Search Results - "Scholten, Jeffrey A."

Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1 by Schnute, Mark E, McReynolds, Matthew D, Kasten, Tom, Yates, Matthew, Jerome, Gina, Rains, John W, Hall, Troii, Chrencik, Jill, Kraus, Michelle, Cronin, Ciaran N, Saabye, Matthew, Highkin, Maureen K, Broadus, Richard, Ogawa, Shinji, Cukyne, Kristin, Zawadzke, Laura E, Peterkin, Vincent, Iyanar, Kaliapan, Scholten, Jeffrey A, Wendling, Jay, Fujiwara, Hideji, Nemirovskiy, Olga, Wittwer, Arthur J, Nagiec, Marek M

“…SphK (sphingosine kinase) is the major source of the bioactive lipid and GPCR (G-protein-coupled receptor) agonist S1P (sphingosine 1-phosphate). S1P promotes…”
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Discovery of a Potent and Selective Sphingosine Kinase 1 Inhibitor through the Molecular Combination of Chemotype-Distinct Screening Hits by Schnute, Mark E, McReynolds, Matthew D, Carroll, Jeffrey, Chrencik, Jill, Highkin, Maureen K, Iyanar, Kaliapan, Jerome, Gina, Rains, John W, Saabye, Matthew, Scholten, Jeffrey A, Yates, Matthew, Nagiec, Marek M

“…Sphingosine kinase (SphK) is the major source of the lipid mediator and G protein-coupled receptor agonist sphingosine-1-phosphate (S1P). S1P promotes cell…”
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Discovery of N‑(4-Fluoro-3-methoxybenzyl)-6-(2-(((2S,5R)‑5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)‑2H‑tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis by Ruminski, Peter G, Massa, Mark, Strohbach, Joseph, Hanau, Cathleen E, Schmidt, Michelle, Scholten, Jeffrey A, Fletcher, Theresa R, Hamper, Bruce C, Carroll, Jeffery N, Shieh, Huey S, Caspers, Nicole, Collins, Brandon, Grapperhaus, Margaret, Palmquist, Katherine E, Collins, Joe, Baldus, John E, Hitchcock, Jeffrey, Kleine, H. Peter, Rogers, Michael D, McDonald, Joseph, Munie, Grace E, Messing, Dean M, Portolan, Silvia, Whiteley, Laurence O, Sunyer, Teresa, Schnute, Mark E

“…Matrix metalloproteinase-13 (MMP-13) is a zinc-dependent protease responsible for the cleavage of type II collagen, the major structural protein of articular…”
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Synthesis and biological evaluation of substituted benzoxazoles as inhibitors of mPGES-1: Use of a conformation-based hypothesis to facilitate compound design by Walker, Daniel P., Arhancet, Graciela B., Lu, Hwang-Fun, Heasley, Steven E., Metz, Sue, Kablaoui, Natasha M., Franco, Francisco M., Hanau, Cathleen E., Scholten, Jeffrey A., Springer, John R., Fobian, Yvette M., Carter, Jeffrey S., Xing, Li, Yang, Shengtian, Shaffer, Alexander F., Jerome, Gina M., Baratta, Michael T., Moore, William M., Vazquez, Michael L.

“…Microsomal prostaglandin E2 synthase-1 (mPGES-1) is a novel therapeutic target for the treatment of inflammation and pain. In the preceding letter, we detailed…”
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Discovery of (pyridin-4-yl)-2H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis by SCHNUTE, Mark E, O'BRIEN, Patrick M, CARROLL, Jeffery N, PATT, William C, SHIEH, Huey S, COLLINS, Brandon, PAVLOVSKY, Alexander G, PALMQUIST, Katherine E, ASTON, Karl W, HITCHCOCK, Jeffrey, ROGERS, Michael D, MCDONALD, Joseph, NAHRA, Joe, JOHNSON, Adam R, MUNIE, Grace E, WITTWER, Arthur J, MAN, Chiu-Fai, SETTLE, Steven L, NEMIROVSKIY, Olga, VICKERY, Lillian E, AGAWAL, Arun, DYER, Richard D, SUNYER, Teresa, MORRIS, Mark, HOWARD ROARK, W, HANAU, Cathleen E, RUMINSKI, Peter G, SCHOLTEN, Jeffrey A, FLETCHER, Theresa R, HAMPER, Bruce C

“…Potent, highly selective and orally-bioavailable MMP-13 inhibitors have been identified based upon a (pyridin-4-yl)-2H-tetrazole scaffold. Co-crystal structure…”
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Discovery of N -(4-Fluoro-3-methoxybenzyl)-6-(2-(((2 S ,5 R )-5-(hydroxymethyl)-1,4-dioxan-2-yl)methyl)-2 H -tetrazol-5-yl)-2-methylpyrimidine-4-carboxamide. A Highly Selective and Orally Bioavailable Matrix Metalloproteinase-13 Inhibitor for the Potential Treatment of Osteoarthritis by Ruminski, Peter G., Massa, Mark, Strohbach, Joseph, Hanau, Cathleen E., Schmidt, Michelle, Scholten, Jeffrey A., Fletcher, Theresa R., Hamper, Bruce C., Carroll, Jeffery N., Shieh, Huey S., Caspers, Nicole, Collins, Brandon, Grapperhaus, Margaret, Palmquist, Katherine E., Collins, Joe, Baldus, John E., Hitchcock, Jeffrey, Kleine, H. Peter, Rogers, Michael D., McDonald, Joseph, Munie, Grace E., Messing, Dean M., Portolan, Silvia, Whiteley, Laurence O., Sunyer, Teresa, Schnute, Mark E.

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Discovery of (pyridin-4-yl)-2 H-tetrazole as a novel scaffold to identify highly selective matrix metalloproteinase-13 inhibitors for the treatment of osteoarthritis by Schnute, Mark E., O’Brien, Patrick M., Nahra, Joe, Morris, Mark, Howard Roark, W., Hanau, Cathleen E., Ruminski, Peter G., Scholten, Jeffrey A., Fletcher, Theresa R., Hamper, Bruce C., Carroll, Jeffery N., Patt, William C., Shieh, Huey S., Collins, Brandon, Pavlovsky, Alexander G., Palmquist, Katherine E., Aston, Karl W., Hitchcock, Jeffrey, Rogers, Michael D., McDonald, Joseph, Johnson, Adam R., Munie, Grace E., Wittwer, Arthur J., Man, Chiu-Fai, Settle, Steven L., Nemirovskiy, Olga, Vickery, Lillian E., Agawal, Arun, Dyer, Richard D., Sunyer, Teresa

“…Potent, highly selective and orally-bioavailable MMP-13 inhibitors have been identified which inhibit production of type II collagen neoepitope (TIINE), a…”
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3-Methyl-4H-[1,2,4]-oxadiazol-5-one: a versatile synthon for protecting monosubstituted acetamidines by Moormann, Alan E., Wang, Jane L., Palmquist, Katherine E., Promo, Michele A., Snyder, Jeffery S., Scholten, Jeffrey A., Massa, Mark A., Sikorski, James A., Webber, R. Keith

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3-Methyl-4 H-[1,2,4]-oxadiazol-5-one: a versatile synthon for protecting monosubstituted acetamidines by Moormann, Alan E., Wang, Jane L., Palmquist, Katherine E., Promo, Michele A., Snyder, Jeffery S., Scholten, Jeffrey A., Massa, Mark A., Sikorski, James A., Webber, R. Keith

“…The utilization of 3-methyl-4 H-[1,2,4]-oxadiazol-5-one as a versatile protected acetamidine is demonstrated through employment in a variety of synthetic…”
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