Search Results - "Morgan, Barry A."

Application of encoded library technology (ELT) to a protein–protein interaction target: Discovery of a potent class of integrin lymphocyte function-associated antigen 1 (LFA-1) antagonists by Kollmann, Christopher S., Bai, Xiaopeng, Tsai, Ching-Hsuan, Yang, Hongfang, Lind, Kenneth E., Skinner, Steven R., Zhu, Zhengrong, Israel, David I., Cuozzo, John W., Morgan, Barry A., Yuki, Koichi, Xie, Can, Springer, Timothy A., Shimaoka, Motomu, Evindar, Ghotas

“…Encoded library technology (ELT) was utilized to identify a class of compounds that disrupt the interaction between lymphocyte function-associated antigen-1…”
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Antiparasitic activities of novel, orally available fumagillin analogs by Arico-Muendel, Christopher, Centrella, Paolo A., Contonio, Brooke D., Morgan, Barry A., O’Donovan, Gary, Paradise, Christopher L., Skinner, Steven R., Sluboski, Barbara, Svendsen, Jennifer L., White, Kerry F., Debnath, Anjan, Gut, Jiri, Wilson, Nathan, McKerrow, James H., DeRisi, Joseph L., Rosenthal, Philip J., Chiang, Peter K.

“…Analogs of fumagillin were shown to inhibit growth of three parasites and possess activity in a mouse model of malaria. Fumagillin, an irreversible inhibitor…”
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Design, synthesis and selection of DNA-encoded small-molecule libraries by Morgan, Barry A, Clark, Matthew A, Acharya, Raksha A, Arico-Muendel, Christopher C, Belyanskaya, Svetlana L, Benjamin, Dennis R, Carlson, Neil R, Centrella, Paolo A, Chiu, Cynthia H, Creaser, Steffen P, Cuozzo, John W, Davie, Christopher P, Ding, Yun, Franklin, G Joseph, Franzen, Kurt D, Gefter, Malcolm L, Hale, Steven P, Hansen, Nils J V, Israel, David I, Jiang, Jinwei, Kavarana, Malcolm J, Kelley, Michael S, Kollmann, Christopher S, Li, Fan, Lind, Kenneth, Mataruse, Sibongile, Medeiros, Patricia F, Messer, Jeffrey A, Myers, Paul, O'Keefe, Heather, Oliff, Matthew C, Rise, Cecil E, Satz, Alexander L, Skinner, Steven R, Svendsen, Jennifer L, Tang, Lujia, van Vloten, Kurt, Wagner, Richard W, Yao, Gang, Zhao, Baoguang

“…Biochemical combinatorial techniques such as phage display, RNA display and oligonucleotide aptamers have proven to be reliable methods for generation of…”
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Discovery of soluble epoxide hydrolase inhibitors through DNA-encoded library technology (ELT) by Ding, Yun, Belyanskaya, Svetlana, DeLorey, Jennifer L., Messer, Jeffrey A., Joseph Franklin, G., Centrella, Paolo A., Morgan, Barry A., Clark, Matthew A., Skinner, Steven R., Dodson, Jason W., Li, Peng, Marino, Joseph P., Israel, David I.

“…[Display omitted] Inhibition of soluble epoxide hydrolase (sEH) has recently emerged as a new approach to treat cardiovascular disease and respiratory disease…”
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Employing Photocatalysis for the Design and Preparation of DNA‐Encoded Libraries: A Case Study by Kölmel, Dominik K., Zhu, Hongyao, Flanagan, Mark E., Sakata, Sylvie K., Harris, Anthony R., Wan, Jinqiao, Morgan, Barry A.

“…This Personal Account describes the authors’ foray into DNA‐encoded libraries. The article addresses several key aspects of this hit generation technology,…”
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PAC-FragmentDEL - photoactivated covalent capture of DNA-encoded fragments for hit discovery by Ma, Huiyong, Murray, James B, Luo, Huadong, Cheng, Xuemin, Chen, Qiuxia, Song, Chao, Duan, Cong, Tan, Ping, Zhang, Lifang, Liu, Jian, Morgan, Barry A, Li, Jin, Wan, Jinqiao, Baker, Lisa M, Finnie, William, Guetzoyan, Lucie, Harris, Richard, Hendrickson, Nicole, Matassova, Natalia, Simmonite, Heather, Smith, Julia, Hubbard, Roderick E, Liu, Guansai

