Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Nicole Barucci"'
Autor:
Gregory H. Bird, J. J. Patten, William Zavadoski, Nicole Barucci, Marina Godes, Benjamin M. Moyer, Callum D. Owen, Paul DaSilva-Jardine, Donna S. Neuberg, Richard A. Bowen, Robert A. Davey, Loren D. Walensky
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-15 (2024)
Abstract The continued emergence of highly pathogenic viruses, which either thwart immune- and small molecule-based therapies or lack interventions entirely, mandates alternative approaches, particularly for prompt and facile pre- and post-exposure p
Externí odkaz:
https://doaj.org/article/379e0f8e24a44fc788e840416e81045c
Autor:
Derek M Erion, Amanda Lapworth, Paul A Amor, Guoyun Bai, Nicholas B Vera, Ronald W Clark, Qingyun Yan, Yimin Zhu, Trenton T Ross, Julie Purkal, Matthew Gorgoglione, Guodong Zhang, Vinicius Bonato, Levenia Baker, Nicole Barucci, Theresa D'Aquila, Alan Robertson, Robert J Aiello, Jiangli Yan, Jeff Trimmer, Timothy P Rolph, Jeffrey A Pfefferkorn
Publikováno v:
PLoS ONE, Vol 9, Iss 5, p e97139 (2014)
Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importan
Externí odkaz:
https://doaj.org/article/646e9e91d00f42f6a75e558c5e50e7cf
Autor:
Qing Zhang, William J. Zavadoski, Robert J. Aiello, M.C. Holt, Nicole Barucci, Jim Valentine, A.J. Stein, Vishwas M. Paralkar, Stéphane De Lombaert, Daniel R. Goldberg, Patricia Bourassa
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 27:413-419
As a follow-up to the discovery of our spirocyclic proline-based TPH1 inhibitor lead, we describe the optimization of this scaffold. Through a combination of X-ray co-crystal structure guided design and an in vivo screen, new substitutions in the lip
Autor:
Nicole Barucci, Stéphane De Lombaert, Vishwas M. Paralkar, Jim Valentine, William J. Zavadoski, Patricia Bourassa, Robert J. Aiello, A.J. Stein, Daniel R. Goldberg, Qing Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2855-2860
An increasing number of diseases have been linked to a dysfunctional peripheral serotonin system. Given that tryptophan hydroxylase 1 (TPH1) is the rate limiting enzyme in the biosynthesis off serotonin, it represents an attractive target to regulate
Autor:
Patricia Bourassa, Nicole Barucci, Stéphane De Lombaert, William J. Zavadoski, Daniel R. Goldberg, Qing Zhang, Robert J. Aiello, James J. Valentine, Vishwas M. Paralkar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:1124-1129
The central role of the biogenic monoamine serotonin (5-hydroxytryptamine, 5-HT) as a neurotransmitter with important cognitive and behavioral functions is well known. However, 5-HT produced in the brain only accounts for approximately 5% of the tota
Autor:
Jeffrey A, Pfefferkorn, Meihua, Tu, Kevin J, Filipski, Angel, Guzman-Perez, Jianwei, Bian, Gary E, Aspnes, Matthew F, Sammons, Wei, Song, Jian-Cheng, Li, Christopher S, Jones, Leena, Patel, Tim, Rasmusson, Dongxiang, Zeng, Kapil, Karki, Michael, Hamilton, Richard, Hank, Karen, Atkinson, John, Litchfield, Robert, Aiello, Levenia, Baker, Nicole, Barucci, Patricia, Bourassa, Francis, Bourbonais, Francis, Bourbounais, Theresa, D'Aquila, David R, Derksen, Margit, MacDougall, Alan, Robertson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7100-7105
Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identificatio
Autor:
Jing Chen, Spiros Liras, Manthena V.S. Varma, Judith L. Treadway, Martha L. Minich, Laurel Sweet, John D. Knafels, Karen Atkinson, Nahor Haddish-Berhane, Angel Guzman-Perez, Benjamin D. Stevens, Alan Robertson, Sharad B. Murdande, David B. Duignan, Mark Ammirati, Timothy P. Rolph, William J. Zavadoski, Christopher S. Jones, Patricia Bourassa, Jeffrey A. Pfefferkorn, John Litchfield, Lili Yao, Kevin J. Filipski, Margit MacDougall, Levenia Baker, John C. Pettersen, Theresa D’Aquila, Ayman El-Kattan, Bo Feng, Francis Bourbonais, Meihua Tu, Robert J. Aiello, Gary Erik Aspnes, Jianwei Bian, David R. Derksen, Paul DaSilva-Jardine, Beijing Tan, James A. Landro, Over Cabrera, Rachel E. Kosa, Hud Lawrence Risley, Shenping Liu, Amanda L. Lapworth, Nicole Barucci
Publikováno v:
Journal of Medicinal Chemistry. 55:1318-1333
Glucokinase is a key regulator of glucose homeostasis, and small molecule allosteric activators of this enzyme represent a promising opportunity for the treatment of type 2 diabetes. Systemically acting glucokinase activators (liver and pancreas) hav
Autor:
Nicole Barucci, Herbert Ogutu, Laurel Sweet, Ronda Ott-Morgan, Louis-David Cantin, Yaxin Li, James N. Livingston, Philip Wickens, Lei Zhu, Sidney X. Liang, Jennifer Burke, Timothy B. Lowinger, Zhonghua Zhang, Bullock William H, Michelle Daly, Robert Schoenleber, Lynn Decarr, Steven Magnuson, Adrian Tersteegen, Ann Gore-Willse, Ellalahewage Kumarasinghe, Alan Olague, Jian Zhu, Marina Breuhaus, David E. Gunn, Margit L. MacDougall, Thomas H. Claus, Helana Hoover-Litty
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2869-2873
Modulation of cAMP levels has been linked to insulin secretion in preclinical animal models and in humans. The high expression of PDE-10A in pancreatic islets suggested that inhibition of this enzyme may provide the necessary modulation to elicit inc
Autor:
William J. Zavadoski, Daniel R. Goldberg, Patricia-Ann Bourassa, Nicole Barucci, Stéphane De Lombaert, Qing Zhang, Robert J. Aiello, Jeffrey Dubins, Vishwas Paralkar
Publikováno v:
4.3 Pulmonary Circulation and Pulmonary Vascular Disease.
Pulmonary arterial hypertension (PAH) is a progressive disease defined by an elevation in pulmonary arterial pressure with extensive pulmonary vascular remodeling and perivascular mast cell accumulation. While the exact etiology of the disease is unk
Autor:
Timothy P. Rolph, Jiangli Yan, Levenia Baker, Alan Robertson, Vinicius Bonato, Jeffrey A. Pfefferkorn, Paul A. Amor, Jeff K. Trimmer, Theresa D’Aquila, Guoyun Bai, Derek M. Erion, Qingyun Yan, Yimin Zhu, Nicole Barucci, Matthew Gorgoglione, Nicholas B. Vera, Ronald W. Clark, Julie Purkal, Robert J. Aiello, Amanda L. Lapworth, Trenton T. Ross, Guodong Zhang
Publikováno v:
PLoS ONE, Vol 9, Iss 5, p e97139 (2014)
PLoS ONE
PLoS ONE
Hyperglycemia resulting from type 2 diabetes mellitus (T2DM) is the main cause of diabetic complications such as retinopathy and neuropathy. A reduction in hyperglycemia has been shown to prevent these associated complications supporting the importan