Zobrazeno 1 - 10
of 15
pro vyhledávání: '"Magdalena R. Mejillano"'
Publikováno v:
Biochemistry. 39:10269-10274
We have determined the binding affinity for binding of the four purine nucleoside triphosphates GTP, ITP, XTP, and ATP to E-site nucleotide- and nucleoside diphosphate kinase-depleted tubulin. The relative binding affinities are 3000 for GTP, 10 for
Autor:
Zacharia S. Cheruvallath, Gunda I. Georg, Magdalena R. Mejillano, Richard H. Himes, Charles T. Burke
Publikováno v:
ChemInform. 24
Taxol (1) is a highly potent antitumor agent, exerting its mechanism of action by promoting the assembly of stable microtubules in cells. We are reporting on the first synthesis and biological evaluation of taxol derivatives with substituted phenyl r
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:1751-1754
The semisynthesis of the four novel taxol analogues baccatin III 13-(N-benzoyl-(2′R,3′S)-3′-(p-tolyl)isoserinate) ( 2 ), baccatin III 13-(N-(p-toluoyl)-(2′R,3′S)-3′-phenylisoserinate) ( 3 ), baccatin III 13-(N-benzoyl-(2′R,3′S)-3′(p
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:735-738
An efficient semi-synthetic approach utilizing the appropriately functionalized (3R,4S)-3-hydroxy-4-phenyl-2-azetidinone ( 4 ) and 7-(p-azidobenzoyl)baccatin III ( 3 ) is described which leads to the targeted biologically active taxol photoaffinity l
Publikováno v:
Biochemistry. 31:3478-3483
In a recent study, we demonstrated that the conversion of carboxyl residues in the C-termini of tubulin to neutral amides with glycine ethyl ester enhanced the ability of the protein to assemble into microtubules and decreased its interaction with mi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 2:295-298
Two novel taxol analogues, baccatin III 13-(N-(p-chlorobenzoyl)-(2′R,3′S)-phenylisoserinate) ( 2 ) and baccatin III 13-(N-benzoyl-(2′R,3′S)-3′(p-chlorophenyl)isoserinate) ( 3 ) were synthesized from 7-triethylsilyl baccatin III ( 4 ) and N-
Publikováno v:
Archives of Biochemistry and Biophysics. 291:356-362
Binding of GTP and GDP to tubulin in the presence or absence of Mg2+ was measured following depletion of the exchangeable site--(E-site) nucleotide. The E-site nucleotide was displaced with a large molar excess of the nonhydrolyzable GTP analogue, GM
Autor:
Magdalena R. Mejillano, Zacharia S. Cheruvallath, Charles T. Burke, Gunda I. Georg, Richard H. Himes
Publikováno v:
Journal of medicinal chemistry. 35(22)
Taxol (1) is a highly potent antitumor agent, exerting its mechanism of action by promoting the assembly of stable microtubules in cells. We are reporting on the first synthesis and biological evaluation of taxol derivatives with substituted phenyl r
Autor:
Jyoti P. Nath, Richard H. Himes, Abraham E. Mathew, Valentino J. Stella, Magdalena R. Mejillano
Publikováno v:
Journal of medicinal chemistry. 35(1)
The synthesis and evaluation of some 2'- and 7-amino acid derivatives of taxol (1) are reported. Reaction of taxol with N-protected amino acids gave 2'-N-protected amino acid esters of taxol. However, deprotection of the amino group and subsequent is
Publikováno v:
Biochemistry. 29(5)
The question of whether nonhydrolyzable nucleotide analogues and other nucleoside triphosphates support tubulin assembly was addressed. Tubulin which contained residual GTP at the exchangeable site polymerized in the absence of added GTP in the prese