Zobrazeno 1 - 10
of 32
pro vyhledávání: '"S. Jane deSolms"'
Autor:
J. Christopher Culberson, Steven M. Pitzenberger, Charles A. Omer, Michael J. Bogusky, Scott D. Mosser, Kenneth S. Koblan, S. Jane Desolms, E A Giuliani
Publikováno v:
Protein Science. 4:681-688
Farnesyl-protein transferase (FPTase) catalyzes the posttranslational farnesylation of the cysteine residue located in the carboxyl-terminal tetrapeptide of the Ras oncoprotein. Prenylation of this residue is essential for the membrane association an
Autor:
Anthony W. Shaw, S. Jane Desolms
Publikováno v:
Tetrahedron Letters. 42:7173-7176
Organometallic addition to tert -butanesufinyl ketimines derived from diaryl and aryl-heteroaryl ketones provided the corresponding α,α-diaryl and α-aryl-α-heteroaryl alkylamines in good yield with high diastereoselectivity. In many cases, imine
Autor:
John S. Wai, Jiunn H. Lin, Cuyue Tang, William E Neway, Christopher J. Dinsmore, Masato Chiba, S. Jane Desolms, Theresa M. Williams
Publikováno v:
Biochemical Pharmacology. 62:773-776
Methyl substitution at the 2-position of the imidazole ring greatly improved drug metabolism profiles, in human liver microsomes, of ras farnesyl-protein transferase inhibitor (FTI) candidates for drug development. Methyl substitution markedly reduce
Autor:
Joseph P. Davide, Robert B. Lobell, Kelly Hamilton, Kenneth S. Koblan, Ronald G. Robinson, Nancy E. Kohl, S. Jane Desolms, Samuel L. Graham, S. C. Mactough, John H. Hutchinson, Anthony W. Shaw, Terrence M. Ciccarone, Marc Abrams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1257-1260
Imidazolemethyl diaryl ethers are potent inhibitors of farnesyl-protein transferase. The SNAr displacement reaction used to prepare these diaryl ethers was amenable to rapid parallel synthesis of FPTase inhibitors. The use of a broad range of commerc
Autor:
Michael J. Breslin, Kelly Hamilton, Samuel L. Graham, E A Giuliani, G. E. Stokker, David L. Pompliano, John H. Hutchinson, Scott D. Mosser, S. Jane Desolms
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3311-3316
The structure-activity relationship of a series of non-thiol CaaX analogs, which are inhibitors of farnesyltransferase, is described. These inhibitors contain a substituted phenyl group at the N terminus, which may occupy a novel binding domain on th
Autor:
Jackson B. Gibbs, Oliff Allen I, S. Jane Desolms, Laura Sepp-Lorenzino, Kenneth S. Koblan, Nancy E. Kohl, Neal Rosen, Michael W. Conner, Samuel L. Graham, Theresa M. Williams, Charles A. Omer, George D. Hartman, Neville J. Anthony
Publikováno v:
Breast Cancer Research and Treatment. 38:75-83
The oncoprotein encoded by mutant ras genes is initially synthesized as a cytoplasmic precursor which requires posttranslational processing to attain biological activity; farnesylation of the cysteine residue present in the CaaX motif located at the
Autor:
Nancy E. Kohl, Charles A. Omer, Michael W. Conner, Neville J. Anthony, Joseph P. Davide, S. Jane Desolms, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Kelly Hamilton, Laurence K. Handt, George D. Hartman, Kenneth S. Koblan, Astrid M. Kral, Patricia J. Miller, Scott D. Mosser, Timothy J. O'Neill, Elaine Rands, Michael D. Schaber, Jackson B. Gibbs, Allen Oliff
Publikováno v:
Nature Medicine. 1:792-797
For Ras oncoproteins to transform mammalian cells, they must be post-translationally modified with a farnesyl group in a reaction catalysed by the enzyme farnesyl-protein transferase (FPTase). Inhibitors of FPTase have therefore been proposed as anti
Autor:
G. E. Stokker, Samuel L. Graham, John H. Hutchinson, Michael J. Breslin, S. Jane Desolms, E A Giuliani, Scott D. Mosser, Hamilton Kelly A. Hamilton Kelly A., David L. Pompliano
Publikováno v:
ChemInform. 30
Autor:
Anthony W. Shaw, S. Jane Desolms
Publikováno v:
ChemInform. 32
Organometallic addition to tert -butanesufinyl ketimines derived from diaryl and aryl-heteroaryl ketones provided the corresponding α,α-diaryl and α-aryl-α-heteroaryl alkylamines in good yield with high diastereoselectivity. In many cases, imine
Autor:
Nancy E. Kohl, Charles A. Omer, Ronald E. Diehl, S. Jane deSolms, Theresa M. Williams, Astrid M. Kral
Publikováno v:
The Journal of biological chemistry. 272(43)
The roles of 11 conserved amino acids of the beta-subunit of human farnesyl:protein transferase (FTase) were examined by performing kinetic and biochemical analyses of site-directed mutants. This biochemical information along with the x-ray crystal s