Zobrazeno 1 - 10
of 33
pro vyhledávání: '"Rex, Denton"'
Autor:
Guanglin Luo, Ling Chen, Walter A. Kostich, Brian Hamman, Jason Allen, Amy Easton, Clotilde Bourin, Michael Gulianello, Jonathan Lippy, Susheel Nara, Sreenivasulu Naidu Pattipati, Kumaran Dandapani, Manoj Dokania, Pradeep Vattikundala, Vivek Sharma, Saravanan Elavazhagan, Manoj Kumar Verma, Manish Lal Das, Santosh Wagh, Anand Balakrishnan, Benjamin M. Johnson, Kenneth S. Santone, George Thalody, Rex Denton, Hariharan Saminathan, Vinay K. Holenarsipur, Anoop Kumar, Abhijith Rao, Siva Prasad Putlur, Sarat Kumar Sarvasiddhi, Ganesh Shankar, Justin V. Louis, Manjunath Ramarao, Charles M. Conway, Yu-Wen Li, Rick Pieschl, Yuan Tian, Yang Hong, Linda Bristow, Charles F. Albright, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba
Publikováno v:
Journal of Medicinal Chemistry. 65:4534-4564
Recent mouse knockout studies identified adapter protein-2-associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. BMS-986176/LX-9211 (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbf11be6e3846cab6b37f029b5b93a8d
https://doi.org/10.1021/acs.jmedchem.1c02132
https://doi.org/10.1021/acs.jmedchem.1c02132
Autor:
Guanglin Luo, Ling Chen, Walter A. Kostich, Brian Hamman, Jason Allen, Amy Easton, Clotilde Bourin, Michael Gulianello, Jonathan Lippy, Susheel Nara, Tarun Kumar Maishal, Kamalraj Thiyagarajan, Prasadrao Jalagam, Sreenivasulu Naidu Pattipati, Kumaran Dandapani, Manoj Dokania, Pradeep Vattikundala, Vivek Sharma, Saravanan Elavazhagan, Manoj Kumar Verma, Manish Lal Das, Santosh Wagh, Anand Balakrishnan, Benjamin M. Johnson, Kenneth S. Santone, George Thalody, Rex Denton, Hariharan Saminathan, Vinay K. Holenarsipur, Anoop Kumar, Abhijith Rao, Siva Prasad Putlur, Sarat Kumar Sarvasiddhi, Ganesh Shankar, Justin V. Louis, Manjunath Ramarao, Charles M. Conway, Yu-Wen Li, Rick Pieschl, Yuan Tian, Yang Hong, Jonathan Ditta, Arvind Mathur, Jianqing Li, Daniel Smith, Joseph Pawluczyk, Dawn Sun, Shiuhang Yip, Dauh-Rurng Wu, Muthalagu Vetrichelvan, Anuradha Gupta, Alan Wilson, Suma Gopinathan, Suman Wason, Linda Bristow, Charles F. Albright, Joanne J. Bronson, John E. Macor, Carolyn D. Dzierba
Publikováno v:
Journal of Medicinal Chemistry. 65:4457-4480
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::38224dcaf3d9ea2fabc4ac6df4a42a84
https://doi.org/10.1021/acs.jmedchem.1c02131
https://doi.org/10.1021/acs.jmedchem.1c02131
Autor:
Aberra Fura, Shiuhang Yip, Georgia Cornelius, Hai-Yun Xiao, Qingjie Liu, Sha Li, Ning Li, Nicholas A. Meanwell, Shailesh Dudhgaonkar, Max Ruzanov, Jenny Xie, Zili Xiao, Purnima Khandelwal, Carolyn A. Weigelt, David J. Shuster, Dauh-Rurng Wu, T. G. Murali Dhar, Tara Sherry, Yang Michael G, Kevin Stefanski, Jignesh Nagar, Rex Denton, Qihong Zhao, Peng Li, Silvi A. Chacko, Arun Govindarajan, Robert M. Borzilleri, John S. Sack, Yeheng Zhu, Yunling Song, Dawn Sun, Anjuman Rudra, Mary T. Obermeier, Jinhong Wang, Douglas G. Batt, Venkata Murali
Publikováno v:
ACS Med Chem Lett
[Image: see text] Structure–activity relationship studies directed toward the replacement of the fused phenyl ring of the lead hexahydrobenzoindole RORγt inverse agonist series represented by 1 with heterocyclic moieties led to the identification
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d3296d470de82e26da82050921646783
https://doi.org/10.1021/acsmedchemlett.1c00112
https://doi.org/10.1021/acsmedchemlett.1c00112
Autor:
