Zobrazeno 1 - 10
of 43
pro vyhledávání: '"David K. Clawson"'
Autor:
Kristy Kikly, Howard Barff Broughton, William Chang, Selma Sapmaz, Richard Morphy, Holly A. Bina, Jim D. Durbin, Sherry Y Guo, Timothy Ivo Richardson, Jimmy P Steele, Ryan Edward Stites, Brian G. Getman, Vaught Grant Matthews, Veavi Ching-Yun Chang, Pamela K. Shetler, Greg L Durst, Denise D Edmondson, Rob Barr, Helene Rudyk, Charles Willis Lugar, Nita J. Patel, Christian Alexander Clarke, Kelly Wayne Furness, Nicole E New, David K. Clawson, Keith R. Stayrook, Mark Chambers, Brian Michael Mathes, Stephanie L. Stout, Wendy H. Gough
Publikováno v:
Journal of Medicinal Chemistry. 64:5470-5484
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::3a80dc241f7e50c8ddb367cc37ea913c
https://doi.org/10.1021/acs.jmedchem.0c01918
https://doi.org/10.1021/acs.jmedchem.0c01918
Autor:
Charles W, Lugar, Christian A, Clarke, Richard, Morphy, Helene, Rudyk, Selma, Sapmaz, Ryan E, Stites, Grant M, Vaught, Kelly, Furness, Howard B, Broughton, Greg L, Durst, David K, Clawson, Stephanie L, Stout, Sherry Y, Guo, Jim D, Durbin, Keith R, Stayrook, Denise D, Edmondson, Kristy, Kikly, Nicole E, New, Holly A, Bina, Mark G, Chambers, Pamela, Shetler, William Y, Chang, Veavi Ching-Yun, Chang, Rob, Barr, Wendy H, Gough, Jimmy P, Steele, Brian, Getman, Nita, Patel, Brian M, Mathes, Timothy I, Richardson
Publikováno v:
Journal of medicinal chemistry. 64(9)
The Th17 pathway has been implicated in autoimmune diseases. The retinoic acid receptor-related orphan receptor C2 (RORγt) is a master regulator of Th17 cells and controls the expression of IL-17A. RORγt is expressed primarily in IL-17A-producing l
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ef03d39fb502b855beadc34c7a19e1e7
https://pubmed.ncbi.nlm.nih.gov/33852312
https://pubmed.ncbi.nlm.nih.gov/33852312
Autor:
Frances Lu, Bryan G. Johnson, Daniel Ursu, Joan H. Carter, Lisa M. Broad, Kofi Adragni, Shane Atwell, Jing Wang, David K. Clawson, Beverly A. Heinz, Steven P. Swanson, James A. Monn, Qi Chen, Helene E. Sanger, David B. Shaw, Steven Marc Massey, Xushan Wang, Marijane Russell, Steven S. Henry, Junliang Hao, Rajni M. Bhardwaj, Diseroad Benjamin Alan, David L. McKinzie, Brian G. Getman, John T. Catlow
Publikováno v:
Journal of Medicinal Chemistry. 61:2303-2328
Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu3) receptors, but small molecule tools are lacking. As part of our ongoing efforts to identify potent, selective, an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::34fd3a986aac486e41e6ea738f1a4465
https://doi.org/10.1021/acs.jmedchem.7b01481
https://doi.org/10.1021/acs.jmedchem.7b01481
Autor:
Michael Lahn, Faming Zhang, William T. McMillen, Jeremy R. Graff, Rikke B. Holmgaard, Chandrasekar V. Iyer, Jason Manro, Bryan D. Anderson, Douglas W. Beight, Maria Jose Lallena, Kyla Driscoll, Lei Yan, J. Scott Sawyer, Michael Kalos, Karen S. Britt, David K. Clawson, Philip W. Iversen, Rolf A. Brekken, Karim A. Benhadji, Xiaohong Xu, Durisala Desaiah, Jonathan Michael Yingling, Huocong Huang
Publikováno v:
Oncotarget
Transforming growth factor-β (TGFβ) is an important driver of tumor growth via intrinsic and extrinsic mechanisms, and is therefore an attractive target for developing cancer therapeutics. Using preclinical models, we characterized the anti-tumor a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6d8441d71dc2f3af0b1cfba12364fde
https://doi.org/10.18632/oncotarget.23795
https://doi.org/10.18632/oncotarget.23795
Autor:
Holly A. Bina, Bryan Edward Jones, Yan Ji, Jirong Lu, Victor J. Wroblewski, Robert J. Benschop, Qing Chai, Stacy Torgerson, Barrett Allan, James Nelson, Shane Atwell, Ningjie Hu, Chi-Kin Chow, Yu Tian, David K. Clawson, Mahmoud Ghanem, Barbra Barmettler, J.R. Fitchett, Joseph Manetta
Publikováno v:
MAbs
