Search Results - "Myers, Joseph E"

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy by Dilger, Andrew K, Pabbisetty, Kumar B, Corte, James R, De Lucca, Indawati, Fang, Tianan, Yang, Wu, Pinto, Donald J. P, Wang, Yufeng, Zhu, Yeheng, Mathur, Arvind, Li, Jianqing, Hou, Xiaoping, Smith, Daniel, Sun, Dawn, Zhang, Huiping, Krishnananthan, Subramaniam, Wu, Dauh-Rurng, Myers, Joseph E, Sheriff, Steven, Rossi, Karen A, Chacko, Silvi, Zheng, Joanna J, Galella, Michael A, Ziemba, Theresa, Dierks, Elizabeth A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl, Wong, Pancras C, Luettgen, Joseph M, Wexler, Ruth R, Ewing, William R

“…Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclinical models…”
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Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212) by Pinto, Donald J. P., Orwat, Michael J., Smith, Leon M., Quan, Mimi L., Lam, Patrick Y. S., Rossi, Karen A., Apedo, Atsu, Bozarth, Jeffrey M., Wu, Yiming, Zheng, Joanna J., Xin, Baomin, Toussaint, Nathalie, Stetsko, Paul, Gudmundsson, Olafur, Maxwell, Brad, Crain, Earl J., Wong, Pancras C., Lou, Zhen, Harper, Timothy W., Chacko, Silvi A., Myers, Joseph E., Sheriff, Steven, Zhang, Huiping, Hou, Xiaoping, Mathur, Arvind, Seiffert, Dietmar A., Wexler, Ruth R., Luettgen, Joseph M., Ewing, William R.

“…Factor XIa (FXIa) is a blood coagulation enzyme that is involved in the amplification of thrombin generation. Mounting evidence suggests that direct inhibition…”
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Crystal structure of microtubule affinity-regulating kinase 4 catalytic domain in complex with a pyrazolopyrimidine inhibitor by Sack, John S., Gao, Mian, Kiefer, Susan E., Myers Jr, Joseph E., Newitt, John A., Wu, Sophie, Yan, Chunhong

“…Microtubule‐associated protein/microtubule affinity‐regulating kinase 4 (MARK4) is a serine/threonine kinase involved in the phosphorylation of MAP proteins…”
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Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability by Clark, Charles G., Rossi, Karen A., Corte, James R., Fang, Tianan, Smallheer, Joanne M., De Lucca, Indawati, Nirschl, David S., Orwat, Michael J., Pinto, Donald J.P., Hu, Zilun, Wang, Yufeng, Yang, Wu, Jeon, Yoon, Ewing, William R., Myers, Joseph E., Sheriff, Steven, Lou, Zhen, Bozarth, Jeffrey M., Wu, Yiming, Rendina, Alan, Harper, Timothy, Zheng, Joanna, Xin, Baomin, Xiang, Qian, Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Lam, Patrick Y.S.

“…[Display omitted] This manuscript describes the discovery of a series of macrocyclic inhibitors of FXIa with oral bioavailability. Assisted by structure based…”
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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties by Pinto, Donald J.P., Smallheer, Joanne M., Corte, James R., Austin, Erin J.D., Wang, Cailan, Fang, Tianan, Smith, Leon M., Rossi, Karen A., Rendina, Alan R., Bozarth, Jeffrey M., Zhang, Ge, Wei, Anzhi, Ramamurthy, Vidhyashankar, Sheriff, Steven, Myers, Joseph E., Morin, Paul E., Luettgen, Joseph M., Seiffert, Dietmar A., Quan, Mimi L., Wexler, Ruth R.