“…We describe a novel approach for screening fragments against a protein that combines the sensitivity of DNA-encoded library technology with the ability of…”
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Discovery of Highly Potent and Selective Small Molecule ADAMTS‑5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT) by Deng, Hongfeng, O’Keefe, Heather, Davie, Christopher P, Lind, Kenneth E, Acharya, Raksha A, Franklin, G. Joseph, Larkin, Jonathan, Matico, Rosalie, Neeb, Michael, Thompson, Monique M, Lohr, Thomas, Gross, Jeffrey W, Centrella, Paolo A, O’Donovan, Gary K, Bedard, Katie L. (Sargent), van Vloten, Kurt, Mataruse, Sibongile, Skinner, Steven R, Belyanskaya, Svetlana L, Carpenter, Tiffany Y, Shearer, Todd W, Clark, Matthew A, Cuozzo, John W, Arico-Muendel, Christopher C, Morgan, Barry A

“…The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed…”
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In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor by Podolin, Patricia L., Bolognese, Brian J., Foley, Joseph F., Long, Edward, Peck, Brian, Umbrecht, Sandra, Zhang, Xiaojun, Zhu, Penny, Schwartz, Benjamin, Xie, Wensheng, Quinn, Chad, Qi, Hongwei, Sweitzer, Sharon, Chen, Stephanie, Galop, Marc, Ding, Yun, Belyanskaya, Svetlana L., Israel, David I., Morgan, Barry A., Behm, David J., Marino, Joseph P., Kurali, Edit, Barnette, Mary S., Mayer, Ruth J., Booth-Genthe, Catherine L., Callahan, James F.

“…► A novel, potent, selective inhibitor of human, rat and mouse sEH, GSK2256294A, is described. ► In vitro, GSK2256294A exhibits concentration-dependent…”
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Discovery of Potent and Selective Inhibitors for ADAMTS‑4 through DNA-Encoded Library Technology (ELT) by Ding, Yun, O’Keefe, Heather, DeLorey, Jennifer L, Israel, David I, Messer, Jeffrey A, Chiu, Cynthia H, Skinner, Steven R, Matico, Rosalie E, Murray-Thompson, Monique F, Li, Fan, Clark, Matthew A, Cuozzo, John W, Arico-Muendel, Christopher, Morgan, Barry A

“…The aggrecan degrading metalloprotease ADAMTS-4 has been identified as a novel therapeutic target for osteoarthritis. Here, we use DNA-encoded Library…”
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Characterization of Specific N -α-Acetyltransferase 50 (Naa50) Inhibitors Identified Using a DNA Encoded Library by Kung, Pei-Pei, Bingham, Patrick, Burke, Benjamin J., Chen, Qiuxia, Cheng, Xuemin, Deng, Ya-Li, Dou, Dengfeng, Feng, Junli, Gallego, Gary M., Gehring, Michael R., Grant, Stephan K., Greasley, Samantha, Harris, Anthony R., Maegley, Karen A., Meier, Jordan, Meng, Xiaoyun, Montano, Jose L., Morgan, Barry A., Naughton, Brigitte S., Palde, Prakash B., Paul, Thomas A., Richardson, Paul, Sakata, Sylvie, Shaginian, Alex, Sonnenburg, William K., Subramanyam, Chakrapani, Timofeevski, Sergei, Wan, Jinqiao, Yan, Wen, Stewart, Albert E.

“…Two novel compounds were identified as Naa50 binders/inhibitors using DNA-encoded technology screening. Biophysical and biochemical data as well as cocrystal…”
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Discovery, SAR, and X‑ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library by Deng, Hongfeng, Zhou, Jingye, Sundersingh, Flora S, Summerfield, Jennifer, Somers, Don, Messer, Jeffrey A, Satz, Alexander L, Ancellin, Nicolas, Arico-Muendel, Christopher C, (Sargent) Bedard, Katie L, Beljean, Arthur, Belyanskaya, Svetlana L, Bingham, Ryan, Smith, Sarah E, Boursier, Eric, Carter, Paul, Centrella, Paolo A, Clark, Matthew A, Chung, Chun-wa, Davie, Christopher P, Delorey, Jennifer L, Ding, Yun, Franklin, G. Joseph, Grady, LaShadric C, Herry, Kenny, Hobbs, Clare, Kollmann, Christopher S, Morgan, Barry A, (Pothier) Kaushansky, Laura J, Zhou, Quan

“…As a potential target for obesity, human BCATm was screened against more than 14 billion DNA encoded compounds of distinct scaffolds followed by off-DNA…”
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Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis by Deng, Hongfeng, Bernier, Sylvie G, Doyle, Elisabeth, Lorusso, Jeanine, Morgan, Barry A, Westlin, William F, Evindar, Ghotas

“…To develop effective oral treatment for multiple sclerosis (MS), we discovered a series of alkyl-substituted biaryl amino alcohols as selective S1P1…”
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Exploring amino acids derivatives as potent, selective, and direct agonists of sphingosine-1-phosphate receptor subtype-1 by Evindar, Ghotas, Deng, Hongfeng, Bernier, Sylvie G, Doyle, Elisabeth, Lorusso, Jeanine, Morgan, Barry A, Westlin, William F

