Search Results - "Kostich, Walter"

Pathways to cures for multiple sclerosis: A research roadmap by Bebo, Bruce F, Allegretta, Mark, Landsman, Douglas, Zackowski, Kathy M, Brabazon, Fiona, Kostich, Walter A, Coetzee, Timothy, Ng, Alexander Victor, Marrie, Ruth Ann, Monk, Kelly R, Bar-Or, Amit, Whitacre, Caroline C

“…Background: Multiple Sclerosis (MS) is a growing global health challenge affecting nearly 3 million people. Progress has been made in the understanding and…”
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Discovery of (S)‑1-((2′,6-Bis(difluoromethyl)-[2,4′-bipyridin]-5-yl)oxy)-2,4-dimethylpentan-2-amine (BMS-986176/LX-9211): A Highly Selective, CNS Penetrable, and Orally Active Adaptor Protein‑2 Associated Kinase 1 Inhibitor in Clinical Trials for the Treatment of Neuropathic Pain by Luo, Guanglin, Chen, Ling, Kostich, Walter A., Hamman, Brian, Allen, Jason, Easton, Amy, Bourin, Clotilde, Gulianello, Michael, Lippy, Jonathan, Nara, Susheel, Maishal, Tarun Kumar, Thiyagarajan, Kamalraj, Jalagam, Prasadrao, Pattipati, Sreenivasulu Naidu, Dandapani, Kumaran, Dokania, Manoj, Vattikundala, Pradeep, Sharma, Vivek, Elavazhagan, Saravanan, Verma, Manoj Kumar, Das, Manish Lal, Wagh, Santosh, Balakrishnan, Anand, Johnson, Benjamin M., Santone, Kenneth S., Thalody, George, Denton, Rex, Saminathan, Hariharan, Holenarsipur, Vinay K., Kumar, Anoop, Rao, Abhijith, Putlur, Siva Prasad, Sarvasiddhi, Sarat Kumar, Shankar, Ganesh, Louis, Justin V., Ramarao, Manjunath, Conway, Charles M., Li, Yu-Wen, Pieschl, Rick, Tian, Yuan, Hong, Yang, Ditta, Jonathan, Mathur, Arvind, Li, Jianqing, Smith, Daniel, Pawluczyk, Joseph, Sun, Dawn, Yip, Shiuhang, Wu, Dauh-Rurng, Vetrichelvan, Muthalagu, Gupta, Anuradha, Wilson, Alan, Gopinathan, Suma, Wason, Suman, Bristow, Linda, Albright, Charles F., Bronson, Joanne J., Macor, John E., Dzierba, Carolyn D.

“…Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. Potent small-molecule…”
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Discovery and Optimization of Biaryl Alkyl Ethers as a Novel Class of Highly Selective, CNS-Penetrable, and Orally Active Adaptor Protein-2-Associated Kinase 1 (AAK1) Inhibitors for the Potential Treatment of Neuropathic Pain by Luo, Guanglin, Chen, Ling, Kostich, Walter A., Hamman, Brian, Allen, Jason, Easton, Amy, Bourin, Clotilde, Gulianello, Michael, Lippy, Jonathan, Nara, Susheel, Pattipati, Sreenivasulu Naidu, Dandapani, Kumaran, Dokania, Manoj, Vattikundala, Pradeep, Sharma, Vivek, Elavazhagan, Saravanan, Verma, Manoj Kumar, Lal Das, Manish, Wagh, Santosh, Balakrishnan, Anand, Johnson, Benjamin M., Santone, Kenneth S., Thalody, George, Denton, Rex, Saminathan, Hariharan, Holenarsipur, Vinay K., Kumar, Anoop, Rao, Abhijith, Putlur, Siva Prasad, Sarvasiddhi, Sarat Kumar, Shankar, Ganesh, Louis, Justin V., Ramarao, Manjunath, Conway, Charles M., Li, Yu-Wen, Pieschl, Rick, Tian, Yuan, Hong, Yang, Bristow, Linda, Albright, Charles F., Bronson, Joanne J., Macor, John E., Dzierba, Carolyn D.

