Search Results - "SMYTH, Mark S"

Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome by DEMO, Susan D, KIRK, Christopher J, SHENK, Kevin D, SMYTH, Mark S, SUN, Congcong M, VALLONE, Marcy K, WOO, Tina M, MOLINEAUX, Christopher J, BENNETT, Mark K, AUJAY, Monette A, BUCHHOLZ, Tonia J, DAJEE, Maya, HO, Mark N, JING JIANG, LAIDIG, Guy J, LEWIS, Evan R, PARLATI, Francesco

“…Clinical studies with bortezomib have validated the proteasome as a therapeutic target for the treatment of multiple myeloma and non-Hodgkin's lymphoma…”
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The First Asymmetric Total Syntheses of (+)-Lycorine and (+)-1-Deoxylycorine by Schultz, Arthur G, Holoboski, Mark A, Smyth, Mark S

“…The first asymmetric total syntheses of (+)-1-deoxylycorine (2a) and (+)-lycorine (2b), the unnatural enantiomer of lycorine (1), are described. Construction…”
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Preparation of fluoro- and hydroxy-4-(phosphonomethyl)-D,L-phenylalanine suitably protected for solid-phase synthesis of peptides containing hydrolytically stable analogs of O-phosphotyrosine by Burke, Terrence R, Smyth, Mark S, Nomizu, Motoyoshi, Otaka, Akira, Roller, Peter R

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Nonhydrolyzable Phosphotyrosyl Mimetics for the Preparation Of Phosphatase-Resistant SH2 Domain Inhibitors by Burke, Terrence R. Jr, Smyth, Mark S, Otaka, Akira, Nomizu, Motoyoshi, Roller, Peter P, Wolf, Gert, Case, Randi, Shoelson, Steven E

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Discovery of Novel 2,8-Diazaspiro[4.5]decanes as Orally Active Glycoprotein IIb-IIIa Antagonists by Mehrotra, Mukund M., Heath, Julie A., Smyth, Mark S., Pandey, Anjali, Rose, Jack W., Seroogy, Joseph M., Volkots, Deborah L., Nannizzi-Alaimo, Lisa, Park, Gary L., Lambing, Joseph L., Hollenbach, Stanley J., Scarborough, Robert M.

“…In our efforts to develop orally active GPIIb-IIIa antagonists with improved pharmaceutical properties, we have utilized a novel 2,8-diazaspiro[4.5]decane…”
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Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: Synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes by MEHROTRA, Mukund M, HEATH, Julie A, PANDEY, Anjali, SCARBOROUGH, Robert M, ROSE, Jack W, SMYTH, Mark S, SEROOGY, Joseph, VOLKOTS, Deborah L, RUHTER, Gerd, SCHOTTEN, Theo, ALAIMO, Lisa, PARK, Gary

“…The synthesis and biological activity of analogues containing spiro piperidinylpyridine and pyrrolidinylpyridine templates are described. The potent activity…”
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The first asymmetric synthesis of a lycorine alkaloid. Total synthesis of (+)-1-deoxylycorine by Schultz, Arthur G, Holoboski, Mark A, Smyth, Mark S

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Fibrinogen Receptor (GPIIb-IIIa) Antagonists Derived from 5,6-Bicyclic Templates. Amidinoindoles, Amidinoindazoles, and Amidinobenzofurans Containing the N-α-Sulfonamide Carboxylic Acid Function as Potent Platelet Aggregation Inhibitors by Su, Ting, Naughton, Mary Ann H, Smyth, Mark S, Rose, Jack W, Arfsten, Ann E, McCowan, Jefferson R, Jakubowski, Joseph A, Wyss, Virginia L, Ruterbories, Kenneth J, Sall, Daniel J, Scarborough, Robert M

“…A series of highly potent and specific fibrinogen receptor antagonists have been discovered and optimized through structural modification of the novel…”
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Use of Conformationally Restricted Benzamidines as Arginine Surrogates in the Design of Platelet GPIIb-IIIa Receptor Antagonists by Sall, Daniel J, Arfsten, Ann E, Bastian, Jolie A, Denney, Michael L, Harms, Cathy S, McCowan, Jefferson R, Morin, John M, Rose, Jack W, Scarborough, Robert M, Smyth, Mark S, Um, Suzane L, Utterback, Barbara G, Vasileff, Robert T, Wikel, James H, Wyss, Virginia L, Jakubowski, Joseph A