Guanglin, Luo, Ling, Chen, Walter A, Kostich, Brian, Hamman, Jason, Allen, Amy, Easton, Clotilde, Bourin, Michael, Gulianello, Jonathan, Lippy, Susheel, Nara, Tarun Kumar, Maishal, Kamalraj, Thiyagarajan, Prasadrao, Jalagam, Sreenivasulu Naidu, Pattipati, Kumaran, Dandapani, Manoj, Dokania, Pradeep, Vattikundala, Vivek, Sharma, Saravanan, Elavazhagan, Manoj Kumar, Verma, Manish Lal, Das, Santosh, Wagh, Anand, Balakrishnan, Benjamin M, Johnson, Kenneth S, Santone, George, Thalody, Rex, Denton, Hariharan, Saminathan, Vinay K, Holenarsipur, Anoop, Kumar, Abhijith, Rao, Siva Prasad, Putlur, Sarat Kumar, Sarvasiddhi, Ganesh, Shankar, Justin V, Louis, Manjunath, Ramarao, Charles M, Conway, Yu-Wen, Li, Rick, Pieschl, Yuan, Tian, Yang, Hong, Jonathan, Ditta, Arvind, Mathur, Jianqing, Li, Daniel, Smith, Joseph, Pawluczyk, Dawn, Sun, Shiuhang, Yip, Dauh-Rurng, Wu, Muthalagu, Vetrichelvan, Anuradha, Gupta, Alan, Wilson, Suma, Gopinathan, Suman, Wason, Linda, Bristow, Charles F, Albright, Joanne J, Bronson, John E, Macor, Carolyn D, Dzierba
Publikováno v:
Journal of medicinal chemistry. 65(6)
Recent mouse knockout studies identified adapter protein-2 associated kinase 1 (AAK1) as a viable target for treating neuropathic pain. Potent small-molecule inhibitors of AAK1 have been identified and show efficacy in various rodent pain models. (
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::1e41976413f9c4afd18a0630ac9bd2a0
https://pubmed.ncbi.nlm.nih.gov/35257579
https://pubmed.ncbi.nlm.nih.gov/35257579
Autor:
Tara Sherry, John E. Macor, Jinhong Wang, Georgia Cornelius, Shiuhang Yip, Luisa Salter-Cid, Qingjie Liu, Purnima Khandelwal, Carolyn A. Weigelt, Max Ruzanov, John S. Sack, Kevin Stefanski, Jenny Xie, T. G. Murali Dhar, Sha Li, Melissa Yarde, Joseph A. Tino, Qihong Zhao, Dauh-Rurng Wu, Mary T. Obermeier, David J. Shuster, Aberra Fura, Douglas G. Batt, Rex Denton
Publikováno v:
ACS Med Chem Lett
[Image: see text] Employing a virtual screening approach, we identified the pyroglutamide moiety as a nonacid replacement for the cyclohexanecarboxylic acid group which, when coupled to our previously reported conformationally locked tricyclic core,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a5cac25cddf4e8f7e9938641eae9eba1
https://doi.org/10.1021/acsmedchemlett.0c00496
https://doi.org/10.1021/acsmedchemlett.0c00496
Autor:
Carolyn A. Weigelt, Sha Li, David Marcoux, Georgia Cornelius, Qihong Zhao, Mary Ellen Cvijic, John E. Macor, Jingwu Duan, Melissa Yarde, Muthalagu Vetrichelvan, David J. Shuster, Qingjie Liu, Richard Rampulla, Kim W. McIntyre, Mary T. Obermeier, Shiuhang Yip, Purnima Khandelwal, Sureshbabu Vishwakrishnan, Anuradha Gupta, Virna Borowski, Peng Li, Kevin Stefanski, Sridharan Ramlingam, Myra Beaudoin-Bertrand, Nageswara Maddala, Sridhar Vanteru, Percy H. Carter, Arvind Mathur, Aberra Fura, Max Ruzanov, John Hynes, Dauh-Rurng Wu, Jinhong Wang, Luisa Salter-Cid, John S. Sack, Cornelius Lyndon A M, Anurag S. Srivastava, Robert J. Cherney, Kumaravel Selvakumar, Mushkin Basha, Arun Kumar Gupta, Douglas G. Batt, Rex Denton, Sukhen Karmakar, Qing Shi, Ananta Karmakar, Naveen Manjunath, Javed Khan, Jenny Xie, Joseph A. Tino, T. G. Murali Dhar
Publikováno v:
Journal of Medicinal Chemistry. 62:9931-9946
RORγt is an important nuclear receptor that regulates the production of several pro-inflammatory cytokines such as IL-17 and IL-22. As a result, RORγt has been identified as a potential target for the treatment of various immunological disorders su
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0eeada291586349dd371c5b816894adb
https://doi.org/10.1021/acs.jmedchem.9b01369
https://doi.org/10.1021/acs.jmedchem.9b01369
Autor:
