ULg; Claus, A.

in Biochemical Pharmacology (1959), 1(4), 267-272

The inhibitory effect of adrenochrome on glutamic decarboxylase from brain homogenates in vitro, does not occur with mescaline and LSD 25. Certain stable derivatives of adrenochrome such as MSCA and AHA ... [more ▼]

The inhibitory effect of adrenochrome on glutamic decarboxylase from brain homogenates in vitro, does not occur with mescaline and LSD 25. Certain stable derivatives of adrenochrome such as MSCA and AHA, in which the quinonic function is blocked, have an opposite effect, and behave like activators of brain glutamic decarboxylase. This activation seems to be indirect; MSCA and AHA do not constitute new coenzymes. [less ▲]

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