“…Recent mouse knockout studies identified adapter protein-2-associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. BMS-986176/LX-9211 (4),…”
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Bicyclic Heterocyclic Replacement of an Aryl Amide Leading to Potent and Kinase-Selective Adaptor Protein 2‑Associated Kinase 1 Inhibitors by Hartz, Richard A, Ahuja, Vijay T, Nara, Susheel J, Kumar, C. M. Vijaya, Manepalli, Raju K. V. L. P, Sarvasiddhi, Sarat Kumar, Honkhambe, Swarnamba, Patankar, Vidya, Dasgupta, Bireshwar, Rajamani, Ramkumar, Muckelbauer, Jodi K, Camac, Daniel M, Ghosh, Kaushik, Pokross, Matthew, Kiefer, Susan E, Brown, Jeffrey M, Hunihan, Lisa, Gulianello, Michael, Lewis, Martin, Lippy, Jonathan S, Surti, Neha, Hamman, Brian D, Allen, Jason, Kostich, Walter A, Bronson, Joanne J, Macor, John E, Dzierba, Carolyn D

“…Adaptor protein 2-associated kinase 1 (AAK1) is a serine/threonine kinase that was identified as a therapeutic target for the potential treatment of…”
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Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists by Mercer, Stephen E., Chaturvedula, Prasad V., Conway, Charles M., Cook, Deborah A., Davis, Carl D., Pin, Sokhom S., Macci, Robert, Schartman, Richard, Signor, Laura J., Widmann, Kimberly A., Whiterock, Valerie J., Chen, Ping, Xu, Cen, Herbst, John J., Kostich, Walter A., Thalody, George, Macor, John E., Dubowchik, Gene M.

“…[Display omitted] Calcitonin gene-related peptide (CGRP) receptor antagonists have been shown clinically to be effective treatments for migraine. Zavegepant…”
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Discovery of (5S,6S,9R)‑5-Amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro‑5H‑cyclohepta[b]pyridin-9-yl 4‑(2-oxo-2,3-dihydro‑1H‑imidazo[4,5‑b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): An Oral Calcitonin Gene-Related Peptide (CGRP) Antagonist in Clinical Trials for Treating Migraine by Luo, Guanglin, Chen, Ling, Conway, Charles M., Denton, Rex, Keavy, Deborah, Signor, Laura, Kostich, Walter, Lentz, Kimberley A., Santone, Kenneth S., Schartman, Richard, Browning, Marc, Tong, Gary, Houston, John G., Dubowchik, Gene M., Macor, John E.

“…Calcitonin gene-related peptide (CGRP) receptor antagonists have demonstrated clinical efficacy in the treatment of acute migraine. Herein, we describe the…”
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Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists by Tora, George, Degnan, Andrew P., Conway, Charles M., Kostich, Walter A., Davis, Carl D., Pin, Sokhom S., Schartman, Richard, Xu, Cen, Widmann, Kimberly A., Macor, John E., Dubowchik, Gene M.

“…A novel series of imidazole derivatives were identified to be potent CGRP antagonists. Extensive SAR of the imidazole ring is presented leading to the…”
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Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia by Higgins, Mendi A., Marcin, Lawrence R., Christopher Zusi, F., Gentles, Robert, Ding, Min, Pearce, Bradley C., Easton, Amy, Kostich, Walter A., Seager, Matthew A., Bourin, Clotilde, Bristow, Linda J., Johnson, Kim A., Miller, Regina, Hogan, John, Whiterock, Valerie, Gulianello, Michael, Ferrante, Meredith, Huang, Yanling, Hendricson, Adam, Alt, Andrew, Macor, John E., Bronson, Joanne J.

