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N-Arylalkyl Pseudopeptide Inhibitors of Farnesyltransferase

Autor: S J deSolms, Rands E, Jackson B. Gibbs, Catherine M. Wiscount, Scholz Th, Robert L. Smith, Kenneth S. Koblan, Nancy E. Kohl, E A Giuliani, David L. Pompliano, Scott D. Mosser, Oliff Allen I, Samuel L. Graham

Publikováno v: Journal of Medicinal Chemistry. 41:2651-2656

Inhibitors of Ras protein farnesyltransferase are described which are reduced pseudopeptides related to the C-terminal tetrapeptide of the Ras protein that signals farnesylation. Reduction of the carbonyl groups linking the first three residues of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8f669f5680f64cda6fe287560a76428f
https://doi.org/10.1021/jm9800907

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Farnesyl: proteintransferase inhibitors as agents to inhibit tumor growth

Autor: Ch. J. Dinsmore, George D. Hartman, Ch. A. Omer, Neville J. Anthony, Kenneth S. Koblan, S J deSolms, Jackson B. Gibbs, A. L. Burkhardt, Robert B. Lobell, Nancy E. Kohl, Oliff Allen I, C. A. Buser‐Doepner, Theresa M. Williams

Publikováno v: BioFactors. 6:359-366

Ras, a signal-transducing protein involved in mediating growth factor-stimulated proliferation, is mutationally activated in over 30% of human tumors. To be functional Ras must bind to the inner surface of the plasma membrane, with post-translational

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::023693b2591ad29d03e4f7323078444e
https://doi.org/10.1002/biof.5520060306

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A priori prediction of activity for HIV-1 protease inhibitors employing energy minimization in the active site

Autor: M K, Holloway, J M, Wai, T A, Halgren, P M, Fitzgerald, J P, Vacca, B D, Dorsey, R B, Levin, W J, Thompson, L J, Chen, S J, deSolms

Publikováno v: Journal of Medicinal Chemistry. 38:305-317

We have observed a high correlation between the intermolecular interaction energy (E inter ) calculated for HIV-1 protease inhibitor complexes and the observed in vitro enzyme inhibition. A training set of 33 inhibitors containing modifications in th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7828284b4e63a048f50ded515d7ac8fd
https://doi.org/10.1021/jm00002a012

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Protein farnesyltransferase inhibitors block the growth of ras-dependent tumors in nude mice

Autor: Lee Ta Jyh, Neville J. Anthony, Robert P. Gomez, S D Mosser, Michael W. Conner, Nancy E. Kohl, W. J. Holtz, F R Wilson, E A Giuliani, S J deSolms

Publikováno v: Proceedings of the National Academy of Sciences. 91:9141-9145

The posttranslational addition of a farnesyl moiety to the Ras oncoprotein is essential for its transforming activity. Cell-active inhibitors of the enzyme that catalyzes this reaction, protein farnesyltransferase, have been shown to selectively bloc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ea781f34fb12e3278cbb8f3cb8222043
https://doi.org/10.1073/pnas.91.19.9141

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Pseudopeptide Inhibitors of Ras Farnesyl-Protein Transferase

Autor: Michael J. Breslin, Samuel L. Graham, Scott D. Mosser, Deana Aa, Rands E, Oliff Allen I, S J deSolms, Nancy E. Kohl, David L. Pompliano, E A Giuliani

Publikováno v: Journal of Medicinal Chemistry. 37:725-732

Inhibitors of Ras farnesyl-protein transferase are described. These are reduced pseudopeptides related to the C-terminal tetrapeptide of the Ras protein that signals farnesylation. Deletion of the carbonyl groups between the first two residues of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::694220638d203e2b4a9bf3af58e0ae80
https://doi.org/10.1021/jm00032a004

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Selective Inhibition of ras -Dependent Transformation by a Farnesyltransferase Inhibitor

Autor: Scott D. Mosser, Samuel L. Graham, Jackson B. Gibbs, Edward M. Scolnick, S J deSolms, David L. Pompliano, E A Giuliani, Oliff Allen I, Robert L. Smith, Nancy E. Kohl

Publikováno v: Science. 260:1934-1937

To acquire transforming potential, the precursor of the Ras oncoprotein must undergo farnesylation of the cysteine residue located in a carboxyl-terminal tetrapeptide. Inhibitors of the enzyme that catalyzes this modification, farnesyl protein transf

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ef69c99b5b0158099dbc81cf91956dc4
https://doi.org/10.1126/science.8316833

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P450 interaction with farnesyl-protein transferase inhibitors metabolic stability, inhibitory potency, and P450 binding spectra in human liver microsomes

Autor: M, Chiba, C, Tang, W E, Neway, T M, Williams, S J, Desolms, C J, Dinsmore, J S, Wai, J H, Lin

Publikováno v: Biochemical pharmacology. 62(6)

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

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::2591c64fe2758cc922578945beeeca0e
https://pubmed.ncbi.nlm.nih.gov/11551523

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Farnesyltransferase inhibitors: a new class of cancer chemotherapeutics

Autor: Neville J. Anthony, Jackson B. Gibbs, Theresa M. Williams, Michael W. Conner, George D. Hartman, Charles A. Omer, S J deSolms, Oliff Allen I, Nancy E. Kohl, Kenneth S. Koblan, Samuel L. Graham

Publikováno v: Biochemical Society transactions. 24(3)

The family of Ras proteins plays a central role in the regulation of cell growth and integration of regulatory signals which can govern the cell cycle and proliferation. Mutant m s genes (derived from murine sarcoma viruses) were among the first onco

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::585f08d1d3e9a70657722b5c233eaf29
https://pubmed.ncbi.nlm.nih.gov/8878827

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