“…In the quest to discover a potent and selective class of direct agonists to the sphingosine-1-phosphate receptor, we explored the carboxylate functional group…”
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Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity by Arico-Muendel, Christopher C, Belanger, Bruce, Benjamin, Dennis, Blanchette, Heather S, Caiazzo, Teresa M, Centrella, Paolo A, DeLorey, Jennifer, Doyle, Elisabeth G, Gradhand, Ulrike, Griffin, Sarah T, Hill, Susan, Labenski, Matthew T, Morgan, Barry A, O'Donovan, Gary, Prasad, Kavirayani, Skinner, Steven, Taghizadeh, Nazbeh, Thompson, Charles D, Wakefield, James, Westlin, William, White, Kerry F

“…The natural product fumagillin exhibits potent antiproliferative and antiangiogenic properties. The semisynthetic analog PPI-2458,…”
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Carbamate Analogues of Fumagillin as Potent, Targeted Inhibitors of Methionine Aminopeptidase-2 by Arico-Muendel, Christopher C, Benjamin, Dennis R, Caiazzo, Teresa M, Centrella, Paolo A, Contonio, Brooke D, Cook, Charles M, Doyle, Elisabeth G, Hannig, Gerhard, Labenski, Matthew T, Searle, Lily L, Lind, Kenneth, Morgan, Barry A, Olson, Gary, Paradise, Christopher L, Self, Christopher, Skinner, Steven R, Sluboski, Barbara, Svendsen, Jennifer L, Thompson, Charles D, Westlin, William, White, Kerry F

“…Inhibition of methionine aminopeptidase-2 (MetAP2) represents a novel approach to antiangiogenic therapy. We describe the synthesis and activity of fumagillin…”
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Exploration of amino alcohol derivatives as novel, potent, and highly selective sphingosine-1-phosphate receptor subtype-1 agonists by Evindar, Ghotas, Bernier, Sylvie G., Doyle, Elisabeth, Kavarana, Malcolm J., Satz, Alexander L., Lorusso, Jeanine, Blanchette, Heather S., Saha, Ashis K., Hannig, Gerhard, Morgan, Barry A., Westlin, William F.

“…Identification of a selectivity enhancing moiety has allowed for discovery of pro-drug PPI-4955 ( 21b), a potent and selective sphingosine-1-phosphate…”
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Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists by Evindar, Ghotas, Bernier, Sylvie G., Kavarana, Malcolm J., Doyle, Elisabeth, Lorusso, Jeanine, Kelley, Michael S., Halley, Keith, Hutchings, Amy, Wright, Albion D., Saha, Ashis K., Hannig, Gerhard, Morgan, Barry A., Westlin, William F.

“…Discovery of two potent and selective sphingosine-1-phosphate receptor agonist chemotypes, alkoxy-phenylamide and alkoxy-phenylimidazole, with potent in vivo…”
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Orally Active Fumagillin Analogues: Transformations of a Reactive Warhead in the Gastric Environment by Arico-Muendel, Christopher C, Blanchette, Heather, Benjamin, Dennis R, Caiazzo, Teresa M, Centrella, Paolo A, DeLorey, Jennifer, Doyle, Elisabeth G, Johnson, Steven R, Labenski, Matthew T, Morgan, Barry A, O’Donovan, Gary, Sarjeant, Amy A, Skinner, Steven, Thompson, Charles D, Griffin, Sarah T, Westlin, William, White, Kerry F

“…Semisynthetic analogues of fumagillin, 1, inhibit methionine aminopeptidase-2 (MetAP2) and have entered the clinic for the treatment of cancer. An optimized…”
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Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists by Evindar, Ghotas, Satz, Alexander L., Bernier, Sylvie G., Kavarana, Malcolm J., Doyle, Elisabeth, Lorusso, Jeanine, Taghizadeh, Nazbeh, Halley, Keith, Hutchings, Amy, Kelley, Michael S., Wright, Albion D., Saha, Ashis K., Hannig, Gerhard, Morgan, Barry A., Westlin, William F.

“…In pursuit of potent and selective sphingosine-1-phosphate receptor agonists, further SAR expansion on our previously reported scaffolds led to discovery of…”
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Rapid Determination of Substrate Specificity of Clostridium histolyticum β-Collagenase Using an Immobilized Peptide Library by Hu, Yongbo, Webb, Erin, Singh, Jasbir, Morgan, Barry A., Gainor, James A., Gordon, Thomas D., Siahaan, Teruna J.

“…The molecular basis of the substrate specificity of Clostridium histolyticum β-collagenase was investigated using a combinatorial method. An immobilized…”
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