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1.
001-es BibID:
BIBFORM060641
Első szerző:
Lee, K. N.
Cím:
Development of selective inhibitors of transglutaminase : phenylthiourea derivatives / K. N. Lee, L. Fesus, S. T. Yancey, J. E. Girard, S. I. Chung
Dátum:
1985
Megjegyzések:
For the purpose of developing a transglutaminase inhibitor which could be effective in physiological and pharmacological studies, a series of phenylthiourea derivatives of alpha, omega-diaminoalkanes were designed, synthesized, and evaluated kinetically as inhibitors of transglutaminases. A homologous series of compounds of the structure phenylthiourea-(CH2)n-NH2, where n = 2, 3, 4, 5, and 6, were tested for the inhibition of both guinea pig liver transglutaminase-catalyzed amine incorporation into various glutamine-containing substrates and plasma transglutaminase (factor XIIIa)-catalyzed amine incorporation into fibrin and fibrin cross-linking. It was found that the inhibitory activity of the compounds increases with increasing number of methylene groups in the side chain up to a maximum of n = 5. A further increase in the length of the methylene side chain to n = 6 results in decreased activity. The Ki value (4.9 X 10(-5) M) of 1-(5-aminopentyl)-3-phenylthiourea (PPTU) (n = 5) for the inhibition of guinea pig transglutaminase-catalyzed amine incorporation into the B chain of oxidized insulin is in close agreement to its Km(app) value (7.1 X 10(-5) M) obtained using 14C-labeled PPTU. PPTU was also found to be a potent inhibitor of plasma transglutaminase-catalyzed fibrin cross-linking. The finding that the specificity of the alkylamines for inhibition is correlated with the length of their methyl side chains is compatible with those reported for aliphatic amines and monodansylcadaverine analogues (where dansyl is 5-dimethylaminonaphthalene-1-sulfonyl). The phenylthiourea derivatives, however, are far less toxic in mice than monodansylcadaverine as indicated by their LD50 values: PPTU, 400 +/- 25 mg/kg; and monodansylcadaverine, 160 +/- 20 mg/kg.
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Orvostudományok
Elméleti orvostudományok
idegen nyelvű folyóiratközlemény külföldi lapban
Megjelenés:
Journal of Biological Chemistry 260 : 27 (1985), p. 14689-14694. -
További szerzők:
Fésüs László (1947-) (orvos biokémikus)
Yancey, S. T.
Girard, James E.
Chung, Soo Il
Internet cím:
Intézményi repozitóriumban (DEA) tárolt változat
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2.
001-es BibID:
BIBFORM060633
Első szerző:
Lee, Kyung No
Cím:
Evaluation of phenylthiourea derivatives as inhibitors of transglutaminase-catalyzed reaction in Chinese hamster ovary cells / Kyung No Lee, Soo Il Chung, James E. Girard, Laszlo Fesus
Dátum:
1988
ISSN:
0167-4889
Megjegyzések:
1-(5-Aminopentyl)-3-phenylthiourea (PPTU), a recently developed inhibitor of the transglutaminase-catalyzed reaction (K.N. Lee, L. Fesus, S.T. Yancey, J.E. Girard, and S.I. Chung, (1985) J. Biol. Chem. 260, 14689-14694) was evaluated as a possible probe to examine the physiological role of transglutaminase (EC 2.3.2.13) in Chinese hamster ovary (CHO) cells. The [14C]PPTU in cell culture was readily taken up by CHO cells and was found to be covalently attached to high-molecular-weight proteins which are associated with the particulate fractions. Incubating cell homogenates, in the presence of Ca2+, incorporated the labeled PPTU exclusively into high-molecular-weight proteins that were also undergoing polymerization. PPTU at 0.1 mM, a concentration close to the Ki value reported for inhibition of tissue transglutaminase-catalyzed amine incorporation into the B chain of oxidized insulin, decreased high-molecular-weight protein polymerization, whereas PPTU at the same concentrations showed no effect on CHO cell proliferation or on in vitro calmodulin activation of cyclic nucleotide phosphodiesterase. These results suggest that transglutaminase may not be a constitutive enzyme in cell proliferation.
Tárgyszavak:
Orvostudományok
Elméleti orvostudományok
idegen nyelvű folyóiratközlemény külföldi lapban
Transglutaminase
1-(5-Aminopentyl)-3-phenylthiourea
Cell proliferation
Chinese hamster ovary cell
Megjelenés:
Biochimica et Biophysica Acta (BBA). Molecular Cell Research. - 972 : 2 (1988), p. 120-130. -
További szerzők:
Chung, Soo Il
Girard, James E.
Fésüs László (1947-) (orvos biokémikus)
Internet cím:
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