“…The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa)…”
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Non-amine based analogs of lavendustin A as protein-tyrosine kinase inhibitors by Smyth, Mark S, Stefanova, Irena, Hartmann, Frank, Horak, Ivan D, Osherov, Nir, Levitzki, Alexander, Burke, Terrence R

“…The fermentation product lavendustin A (1) is a protein-tyrosine kinase (PTK) inhibitor whose active pharmacophore has previously been shown to reside in the…”
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Hydroxylated 2-(5'-salicyl)naphthalenes as protein-tyrosine kinase inhibitors by Smyth, Mark S, Stefanova, Irena, Horak, Ivan D, Burke, Terrence R

“…The salicyl group figures prominently in several potent protein-tyrosine kinase (PTK) inhibitors, including the fermentation product lavendustin A (3), the…”
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Bimolecular cyclization of 2-fluoro-N-(hydroxyalkyl)benzamides. 2. Synthesis and structural characterization of 17- and 20-membered macrocycles by Schultz, Arthur G, Smyth, Mark S, Tham, Fook S

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A Proteasome Specific Binding Assay for Quantitation of Constitutive and Immunoproteasome Active Sites by Bennett, Mark K., Aujay, Monette A., Buchholz, Tonia J., Demo, Susan D., Laidig, Guy J., Sun, Congcong M., Vallone, Marcy K., Woo, Tina, Smyth, Mark S.

“…The ubiquitin-proteasome pathway constitutes a major intracellular system for protein degradation. Substrates for this pathway include misfolded or unassembled…”
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Why Is Phosphonodifluoromethyl Phenylalanine a More Potent Inhibitory Moiety Than Phosphonomethyl Phenylalanine Toward Protein-Tyrosine Phosphatases by Chen, L., Wu, L., Otaka, A., Smyth, M.S., Roller, P.P., Burke, T.R., Denhertog, J., Zhang, Z.Y.

“…The phosphonodifluoromethyl phenylalanine (F2Pmp) is superior to phosphonomethyl phenylalanine (Pmp) as a non-hydrolyzable phosphotyrosine (pTyr) mimetic. The…”
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Pharmacokinetics, Pharmacodynamics and Anti-Tumor Efficacy of PR-171, a Novel Inhibitor of the 20S Proteasome by Kirk, Christopher J., Bennett, Mark K., Buchholz, Tonia J., Demo, Susan D., Ho, Mark N., Jiang, Jing, Laidig, Guy J., Lewis, Evan R., Shenk, Kevin D., Smyth, Mark S., Sun, Congcong M., Vallone, Marcy K., Woo, Tina M., Molineaux, Christopher J.

“…Clinical studies using the boronic acid-based proteasome inhibitor bortezomib (VelcadeTM) have validated the proteasome as a therapeutic intervention point for…”
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Biochemical and Cellular Characterization of the Novel Proteasome Inhibitor PR-171 by Demo, Susan D., Buchholz, Tonia J., Laidig, Guy J., Parlati, Francesco, Shenk, Kevin D., Smyth, Mark S., Sullivan, Carol M., Sun, Congcong M., Vallone, Marcy K., Woo, Tina, Bennett, Mark K.

“…Recent clinical studies have identified the proteasome as an important therapeutic target for hematologic malignances. The proteasome inhibitor, bortezomib,…”
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Cyclic peptide inhibitors of phosphatidylinositol 3-kinase p85 SH2 domain binding by Burke, Jr, T R, Nomizu, M, Otaka, A, Smyth, M S, Roller, P P, Case, R D, Wolf, G, Shoelson, S E

“…Cyclic hexameric peptides based on the amino acid sequence "Gly-Xxx-Val-Pro-Met-Leu", where Xxx is either phosphotyrosyl (pTyr) residue or a hydrolytically…”
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