Search Results - "MARCOTTE, P. A"

Discovery of Potent Nonpeptide Inhibitors of Stromelysin Using SAR by NMR by Hajduk, P. J, Sheppard, G, Nettesheim, D. G, Olejniczak, E. T, Shuker, S. B, Meadows, R. P, Steinman, D. H, Carrera, G. M, Marcotte, P. A, Severin, J, Walter, K, Smith, H, Gubbins, E, Simmer, R, Holzman, T. F, Morgan, D. W, Davidsen, S. K, Summers, J. B, Fesik, S. W

“…With the use of an NMR-based method, potent (IC50 < 25 nM) nonpeptide inhibitors of the matrix metalloproteinase stromelysin (MMP-3) were discovered. The…”
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Differential protein acetylation induced by novel histone deacetylase inhibitors by Glaser, K.B., Li, J., Pease, L.J., Staver, M.J., Marcotte, P.A., Guo, J., Frey, R.R., Garland, R.B., Heyman, H.R., Wada, C.K., Vasudevan, A., Michaelides, M.R., Davidsen, S.K., Curtin, M.L.

“…Histone deacetylase (HDAC) inhibitors induce the hyperacetylation of nucleosomal histones in carcinoma cells resulting in the expression of repressed genes…”
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Stromelysin Inhibitors Designed from Weakly Bound Fragments:  Effects of Linking and Cooperativity by Olejniczak, E. T, Hajduk, P. J, Marcotte, P. A, Nettesheim, D. G, Meadows, R. P, Edalji, R, Holzman, T. F, Fesik, Stephen W

“…In the preceding paper, we reported on the discovery of potent, nonpeptide inhibitors of the matrix metalloproteinase stromelysin that were prepared by linking…”
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The matrix metalloproteinase pump-1 catalyzes formation of low molecular weight (pro)urokinase in cultures of normal human kidney cells by MARCOTTE, P. A, KOZAN, I. M, DORWIN, S. A, RYAN, J. M

“…The enzyme responsible for the metalloproteinase activity which cleaves the Glu143-Leu144 bond of (pro)urokinase has been isolated from the conditioned medium…”
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The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors by Steinman, Douglas H., Curtin, Michael L., Garland, Robert B., Davidsen, Steven K., Heyman, H.Robin, Holms, James H., Albert, Daniel H., Magoc, Terry J., Nagy, Ildiko B., Marcotte, Patrick A., Li, Junling, Morgan, Douglas W., Hutchins, Charles, Summers, James B.

“…A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix…”
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Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors by Sheppard, George S., Florjancic, Alan S., Giesler, Jamie R., Xu, Lianhong, Guo, Yan, Davidsen, Steven K., Marcotte, Patrick A., Elmore, Ildiko, Albert, Daniel H., Magoc, Terrance J., Bouska, Jennifer J., Goodfellow, Carole L., Morgan, Douglas W., Summers, James B.

“…A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid…”
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Phenoxyphenyl Sulfone N-Formylhydroxylamines (Retrohydroxamates) as Potent, Selective, Orally Bioavailable Matrix Metalloproteinase Inhibitors by Wada, Carol K, Holms, James H, Curtin, Michael L, Dai, Yujia, Florjancic, Alan S, Garland, Robert B, Guo, Yan, Heyman, H. Robin, Stacey, Jamie R, Steinman, Douglas H, Albert, Daniel H, Bouska, Jennifer J, Elmore, Ildiko N, Goodfellow, Carole L, Marcotte, Patrick A, Tapang, Paul, Morgan, Douglas W, Michaelides, Michael R, Davidsen, Steven K

“…A novel series of sulfone N-formylhydroxylamines (retrohydroxamates) have been investigated as matrix metalloproteinases (MMP) inhibitors. The substitution of…”
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Pure human inactive renin. Evidence that native inactive renin is prorenin by Higashimori, K, Mizuno, K, Nakajo, S, Boehm, F H, Marcotte, P A, Egan, D A, Holleman, W H, Heusser, C, Poisner, A M, Inagami, T

“…To clarify contradicting observations on the identity of inactive renin and prorenin, inactive renin was completely purified from native human chorion laeve…”
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Renin inhibitors. Dipeptide analogs of angiotensinogen utilizing a dihydroxyethylene transition-state mimic at the scissile bond to impart greater inhibitory potency by Luly, Jay R, BaMaung, Nwe, Soderquist, Jeff, Fung, Anthony K. L, Stein, Herman, Kleinert, Hollis D, Marcotte, Patrick A, Egan, David A, Bopp, Barbara

