Search Results - "Shen, Marina W H"

Indole Cytosolic Phospholipase A2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic Acid, Efipladib by McKew, John C, Lee, Katherine L, Shen, Marina W. H, Thakker, Paresh, Foley, Megan A, Behnke, Mark L, Hu, Baihua, Sum, Fuk-Wah, Tam, Steve, Hu, Yonghan, Chen, Lihren, Kirincich, Steven J, Michalak, Ronald, Thomason, Jennifer, Ipek, Manus, Wu, Kun, Wooder, Lane, Ramarao, Manjunath K, Murphy, Elizabeth A, Goodwin, Debra G, Albert, Leo, Xu, Xin, Donahue, Frances, Ku, M. Sherry, Keith, James, Nickerson-Nutter, Cheryl L, Abraham, William M, Williams, Cara, Hegen, Martin, Clark, James D

“…The optimization of a class of indole cPLA2α inhibitors is described herein. The importance of the substituent at C3 and the substitution pattern of the…”
Get full text

Discovery of Clinical Candidate 1‑{[(2S,3S,4S)‑3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin‑1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design by Lee, Katherine L, Ambler, Catherine M, Anderson, David R, Boscoe, Brian P, Bree, Andrea G, Brodfuehrer, Joanne I, Chang, Jeanne S, Choi, Chulho, Chung, Seungwon, Curran, Kevin J, Day, Jacqueline E, Dehnhardt, Christoph M, Dower, Ken, Drozda, Susan E, Frisbie, Richard K, Gavrin, Lori K, Goldberg, Joel A, Han, Seungil, Hegen, Martin, Hepworth, David, Hope, Heidi R, Kamtekar, Satwik, Kilty, Iain C, Lee, Arthur, Lin, Lih-Ling, Lovering, Frank E, Lowe, Michael D, Mathias, John P, Morgan, Heidi M, Murphy, Elizabeth A, Papaioannou, Nikolaos, Patny, Akshay, Pierce, Betsy S, Rao, Vikram R, Saiah, Eddine, Samardjiev, Ivan J, Samas, Brian M, Shen, Marina W. H, Shin, Julia H, Soutter, Holly H, Strohbach, Joseph W, Symanowicz, Peter T, Thomason, Jennifer R, Trzupek, John D, Vargas, Richard, Vincent, Fabien, Yan, Jiangli, Zapf, Christoph W, Wright, Stephen W

“…Through fragment-based drug design focused on engaging the active site of IRAK4 and leveraging three-dimensional topology in a ligand-efficient manner, a…”
Get full text

Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α2α by Lee, Katherine L, Foley, Megan A, Chen, Lihren, Behnke, Mark L, Lovering, Frank E, Kirincich, Steven J, Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W. H, Khor, SooPeang, Xu, Xin, Goodwin, Debra G, Ramarao, Manjunath K, Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M. Sherry, Clark, James D, McKew, John C

“…The synthesis and structure−activity relationship of a series of indole inhibitors of cytosolic phospholipase A2α (cPLA2α, type IVA phospholipase) are…”
Get full text

Inhibition of Cytosolic Phospholipase A2α: Hit to Lead Optimization by McKew, John C, Foley, Megan A, Thakker, Paresh, Behnke, Mark L, Lovering, Frank E, Sum, Fuk-Wah, Tam, Steve, Wu, Kun, Shen, Marina W. H, Zhang, Wen, Gonzalez, Mario, Liu, Shanghao, Mahadevan, Anu, Sard, Howard, Khor, Soo Peang, Clark, James D

“…Compound 1 was previously reported to be a potent inhibitor of cPLA2α in both artificial monomeric substrate and cell-based assays. However, 1 was inactive in…”
Get full text

Cytosolic phospholipase A2 alpha-deficient mice are resistant to experimental autoimmune encephalomyelitis by Marusic, Suzana, Leach, Michael W, Pelker, Jeffrey W, Azoitei, Mihai L, Uozumi, Naonori, Cui, Junqing, Shen, Marina W H, DeClercq, Charlene M, Miyashiro, Joy S, Carito, Brenda A, Thakker, Paresh, Simmons, David L, Leonard, John P, Shimizu, Takao, Clark, James D

“…Experimental autoimmune encephalomyelitis (EAE), a Th1-mediated inflammatory disease of the central nervous system (CNS), is a model of human multiple…”
Get full text