“…[Display omitted] Compound 2 was previously identified as a potent inhibitor of factor XIa lacking oral bioavailability. A structure-based approach was used to…”
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Crystal Structures of MEK1 Binary and Ternary Complexes with Nucleotides and Inhibitors by Fischmann, Thierry O, Smith, Catherine K, Mayhood, Todd W, Myers, Joseph E, Reichert, Paul, Mannarino, Anthony, Carr, Donna, Zhu, Hugh, Wong, Jesse, Yang, Rong-Sheng, Le, Hung V, Madison, Vincent S

“…MEK1 is a member of the MAPK signal transduction pathway that responds to growth factors and cytokines. We have determined that the kinase domain spans…”
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Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker by Corte, James R, Fang, Tianan, Osuna, Honey, Pinto, Donald J. P, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Harper, Timothy W, Bozarth, Jeffrey M, Wu, Yiming, Luettgen, Joseph M, Seiffert, Dietmar A, Decicco, Carl P, Wexler, Ruth R, Quan, Mimi L

“…A novel series of macrocyclic FXIa inhibitors was designed based on our lead acyclic phenyl imidazole chemotype. Our initial macrocycles, which were…”
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Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups by Corte, James R, Pinto, Donald J. P, Fang, Tianan, Osuna, Honey, Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Sun, Jung-Hui, Rampulla, Richard, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Li, Yi-Xin Cindy, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Harper, Timothy W, Huang, Christine, Zheng, Joanna J, Bozarth, Jeffrey M, Wu, Yiming, Wong, Pancras C, Crain, Earl J, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R

“…Factor XIa (FXIa) inhibitors are promising novel anticoagulants, which show excellent efficacy in preclinical thrombosis models with minimal effects on…”
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Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors by Hu, Zilun, Wang, Cailan, Han, Wei, Rossi, Karen A., Bozarth, Jeffrey M., Wu, Yiming, Sheriff, Steven, Myers, Joseph E., Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.

“…[Display omitted] Pyridazine and pyridazinone derivatives were designed and synthesized as coagulation factor XIa inhibitors. Potent and selective inhibitors…”
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Macrocyclic factor XIa inhibitors by Wang, Cailan, Corte, James R., Rossi, Karen A., Bozarth, Jeffrey M., Wu, Yiming, Sheriff, Steven, Myers, Joseph E., Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.

“…[Display omitted] A series of macrocyclic factor XIa (FXIa) inhibitors was designed based on an analysis of the crystal structures of the acyclic…”
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Orally bioavailable amine-linked macrocyclic inhibitors of factor XIa by Fang, Tianan, Corte, James R., Gilligan, Paul J., Jeon, Yoon, Osuna, Honey, Rossi, Karen A., Myers, Joseph E., Sheriff, Steven, Lou, Zhen, Zheng, Joanna J., Harper, Timothy W., Bozarth, Jeffrey M., Wu, Yiming, Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Lam, Patrick Y.S.

“…[Display omitted] The discovery of orally bioavailable FXIa inhibitors has been a challenge. Herein, we describe our efforts to address this challenge by…”
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Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency by Corte, James R., Yang, Wu, Fang, Tianan, Wang, Yufeng, Osuna, Honey, Lai, Amy, Ewing, William R., Rossi, Karen A., Myers, Joseph E., Sheriff, Steven, Lou, Zhen, Zheng, Joanna J., Harper, Timothy W., Bozarth, Jeffrey M., Wu, Yiming, Luettgen, Joseph M., Seiffert, Dietmar A., Quan, Mimi L., Wexler, Ruth R., Lam, Patrick Y.S.

“…[Display omitted] Optimization of macrocyclic inhibitors of FXIa is described which focused on modifications to both the macrocyclic linker and the P1 group…”
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Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group by Corte, James R., Fang, Tianan, Pinto, Donald J.P., Orwat, Michael J., Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashankar, Myers, Joseph E., Sheriff, Steven, Narayanan, Rangaraj, Harper, Timothy W., Zheng, Joanna J., Li, Yi-Xin, Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.