“…The synthesis of diol-containing renin inhibitors has revealed that a simple vicinal diol functionality corresponding to the scissile Leu-Val bond in human…”
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Renin inhibitors. Dipeptide analogs of angiotensinogen utilizing a structurally modified phenylalanine residue to impart proteolytic stability by Plattner, Jacob J, Marcotte, Patrick A, Kleinert, Hollis D, Stein, Herman H, Greer, Jonathan, Bolis, Giorgio, Fung, Anthony K. L, Bopp, Barbara A, Luly, Jay R

“…A series of renin inhibitors have been prepared and evaluated for their susceptibility to cleavage by the serine protease chymotrypsin. The compounds were…”
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Renin inhibitors. Design and synthesis of a new class of conformationally restricted analogs of angiotensinogen by Sham, Hing L, Bolis, Giorgio, Stein, Herman H, Fesik, Stephen W, Marcotte, Patrick A, Plattner, Jacob J, Rempel, Cheryl A, Greer, Jonathan

“…Molecular modeling methods have been used to design a novel series of conformationally constrained cyclic peptide inhibitors of human renin. Three goals were…”
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Renin inhibitors. Dipeptide analogs of angiotensinogen incorporating transition-state, nonpeptidic replacements at the scissile bond by Bolis, Giorgio, Fung, Anthony K. L, Greer, Jonathan, Kleinert, Hollis D, Marcotte, Patrick A, Perun, Thomas J, Plattner, Jacob J, Stein, Herman H

“…A series of dipeptide analogues of angiotensinogen have been prepared and evaluated for their ability to inhibit the aspartic proteinase renin. The compounds…”
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Renin inhibitors Improvements in the stability and biological activity of small peptides containing novel Leu-Val replacements by Kleinert, Hollis D., Luly, Jay R., Marcotte, Patrick A., Perun, Thomas J., Plattner, Jacob J., Stein, Herman

“…We have designed a novel class of potent (0.3–7 nM) renin inhibitors which contain a dihydroxyethylene replacement for what is formally the Leu 1O-Val 11 amide…”
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Biaryl Ether Retrohydroxamates as Potent, Long-lived, Orally Bioavailable MMP Inhibitors by Michaelides, Michael R., Dellaria, Joseph F., Gong, Jane, Holms, James H., Bouska, Jennifer J., Stacey, Jamie, Wada, Carol K., Heyman, H.Robin, Curtin, Michael L., Guo, Yan, Goodfellow, Carole L., Elmore, Ildiko B., Albert, Daniel H., Magoc, Terrance J., Marcotte, Patrick A., Morgan, Douglas W., Davidsen, Steven K.

“…A novel series of biaryl ether reverse hydroxamate MMP inhibitors has been developed. These compounds are potent MMP-2 inhibitors with limited activity against…”
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Novel renin inhibitors containing analogs of statine retro-inverted at the C-termini. Specificity at the P2 histidine site by Rosenberg, Saul H, Plattner, Jacob J, Woods, Keith W, Stein, Herman H, Marcotte, Patrick A, Cohen, Jerome, Perun, Thomas J

“…Substituted 1,3- and 1,4-diamines were prepared from epoxides derived from Boc-leucine or Boc-cyclohexylalanine. These diamines were incorporated into renin…”
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Design of mechanism-based inactivators of human placental aromatase by Marcotte, P A, Robinson, C H

“…This article reviews the design and study, in our own laboratory and in other laboratories, of new 10 beta-substituted analogs of estr-4-ene-3,17-dione. These…”
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Inactivation of bacterial D-amino acid transaminases by the olefinic amino acid D-vinylglycine by Soper, T S, Manning, J M, Marcotte, P A, Walsh, C T

“…D-Vinylglycine (2-amino-3-butenoate) functions as a transamination substrate and irreversible inactivator of the homogeneous pyridoxal phosphate-dependent…”
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Modified peptides which display potent and specific inhibition of human renin by Luly, J R, Plattner, J J, Stein, H, Yi, N, Soderquist, J, Marcotte, P A, Kleinert, H D, Perun, T J

“…A new class of angiotensinogen analogues which contain heteroatom-methylene and retro-inverso amide bond replacements was synthesized and evaluated for renin…”
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Human placental chorionic renin: production, purification and characterization by Egan, D A, Grzegorczyk, V, Tricarico, K A, Rueter, A, Holleman, W H, Marcotte, P A

“…Native human renin, produced from the culture of human chorionic trophoblasts, has been purified to homogeneity on a milligram scale using a five-step…”
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Characterization of matrix metalloproteinase inhibitors: enzymatic assays by Marcotte, P A, Davidsen, S K

“…The matrix metalloproteinases (MMPs) are a family of tightly regulated proteases that are involved in the catabolic aspect of remodeling and maintenance of…”
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