Discovery of ecopladib, an indole inhibitor of cytosolic phospholipase A2α by LEE, Katherine L, FOLEY, Megan A, KHOR, Soopeang, XIN XU, GOODWIN, Debra G, RAMARAO, Manjunath K, NICKERSON-NUTTER, Cheryl, DONAHUE, Frances, SHERRY KU, M, DARK, James D, MCKEW, John C, CHEN, Lihren, BEHNKE, Mark L, LOVERING, Frank E, KIRINCICH, Steven J, WEIHENG WANG, SHIM, Jaechul, TAM, Steve, SHEN, Marina W. H

Get full text

Blockade of cytosolic phospholipase A2 α prevents experimental autoimmune encephalomyelitis and diminishes development of Th1 and Th17 responses by Marusic, Suzana, Thakker, Paresh, Pelker, Jeffrey W, Stedman, Nancy L, Lee, Katherine L, McKew, John C, Han, Lixin, Xu, Xin, Wolf, Stan F, Borey, Adam J, Cui, Junqing, Shen, Marina W.H, Donahue, Fran, Hassan-Zahraee, Mina, Leach, Michael W, Shimizu, Takao, Clark, James D

“…Abstract Cytosolic phospholipase A2 α (cPLA2 α) is the rate-limiting enzyme for release of arachidonic acid, which is converted primarily to prostaglandins via…”
Get full text

Benzhydrylquinazolinediones: Novel cytosolic phospholipase A2α inhibitors with improved physicochemical properties by KIRINCICH, Steven J, JASON XIANG, GREEN, Neal, TAM, Steve, YANG, Hui Y, SHIM, Jaechul, SHEN, Marina W. H, CLARK, James D, MCKEW, John C

Get full text

Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A 2 α Inhibitors by Chen, Lihren, Wang, Weiheng, Lee, Katherine L., Shen, Marina W. H., Murphy, Elizabeth A., Zhang, Wen, Xu, Xin, Tam, Steve, Nickerson-Nutter, Cheryl, Goodwin, Debra G., Clark, James D., McKew, John C.

Get full text

A fluorescence-based assay for fatty acid amide hydrolase compatible with high-throughput screening by Ramarao, Manjunath K., Murphy, Elizabeth A., Shen, Marina W.H., Wang, Yuren, Bushell, Kristen N., Huang, Nelson, Pan, Ning, Williams, Cara, Clark, James D.

“…A novel fluorescent assay to continuously monitor fatty acid amide hydrolase (FAAH) activity that is simple, sensitive, and amenable to high-throughput…”
Get full text

The cPLA2α inhibitor efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid by Nickerson-Nutter, Cheryl L, Goodwin, Debra, Shen, Marina W H, Damphousse, Christy, Duan, Weili, Samad, Tarek A, McKew, John C, Lee, Katherine L, Zaleska, Margaret M, Mollova, Nevena, Clark, James D

“…The contribution of central PGE(2) levels to the nociceptive response in rats was assessed and the effects of the selective cPLA(2)α inhibitor efipladib, and…”
Get full text

Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2α : Optimization of in vitro potency and rat pharmacokinetics for oral efficacy by LEE, Katherine L, BEHNKE, Mark L, SHEN, Marina W. H, RAMARAO, Manjunath K, GOODWIN, Debra G, NICKERSON-NUTTER, Cheryl L, ABRAHAM, William M, WILLIAMS, Cara, CLARK, James D, MCKEW, John C, FOLEY, Megan A, CHEN, Lihren, WEIHENG WANG, VARGAS, Richard, NUNEZ, Jill, TAM, Steve, MOLLOVA, Nevena, XIN XU

Get full text

Thermodynamic characterization of cytosolic phospholipase A2 alpha inhibitors by Ramarao, Manjunath K, Shen, Marina W H, Murphy, Elizabeth A, Duan, Weili, Zhao, Yajuan, McKew, John, Lee, Katherine L, Thakker, Paresh, Behnke, Mark L, Clark, James D

“…Cytosolic phospholipase A(2) alpha (cPLA(2)alpha, type IVA phospholipase) acts at the membrane surface to release free arachidonic acid, which is metabolized…”
Get full text

Reactions of Functionalized Sulfonamides: Application to Lowering the Lipophilicity of Cytosolic Phospholipase A2α Inhibitors by Chen, Lihren, Wang, Weiheng, Lee, Katherine L, Shen, Marina W. H, Murphy, Elizabeth A, Zhang, Wen, Xu, Xin, Tam, Steve, Nickerson-Nutter, Cheryl, Goodwin, Debra G, Clark, James D, McKew, John C