“…[Display omitted] Triazolopyridine ethers with mGlu2 positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and…”
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Small Molecule Receptor Protein Tyrosine Phosphatase γ (RPTPγ) Ligands That Inhibit Phosphatase Activity via Perturbation of the Tryptophan–Proline–Aspartate (WPD) Loop by Sheriff, Steven, Beno, Brett R, Zhai, Weixu, Kostich, Walter A, McDonnell, Patricia A, Kish, Kevin, Goldfarb, Valentina, Gao, Mian, Kiefer, Susan E, Yanchunas, Joseph, Huang, Yanling, Shi, Shuhao, Zhu, Shirong, Dzierba, Carolyn, Bronson, Joanne, Macor, John E, Appiah, Kingsley K, Westphal, Ryan S, O’Connell, Jonathan, Gerritz, Samuel W

“…Protein tyrosine phosphatases (PTPs) catalyze the dephosphorylation of tyrosine residues, a process that involves a conserved tryptophan–proline–aspartate…”
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Immunohistochemical visualization of corticotropin-releasing factor type 1 (CRF1) receptors in monkey brain by Kostich, Walter A., Grzanna, Reinhard, Lu, Nick Z., Largent, Brian L.

“…Corticotropin‐releasing factor receptor type 1, CRF1, plays a prominent role in the hypothalamic‐pituitary‐adrenal (HPA) axis and is implicated in the…”
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A high-throughput screen for receptor protein tyrosine phosphatase-gamma selective inhibitors by Appiah, Kingsley K, Kostich, Walter A, Gerritz, Samuel W, Huang, Yanling, Hamman, Brian D, Allen, Jason, Zhang, Wandong, Lanthorn, Thomas H, Albright, Charles F, Westphal, Ryan, Banks, Martyn N, O'Connell, Jonathan C

“…Protein tyrosine phosphatase-γ (PTP-γ) is a receptor-like PTP whose biological function is poorly understood. A recent mouse PTP-γ genetic deletion model…”
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Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase γ in three different crystal forms by Kish, Kevin, McDonnell, Patricia A., Goldfarb, Valentina, Gao, Mian, Metzler, William J., Langley, David R., Bryson, James W., Kiefer, Susan E., Carpenter, Brian, Kostich, Walter A., Westphal, Ryan S., Sheriff, Steven

“…Protein tyrosine phosphatase γ is a membrane‐bound receptor and is designated RPTPγ. RPTPγ and two mutants, RPTPγ(V948I, S970T) and RPTPγ(C858S, S970T), were…”
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Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase [gamma] in three different crystal forms by Kish, Kevin, McDonnell, Patricia A, Goldfarb, Valentina, Gao, Mian, Metzler, William J, Langley, David R, Bryson, James W, Kiefer, Susan E, Carpenter, Brian, Kostich, Walter A, Westphal, Ryan S, Sheriff, Steven

“…Protein tyrosine phosphatase [gamma] is a membrane-bound receptor and is designated RPTP[gamma]. RPTP[gamma] and two mutants, RPTP[gamma](V948I, S970T) and…”
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From the prodromal stage of multiple sclerosis to disease prevention by Marrie, Ruth Ann, Allegretta, Mark, Barcellos, Lisa F., Bebo, Bruce, Calabresi, Peter A., Correale, Jorge, Davis, Benjamin, De Jager, Philip L., Gasperi, Christiane, Greenbaum, Carla, Helme, Anne, Hemmer, Bernhard, Kanellis, Pamela, Kostich, Walter, Landsman, Douglas, Lebrun-Frenay, Christine, Makhani, Naila, Munger, Kassandra L., Okuda, Darin T., Ontaneda, Daniel, Postuma, Ronald B., Quandt, Jacqueline A., Roman, Sharon, Saidha, Shiv, Sormani, Maria Pia, Strum, Jon, Valentine, Pamela, Walton, Clare, Zackowski, Kathleen M., Zhao, Yinshan, Tremlett, Helen

