Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Justin A. Caravella"'
Autor:
Justin A. Caravella, Daliya Banerjee, Noel A. Powell, Jason D. Fontenot, Andres McKenzie, Istvan J. Enyedy, Victor Sukbong Hong, Douglas Marcotte, Laura Silvian, Jianhua Chao, Kurt Van Vloten
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:2459-2463
RORγ plays a critical role in controlling a pro-inflammatory gene expression program in several lymphocyte lineages including T cells, γδ T cells, and innate lymphoid cells. RORγ-mediated inflammation has been linked to susceptibility to Crohn's
Autor:
Stephen Demarest, Justin A. Caravella, Elizabeth A. Proctor, Pradeep Kota, Nikolay V. Dokholyan
Publikováno v:
Proteins: Structure, Function, and Bioinformatics. 81:884-895
The ability to generate and design antibodies recognizing specific targets has revolutionized the pharmaceutical industry and medical imaging. Engineering antibody therapeutics in some cases requires modifying their constant domains to enable new and
Autor:
Justin A. Caravella, Alexey Lugovskoy
Publikováno v:
Current Opinion in Chemical Biology. 14:520-528
Since the first protein therapeutics were approved two decades ago, the field has seen a transition from the development of naturally occurring proteins to design of molecules engineered for optimal target recognition, pharmacokinetics, biodistributi
Publikováno v:
Current Computer Aided-Drug Design. 6:128-138
Monoclonal antibodies capable of recognizing antigens with high affinity and specificity represent a wellestablished class of biological agents. Since the development of hybridoma technology in 1975, advances in recombinant DNA technologies and compu
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:
Justin A. Caravella, David N. Deaton, Katrina L. Creech, G. Bruce Wisely, Jonathan Y. Bass, Lihong Chen, Harry B. Marr, Robert B. McFadyen, Shawn P. Williams, Richard Dana Caldwell, Kevin P. Madauss, Aaron B. Miller, Derek J. Parks, Dan Todd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2969-2973
Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this series, with a tether between the isoxazole ring and the 3-posit
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
Autor:
Istvan Kaldor, Boggs Sharon Davis, David N. Deaton, Katrina L. Creech, Lihong Chen, Justin A. Caravella, Terrence L. Smalley, Derek J. Parks
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(2)
The farnesoid X receptor (FXR) may play a crucial role in a number of metabolic diseases and, as such, could potentially serve as a target for the development of therapeutics as a treatment for those diseases. Previous work has described GW4064 as an
Publikováno v:
Journal of the American Chemical Society. 121:4340-4347
Affinity capillary electrophoresis and protein charge ladders are used together to measure the contributions of long-range electrostatic interactions to binding of substituted benzene sulfonamide inhibitors to derivatives of human carbonic anhydrase
Publikováno v:
Proteins: Structure, Function, and Genetics. 24:394-401
A model of the structure of erythropoietin (Epo) is presented based on structural homology to other hemopoietic cytokines. A model of the erythropoietin receptor complex was made based on evidence that this includes a homodimer of the receptor chain