“…The cPLA2α inhibitors we reported earlier were potent in both isolated enzyme and rat whole blood assays but have high plogD7.4. To address these issues,…”
Get full text

Indole Cytosolic Phospholipase A 2 α Inhibitors: Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1 H -indol-3-yl]propyl}benzoic Acid, Efipladib by McKew, John C., Lee, Katherine L., Shen, Marina W. H., Thakker, Paresh, Foley, Megan A., Behnke, Mark L., Hu, Baihua, Sum, Fuk-Wah, Tam, Steve, Hu, Yonghan, Chen, Lihren, Kirincich, Steven J., Michalak, Ronald, Thomason, Jennifer, Ipek, Manus, Wu, Kun, Wooder, Lane, Ramarao, Manjunath K., Murphy, Elizabeth A., Goodwin, Debra G., Albert, Leo, Xu, Xin, Donahue, Frances, Ku, M. Sherry, Keith, James, Nickerson-Nutter, Cheryl L., Abraham, William M., Williams, Cara, Hegen, Martin, Clark, James D.

Get full text

Discovery of Ecopladib, an indole inhibitor of cytosolic phospholipase A2alpha by Lee, Katherine L, Foley, Megan A, Chen, Lihren, Behnke, Mark L, Lovering, Frank E, Kirincich, Steven J, Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W H, Khor, Soopeang, Xu, Xin, Goodwin, Debra G, Ramarao, Manjunath K, Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M Sherry, Clark, James D, McKew, John C

“…The synthesis and structure-activity relationship of a series of indole inhibitors of cytosolic phospholipase A2alpha (cPLA2alpha, type IVA phospholipase) are…”
Get full text

Discovery of Ecopladib, an Indole Inhibitor of Cytosolic Phospholipase Α 2 α by Lee, Katherine L., Foley, Megan A., Chen, Lihren, Behnke, Mark L., Lovering, Frank E., Kirincich, Steven J., Wang, Weiheng, Shim, Jaechul, Tam, Steve, Shen, Marina W. H., Khor, SooPeang, Xu, Xin, Goodwin, Debra G., Ramarao, Manjunath K., Nickerson-Nutter, Cheryl, Donahue, Frances, Ku, M. Sherry, Clark, James D., McKew, John C.

Get full text

Indole Cytosolic Phospholipase A2 α Inhibitors : Discovery and in Vitro and in Vivo Characterization of 4-{3-[5-Chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-l-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic Acid, Efipladib by MCKEW, John C, LEE, Katherine L, CHEN, Lihren, KIRINCICH, Steven J, MICHALAK, Ronald, THOMASON, Jennifer, IPEK, Manus, KUN WU, WOODER, Lane, RAMARAO, Manjunath K, MURPHY, Elizabeth A, GOODWIN, Debra G, SHEN, Marina W. H, ALBERT, Leo, XIN XU, DONAHUE, Frances, SHERRY KU, M, KEITH, James, NICKERSON-NUTTER, Cheryl L, ABRAHAM, William M, WILLIAMS, Cara, HEGEN, Martin, CLARK, James D, THAKKER, Paresh, FOLEY, Megan A, BEHNKE, Mark L, BAIHUA HU, SUM, Fuk-Wah, TAM, Steve, YONGHAN HU

Get full text

Inhibition of cytosolic phospholipase A2alpha: hit to lead optimization by McKew, John C, Foley, Megan A, Thakker, Paresh, Behnke, Mark L, Lovering, Frank E, Sum, Fuk-Wah, Tam, Steve, Wu, Kun, Shen, Marina W H, Zhang, Wen, Gonzalez, Mario, Liu, Shanghao, Mahadevan, Anu, Sard, Howard, Khor, Soo Peang, Clark, James D

“…Compound 1 was previously reported to be a potent inhibitor of cPLA(2)alpha in both artificial monomeric substrate and cell-based assays. However, 1 was…”
Get full text

Inhibition of Cytosolic Phospholipase A 2 α: Hit to Lead Optimization by McKew, John C., Foley, Megan A., Thakker, Paresh, Behnke, Mark L., Lovering, Frank E., Sum, Fuk-Wah, Tam, Steve, Wu, Kun, Shen, Marina W. H., Zhang, Wen, Gonzalez, Mario, Liu, Shanghao, Mahadevan, Anu, Sard, Howard, Khor, Soo Peang, Clark, James D.

Get full text