“…A prodrome is an early set of signs or symptoms that indicate the onset of a disease before more typical symptoms develop. Prodromal stages are well recognized…”
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Discovery, Structure–Activity Relationships, and In Vivo Evaluation of Novel Aryl Amides as Brain Penetrant Adaptor Protein 2‑Associated Kinase 1 (AAK1) Inhibitors for the Treatment of Neuropathic Pain by Hartz, Richard A, Ahuja, Vijay T, Nara, Susheel J, Kumar, C.M. Vijaya, Brown, Jeffrey M, Bristow, Linda J, Rajamani, Ramkumar, Muckelbauer, Jodi K, Camac, Daniel, Kiefer, Susan E, Hunihan, Lisa, Gulianello, Michael, Lewis, Martin, Easton, Amy, Lippy, Jonathan S, Surti, Neha, Pattipati, Sreenivasulu N, Dokania, Manoj, Elavazhagan, Saravanan, Dandapani, Kumaran, Hamman, Brian D, Allen, Jason, Kostich, Walter, Bronson, Joanne J, Macor, John E, Dzierba, Carolyn D

“…Effective treatment of chronic pain, in particular neuropathic pain, without the side effects that often accompany currently available treatment options is an…”
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Molecular Identification and Analysis of a Novel Human Corticotropin-Releasing Factor (CRF) Receptor: The CRF2γ Receptor by Kostich, Walter A, Chen, Airu, Sperle, Karen, Largent, Brian L

“…We report the discovery of a new CRF2 receptor splice isoform found in human brain, which we have termed the CRF2γ receptor. The CRF2γ cDNA encodes for a…”
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Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain by Kostich, Walter, Hamman, Brian D, Li, Yu-Wen, Naidu, Sreenivasulu, Dandapani, Kumaran, Feng, Jianlin, Easton, Amy, Bourin, Clotilde, Baker, Kevin, Allen, Jason, Savelieva, Katerina, Louis, Justin V, Dokania, Manoj, Elavazhagan, Saravanan, Vattikundala, Pradeep, Sharma, Vivek, Das, Manish Lal, Shankar, Ganesh, Kumar, Anoop, Holenarsipur, Vinay K, Gulianello, Michael, Molski, Ted, Brown, Jeffrey M, Lewis, Martin, Huang, Yanling, Lu, Yifeng, Pieschl, Rick, O'Malley, Kevin, Lippy, Jonathan, Nouraldeen, Amr, Lanthorn, Thomas H, Ye, Guilan, Wilson, Alan, Balakrishnan, Anand, Denton, Rex, Grace, James E, Lentz, Kimberley A, Santone, Kenneth S, Bi, Yingzhi, Main, Alan, Swaffield, Jon, Carson, Ken, Mandlekar, Sandhya, Vikramadithyan, Reeba K, Nara, Susheel J, Dzierba, Carolyn, Bronson, Joanne, Macor, John E, Zaczek, Robert, Westphal, Ryan, Kiss, Laszlo, Bristow, Linda, Conway, Charles M, Zambrowicz, Brian, Albright, Charles F

“…To identify novel targets for neuropathic pain, 3097 mouse knockout lines were tested in acute and persistent pain behavior assays. One of the lines from this…”
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Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead by Luo, Guanglin, Jiang, Xiang-Jun, Chen, Ling, Conway, Charles M., Gulianello, Michael, Kostich, Walter, Keavy, Deborah, Signor, Laura J., Chen, Ping, Davis, Carl, Whiterock, Valerie J., Schartman, Richard, Widmann, Kimberly A., Macor, John E., Dubowchik, Gene M.

“…[Display omitted] In our efforts to identify orally bioavailable CGRP receptor antagonists, we previously discovered a novel series of orally available…”
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Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine by Luo, Guanglin, Chen, Ling, Conway, Charles M., Kostich, Walter, Macor, John E., Dubowchik, Gene M.

“…An asymmetric synthesis of novel heterocyclic analogue of the CGRP receptor antagonist rimegepant (BMS-927711, 3) is reported. The cycloheptane ring was…”
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Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis by Luo, Guanglin, Chen, Ling, Conway, Charles M, Kostich, Walter, Johnson, Benjamin M, Ng, Alicia, Macor, John E, Dubowchik, Gene M

“…An asymmetric synthesis of the major metabolite of the calcitonin gene-related peptide recepotor antagonist BMS-846372 is presented. The variously substituted…”
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