“…[Display omitted] Pyridine-based Factor XIa (FXIa) inhibitor (S)-2 was optimized by modifying the P2 prime, P1, and scaffold regions. This work resulted in the…”
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Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)‑one as the P2′ Moiety by Hu, Zilun, Wong, Pancras C, Gilligan, Paul J, Han, Wei, Pabbisetty, Kumar B, Bozarth, Jeffrey M, Crain, Earl J, Harper, Timothy, Luettgen, Joseph M, Myers, Joseph E, Ramamurthy, Vidhyashankar, Rossi, Karen A, Sheriff, Steven, Watson, Carol A, Wei, Anzi, Zheng, Joanna J, Seiffert, Dietmar A, Wexler, Ruth R, Quan, Mimi L

“…Structure–activity relationship optimization of phenylalanine P1′ and P2′ regions with a phenylimidazole core resulted in a series of potent FXIa inhibitors…”
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Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species by Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Corte, James R, Fang, Tianan, Gilligan, Paul J, Jeon, Yoon, Pabbisetty, Kumar B, Rampulla, Richard A, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Arumugam, Arunachalam, Raju, Sivashankaran, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Chacko, Silvi A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl J, Wong, Pancras C, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R

“…Oral factor XIa (FXIa) inhibitors may provide a promising new antithrombotic therapy with an improved benefit to bleeding risk profile over existing…”
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Discovery of a phenylpyrazole amide ROCK inhibitor as a tool molecule for in vivo studies by Hu, Zilun, Wang, Cailan, Glunz, Peter W., Li, Julia, Cheadle, Nathan L., Chen, Alice Y., Chen, Xue-Qing, Myers, Joseph E., Guarino, Victor R., Rose, Anne, Sack, John S., Sitkoff, Doree, Taylor, David S., Xu, Songmei, Yan, Chunhong, Zhang, Hongwei, Zhang, Lisa, Hennan, James, Adam, Leonard P., Wexler, Ruth R., Quan, Mimi L.

“…[Display omitted] •SAR optimization is explored on a series of phenylpyrazole amides in the discovery of dual ROCK1 and ROCK2 inhibitors.•ROCK1 and ROCK2…”
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Essentiality, Expression, and Characterization of the Class II 3-Hydroxy-3-Methylglutaryl Coenzyme A Reductase ofStaphylococcus aureus by E. Imogen Wilding, Dong-Yul Kim, Alexander P. Bryant, Michael N. Gwynn, R. Dwayne Lunsford, Damien McDevitt, Joseph E. Myers Jr, Martin Rosenberg, Daniel Sylvester, Cynthia V. Stauffacher, Victor W. Rodwell

“…Article Usage Stats Services JB Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group by Corte, James R., Fang, Tianan, Pinto, Donald J. P., Orwat, Michael J., Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashankar, Myers, Jr., Joseph E., Sheriff, Steven, Narayanan, Rangaraj, Harper, Timothy W., Zheng, Joanna J., Li, Yi-Xin, Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.

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Essentiality, expression, and characterization of the class II 3-hydroxy-3-methylglutaryl coenzyme A reductase of Staphylococcus aureus by Wilding, E I, Kim, D Y, Bryant, A P, Gwynn, M N, Lunsford, R D, McDevitt, D, Myers, Jr, J E, Rosenberg, M, Sylvester, D, Stauffacher, C V, Rodwell, V W

“…Sequence comparisons have implied the presence of genes encoding enzymes of the mevalonate pathway for isopentenyl diphosphate biosynthesis in the…”
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Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties by Pinto, Donald J. P., Smallheer, Joanne M., Corte, James R., Austin, Erin J. D., Wang, Cailan, Fang, Tianan, Smith, II, Leon M., Rossi, Karen A., Rendina, Alan R., Bozarth, Jeffrey M., Zhang, Ge, Wei, Anzhi, Ramamurthy, Vidhyashankar, Sheriff, Steven, Myers, Jr., Joseph E., Morin, Paul E., Luettgen, Joseph M., Seiffert, Dietmar A., Quan, Mimi L., Wexler, Ruth R.

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