John E. Macor, Yunhui Zhang, James E. Grace, Lorin A. Thompson, Jeremy H. Toyn, Lawrence R. Marcin, Subramaniam Krishnananthan, Jianliang Shi, Dmitry Zuev, Daniel Smith, Jianqing Li, Yong-Jin Wu, Jason M. Guernon, Xiaoliang Zhuo, Tatyana Zvyaga, Xu Li, Arvind Mathur, John Morrison, Jere E. Meredith, Charles F. Albright, S. Roy Kimura, Mendi A. Higgins, Kimberley A. Lentz, Richard E. Olson, Rex Denton, Kenneth M. Boy, Catherine R. Burton, Ashok K. Trehan, Michael K. Ahlijanian
Publikováno v:
ACS Medicinal Chemistry Letters
A triazine hit identified from a screen of the BMS compound collection was optimized for potency, in vivo activity, and off-target profile to produce the bicyclic pyrimidine γ-secretase modulator BMS-932481. The compound showed robust reductions of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed62d494eee5e78e1c6f0f7838951135
http://europepmc.org/articles/PMC6421538
http://europepmc.org/articles/PMC6421538
Autor:
Jeremy H. Toyn, Lorin A. Thompson, Kimberley A. Lentz, Jere E. Meredith, Catherine R. Burton, Sethu Sankaranararyanan, Valerie Guss, Tracey Hall, Lawrence G. Iben, Carol M. Krause, Rudy Krause, Xu-Alan Lin, Maria Pierdomenico, Craig Polson, Alan S. Robertson, R. Rex Denton, James E. Grace, John Morrison, Joseph Raybon, Xiaoliang Zhuo, Kimberly Snow, Ramesh Padmanabha, Michele Agler, Kim Esposito, David Harden, Margaret Prack, Sam Varma, Victoria Wong, Yingjie Zhu, Tatyana Zvyaga, Samuel Gerritz, Lawrence R. Marcin, Mendi A. Higgins, Jianliang Shi, Cong Wei, Joseph L. Cantone, Dieter M. Drexler, John E. Macor, Richard E. Olson, Michael K. Ahlijanian, Charles F. Albright
Publikováno v:
International Journal of Alzheimer's Disease, Vol 2014 (2014)
Alzheimer’s disease is the most prevalent cause of dementia and is associated with accumulation of amyloid-β peptide (Aβ), particularly the 42-amino acid Aβ1-42, in the brain. Aβ1-42 levels can be decreased by γ-secretase modulators (GSM), whi
Externí odkaz:
https://doaj.org/article/1dce320132d4411583a19dcbfe2b54ae
Autor:
Qingjie Liu, Mary T. Obermeier, John S. Sack, Carolyn A. Weigelt, Georgia Cornelius, Percy H. Carter, David J. Shuster, Luisa Salter-Cid, Aberra Fura, Virna Borowski, Jingwu Duan, Purnima Khandelwal, Qing Shi, Robert J. Cherney, Cornelius Lyndon A M, Jinhong Wang, Jenny Xie, Max Ruzanov, Kevin Stefanski, Rex Denton, T. G. Murali Dhar, David Marcoux, Shiuhang Yip, Melissa Yarde, Douglas G. Batt, Javed Khan, Joseph A. Tino, Qihong Zhao, Anurag S. Srivastava, Arvind Mathur, Mary Ellen Cvijic, John E. Macor, Sha Li, Dauh-Rurng Wu
Publikováno v:
ACS Med Chem Lett
[Image: see text] Novel tricyclic analogues were designed, synthesized, and evaluated as RORγt inverse agonists. Several of these compounds were potent in an IL-17 human whole blood assay and exhibited excellent oral bioavailability in mouse pharmac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::12c0984e9b1636552c6620f1a6235555
https://pubmed.ncbi.nlm.nih.gov/32551004
https://pubmed.ncbi.nlm.nih.gov/32551004
Autor:
Regina Miller, Nicholas J. Lodge, John E. Macor, Wendy Clarke, Lizbeth Gallagher, Linda J. Bristow, Daniel G. Morgan, Christiana I. Iwuagwu, Ryan Westphal, Haiquan Fang, Kimberley A. Lentz, Debra J. Post-Munson, Amy Easton, Matthew D. Hill, Bei Wang, Robert A. Mate, Ivar M. McDonald, James H. Cook, Yulia Benitex, Dalton King, Thaddeus F. Molski, Ronald J. Knox, F. Christopher Zusi, Richard E. Olson, Rex Denton, Jingsong Fan, Rulin Zhao, Robert Zaczek
Publikováno v:
ACS Medicinal Chemistry Letters. 8:366-371
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c4993c640b254a344e08c8bc412ffe3
https://doi.org/10.1021/acsmedchemlett.7b00032
https://doi.org/10.1021/acsmedchemlett.7b00032