Zobrazeno 1 - 10
of 172
pro vyhledávání: '"Richard A. Caldwell"'
Autor:
Richard M Caldwell, Wayne Dickey, Aaron Sawyer, Elizabeth A Mann-Salinas, Lawrence Crozier, Harold R Montgomery, Giselle Moody
Publikováno v:
Journal of Special Operations Medicine.
Autor:
Dusica Cvetinovic Santos, Klaus Urbahns, Simone C. Zimmerli, Andreas Goutopoulos, Justin R. Potnick, Andrew Bender, Michael Meyring, Adam Shutes, Christopher Charles Victor Jones, Jared Head, Ben C. Askew, Bayard R. Huck, Ansgar Wegener, Hui Qiu, Theresa L. Johnson, Nadia Brugger, Sherer Brian A, Ngan Nguyen, Mohanraj Dhanabal, Ralf Schmidt, Roland Grenningloh, Reinaldo Jones, Richard D. Caldwell, Ariele Viacava Follis, Brian Healey, Montserrat Camps, Igor Mochalkin, Federica Morandi, Lesley Liu-Bujalski, Vikram Dutt, Brian L. Hodous, Anna Gardberg, Thomas Eichhorn
Publikováno v:
Journal of Medicinal Chemistry. 62:7643-7655
Bruton's tyrosine kinase (BTK) inhibitors such as ibrutinib hold a prominent role in the treatment of B cell malignancies. However, further refinement is needed to this class of agents, particularly in terms of adverse events (potentially driven by k
Autor:
Andrew Bender, Anna Gardberg, Lesley Liu-Bujalski, Jared Head, Igor Mochalkin, Potnick Justin, Johnson Theresa L, Federica Morandi, Roland Grenningloh, Richard D. Caldwell, Reinaldo Jones, Ariele Viacava Follis, Hui Qiu, Andreas Goutopoulos, Daigen Xu, Sherer Brian A
Publikováno v:
ChemMedChem. 14:217-223
Bruton's tyrosine kinase (Btk) is an attractive target for the treatment of a wide array of B-cell malignancies and autoimmune diseases. Small-molecule covalent irreversible Btk inhibitors targeting Cys481 have been developed for the treatment of suc
Design Strategies for Second-Generation Irreversible Covalent Inhibitors of Bruton’s Tyrosine Kinase
Autor:
Momar Toure, Roland Grenningloh, Hui Qiu, Maria C. DiPoto, Richard Dana Caldwell, Rebecca Casaubon
Publikováno v:
2020 Medicinal Chemistry Reviews ISBN: 9781734427400
2020 Medicinal Chemistry Reviews
2020 Medicinal Chemistry Reviews
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::2c974bdcf7e6eb7396a0308adf2d02b9
https://doi.org/10.29200/acsmedchemrev-v55.ch21
https://doi.org/10.29200/acsmedchemrev-v55.ch21
Autor:
Constantin Neagu, Johnson Theresa L, Federica Morandi, Sherer Brian A, Roland Grenningloh, Jared Head, Reinaldo Jones, Hui Qiu, Andreas Goutopoulos, Anna Gardberg, Lesley Liu-Bujalski, Igor Mochalkin, Ariele Viacava Follis, Richard D. Caldwell
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3419-3424
Btk is an attractive target for the treatment of a range of Bcell malignancies as well as several autoimmune diseases such as murine lupus and rheumatoid arthritis. Several covalent irreversible inhibitors of Btk are currently in development includin
Autor:
Hui Tian, Richard D. Caldwell, Jayadevan Jayashankaran, Andreas Goutopoulos, Srinivasa R. Karra, Sherer Brian A, Matthew Bleich, Susan Zhang, Jeyaprakashnarayanan Seenisamy, Noune Tahmassian Morse, Potnick Justin, Chekler Eugene, Mohanraj Dhanabal, Yufang Xiao, Venkataraman Sriraman
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(13)
The P2X7 receptor (P2X7R) plays an important role in diverse conditions associated with tissue damage and inflammation, suggesting that the human P2X7R (hP2X7R) is an attractive therapeutic target. In the present study, the synthesis and structure-ac
Autor:
Anna Gardberg, Federica Morandi, Katherine Roe, Carolyn Wing, Andreas Goutopoulos, Richard D. Caldwell, Johnson Theresa L, Yi-Ying Chen, Constantin Neagu, Shashank Kulkarni, Ralf Schmidt, Roland Grenningloh, Sherer Brian A, Sven Poetzsch, Andrew Bender, Anja Goettsche, Nina Glaser, Christopher Charles Victor Jones, Xiaohua Zhu, Zahid Ali, Jared Head, Zhizhou Fang, Christine Maurer, Ariele Viacava Follis, Potnick Justin, Reinaldo Jones, Hui Qiu, Bettina Hanschke
Publikováno v:
Bioorganic & Medicinal Chemistry. 40:116163
Bruton’s tyrosine kinase (BTK) is a cytoplasmic, non-receptor tyrosine kinase member of the TEC family of tyrosine kinases. Pre-clinical and clinical data have shown that targeting BTK can be used for the treatment for B-cell disorders. Here we dis
Autor:
Jared Head, Federica Morandi, Roland Grenningloh, Andreas Goutopoulos, Anna Gardberg, Lesley Liu-Bujalski, Constantin Neagu, Reinaldo Jones, Hui Qiu, Sherer Brian A, Johnson Theresa L, Richard D. Caldwell, Ariele Viacava Follis, Igor Mochalkin
Publikováno v:
Bioorganicmedicinal chemistry letters. 28(17)
Bruton's Tyrosine Kinase (BTK) is a member of the TEC kinase family that is expressed in cells of hematopoietic lineage (e.g., in B cells, macrophages, monocytes, and mast cells). Small molecule covalent irreversible BTK inhibitor targeting Cys481 wi
Autor:
Harry B. Marr, Kevin P. Madauss, Jonathan Y. Bass, Shawn P. Williams, Dan Todd, Paul Kenneth Spearing, Adwoa Akwabi-Ameyaw, Lihong Chen, Robert B. McFadyen, Justin A. Caravella, Derek J. Parks, Frank Navas, David N. Deaton, Katrina L. Creech, G. Bruce Wisely, Richard Dana Caldwell, Aaron B. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:4733-4739
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the identification of potent full agonists 2a and 2
Autor:
Lihong Chen, Jonathan Y. Bass, David N. Deaton, Aaron B. Miller, Justin A. Caravella, Istvan Kaldor, Robert B. McFadyen, Stacey A. Jones, Dan Todd, Paul Kenneth Spearing, Kevin P. Madauss, Adwoa Akwabi-Ameyaw, Derek J. Parks, Richard Dana Caldwell, Frank Navas, Yaping Liu, Katrina L. Creech, G. Bruce Wisely, Harry B. Marr, Shawn P. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:4339-4343
Starting from the known FXR agonist GW 4064 1a, a series of stilbene replacements were prepared. The 6-substituted 1-naphthoic acid 1b was an equipotent FXR agonist with improved developability parameters relative to 1a. Analog 1b also reduced the se