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Page 1
The Role of the DNA Backbone in Minor-Groove Ligand Binding.
Díaz-Gómez DG, Galindo-Murillo R, Cortés-Guzmán F. Díaz-Gómez DG, et al. Chemphyschem. 2017 Jul 19;18(14):1909-1915. doi: 10.1002/cphc.201700260. Epub 2017 May 29. Chemphyschem. 2017. PMID: 28463411
Herein, we determined the specific interactions between the binder CGP 40215A and the minor-groove atoms, based on the local properties of electron density. ...
Herein, we determined the specific interactions between the binder CGP 40215A and the minor-groove atoms, based on the local p …
In vivo trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors.
Bacchi CJ, Brun R, Croft SL, Alicea K, Bühler Y. Bacchi CJ, et al. Antimicrob Agents Chemother. 1996 Jun;40(6):1448-53. doi: 10.1128/AAC.40.6.1448. Antimicrob Agents Chemother. 1996. PMID: 8726018 Free PMC article.
Curative combinations were 14 days of oral 2% DFMO (approximately 5 g/kg/day) plus 5, 10, or 25 mg/kg/day for 3 or 7 days given by intraperitoneal injection or with a miniosmotic pump. Combinations were most effective if CGP 40215A was given in the second half or at …
Curative combinations were 14 days of oral 2% DFMO (approximately 5 g/kg/day) plus 5, 10, or 25 mg/kg/day for 3 or 7 days given by intraperi …
3-Aminooxy-1-aminopropane and derivatives have an antiproliferative effect on cultured Plasmodium falciparum by decreasing intracellular polyamine concentrations.
Das Gupta R, Krause-Ihle T, Bergmann B, Müller IB, Khomutov AR, Müller S, Walter RD, Lüersen K. Das Gupta R, et al. Antimicrob Agents Chemother. 2005 Jul;49(7):2857-64. doi: 10.1128/AAC.49.7.2857-2864.2005. Antimicrob Agents Chemother. 2005. PMID: 15980361 Free PMC article.
While the effects of the ODC inhibitors were completely abolished by the addition of putrescine, growth inhibition by the AdoMetDC inhibitor CGP 40215A could not be antagonized by putrescine or spermidine. Moreover, CGP 40215A did not affect the cellul …
While the effects of the ODC inhibitors were completely abolished by the addition of putrescine, growth inhibition by the AdoMetDC inhibitor …
Antileishmanial effect of a potent S-adenosylmethionine decarboxylase inhibitor: CGP 40215A.
Mukhopadhyay R, Kapoor P, Madhubala R. Mukhopadhyay R, et al. Pharmacol Res. 1996 Jan;33(1):67-70. doi: 10.1006/phrs.1996.0011. Pharmacol Res. 1996. PMID: 8817649
CGP 40215A, specific S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor was found to inhibit the growth of Leishmania donovani promastigotes (strain UR6) in a dose-dependent manner with an IC50 of 18 microM. ...The combination of CGP 40215A with o
CGP 40215A, specific S-adenosylmethionine decarboxylase (AdoMetDC) inhibitor was found to inhibit the growth of Leishmania don
In vitro trypanocidal activities of new S-adenosylmethionine decarboxylase inhibitors.
Brun R, Bühler Y, Sandmeier U, Kaminsky R, Bacchi CJ, Rattendi D, Lane S, Croft SL, Snowdon D, Yardley V, Caravatti G, Frei J, Stanek J, Mett H. Brun R, et al. Antimicrob Agents Chemother. 1996 Jun;40(6):1442-7. doi: 10.1128/AAC.40.6.1442. Antimicrob Agents Chemother. 1996. PMID: 8726017 Free PMC article.
Results obtained in three laboratories employing different methods and trypanosome populations consistently ranked compound CGP 40215A highest. This compound had a 50% inhibitory concentration of 0.0045 microM for Trypanosoma brucei rhodesiense, was also active agai …
Results obtained in three laboratories employing different methods and trypanosome populations consistently ranked compound CGP 40
Characterization of a novel DNA minor-groove complex.
Nguyen B, Hamelberg D, Bailly C, Colson P, Stanek J, Brun R, Neidle S, Wilson WD. Nguyen B, et al. Biophys J. 2004 Feb;86(2):1028-41. doi: 10.1016/s0006-3495(04)74178-8. Biophys J. 2004. PMID: 14747338 Free PMC article.
Para-substituted aromatic diamidines such as furamidine, which is currently being tested against trypanosomiasis in humans, and berenil, which is used in animals, are typical examples of this class. Recently, a meta-substituted diamidine, CGP 40215A, has been found …
Para-substituted aromatic diamidines such as furamidine, which is currently being tested against trypanosomiasis in humans, and berenil, whi …
Characterization of putrescine uptake in hamster amelanocytic melanoma AMEL-3 cells.
García-Fernández AJ, Rodríguez RA, Pérez-Pertejo Y, Balaña-Fouce R. García-Fernández AJ, et al. Mol Cells. 2005 Aug 31;20(1):127-35. Mol Cells. 2005. PMID: 16258251 Free article.
Putrescine, in turn, induced the negative expression of the carrier, thus suggesting that this influx mechanism is governed by up/down regulation. The cationic diamidine CGP 40215A and its analogue CGP039937A competitively inhibited putrescine transport, with Ki val …
Putrescine, in turn, induced the negative expression of the carrier, thus suggesting that this influx mechanism is governed by up/down regul …
Strong binding in the DNA minor groove by an aromatic diamidine with a shape that does not match the curvature of the groove.
Nguyen B, Lee MP, Hamelberg D, Joubert A, Bailly C, Brun R, Neidle S, Wilson WD. Nguyen B, et al. J Am Chem Soc. 2002 Nov 20;124(46):13680-1. doi: 10.1021/ja027953c. J Am Chem Soc. 2002. PMID: 12431090
A combination of biophysical techniques has been used to characterize the interaction of an antitrypanosomal agent, CGP 40215A, with DNA. The results from a broad array of methods (DNase I footprinting, surface plasmon resonance, X-ray crystallography, and molecular …
A combination of biophysical techniques has been used to characterize the interaction of an antitrypanosomal agent, CGP 40215A
Binding-linked protonation of a DNA minor-groove agent.
Nguyen B, Stanek J, Wilson WD. Nguyen B, et al. Biophys J. 2006 Feb 15;90(4):1319-28. doi: 10.1529/biophysj.105.071381. Epub 2005 Nov 18. Biophys J. 2006. PMID: 16299076 Free PMC article.
The energetics for binding of a diphenyl diamidine antitrypanosomal agent CGP 40215A to DNA have been studied by spectroscopy, isothermal titration calorimetry, and surface plasmon resonance biosensor methods. ...
The energetics for binding of a diphenyl diamidine antitrypanosomal agent CGP 40215A to DNA have been studied by spectroscopy, …
14 results