We describe a bispecific dual-antagonist antibody against human B cell activating factor (BAFF) and interleukin 17A (IL-17). An anti-IL-17 single-chain variable fragment (scFv) derived from ixekizumab (Taltz®) was fused via a glycine-rich linker to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::875fe1f65f13696c2fbf292fb27f362d
https://pubmed.ncbi.nlm.nih.gov/31181988
https://pubmed.ncbi.nlm.nih.gov/31181988
Autor:
Yilin Meng, Cen Gao, Michal Vieth, Shane Atwell, Marijane Russell, Benoît Roux, David K. Clawson
Understanding protein conformational variability remains a challenge in drug discovery. The issue arises in protein kinases, whose multiple conformational states can affect the binding of small-molecule inhibitors. To overcome this challenge, we prop
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1f561d0d49719d28f107f83c9e480c8e
https://europepmc.org/articles/PMC6317529/
https://europepmc.org/articles/PMC6317529/
Autor:
James A, Monn, Steven S, Henry, Steven M, Massey, David K, Clawson, Qi, Chen, Benjamin A, Diseroad, Rajni M, Bhardwaj, Shane, Atwell, Frances, Lu, Jing, Wang, Marijane, Russell, Beverly A, Heinz, Xu-Shan, Wang, Joan H, Carter, Brian G, Getman, Kofi, Adragni, Lisa M, Broad, Helene E, Sanger, Daniel, Ursu, John T, Catlow, Steven, Swanson, Bryan G, Johnson, David B, Shaw, David L, McKinzie, Junliang, Hao
Publikováno v:
Journal of medicinal chemistry. 61(6)
Multiple therapeutic opportunities have been suggested for compounds capable of selective activation of metabotropic glutamate 3 (mGlu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::0b0a91b923b376e1620dd4223a841b23
https://pubmed.ncbi.nlm.nih.gov/29350927
https://pubmed.ncbi.nlm.nih.gov/29350927
Autor:
Mark G. Bures, David Edward Tupper, Joan H. Carter, James A. Monn, David L. McKinzie, Marijane Russell, Lourdes Prieto, Steven S. Henry, Reinhard Matthew Robert, Alicia Marcos, Lesley Walton, Christopher David Beadle, Bryan G. Johnson, Brian G. Getman, John T. Catlow, Frances Lu, Xushan Wang, Lorena Taboada, S. Richard Baker, Beverly A. Heinz, Helene Rudyk, David B. Shaw, Jaime Blanco, Carlos Lamas, Steven Swanson, David K. Clawson, Junliang Hao, Carlos Montero, Teresa Man, Shane Atwell, Barry Peter Clark, Jing Wang
Publikováno v:
Journal of Medicinal Chemistry. 58:7526-7548
Identification of orthosteric mGlu(2/3) receptor agonists capable of discriminating between individual mGlu2 and mGlu3 subtypes has been highly challenging owing to the glutamate-site sequence homology between these proteins. Herein we detail the pre
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::13d4b305d2ec1acea2f3d473c73251c1
https://doi.org/10.1021/acs.jmedchem.5b01124
https://doi.org/10.1021/acs.jmedchem.5b01124
Autor:
Matthew W. Carson, Robert J. Barr, Dana Sindelar, Daniel Timothy Kohlman, Bradley Condon, David K. Clawson, A. Pustilnik, M. Joelle Dill, James S. Bean, John G. Luz, Michael J. Coghlan, Milan Maletic
Publikováno v:
Journal of Medicinal Chemistry. 58:6607-6618
To further elucidate the structural activity correlation of glucocorticoid receptor (GR) antagonism, the crystal structure of the GR ligand-binding domain (GR LBD) complex with a nonsteroidal antagonist, compound 8, was determined. This novel indole
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05523d9b3d43e70486cf70fa19d94a56
https://doi.org/10.1021/acs.jmedchem.5b00736
https://doi.org/10.1021/acs.jmedchem.5b00736
Autor:
Junliang Hao, Matt R. Reinhard, Barry Peter Clark, Jaime Blanco, Concepción Pedregal, Shane Atwell, Michael P. Johnson, Paul Goldsmith, Carlos Montero, Rosa Maria A. Simmons, James A. Monn, Steven Swanson, Chuanxi Xiang, Bryan G. Johnson, Frances Lu, Lorena Taboada, Teresa Man, David K. Clawson, Marijane Russell, Lesley Walton, Steven S. Henry, Jing Wang, Beverly A. Heinz, S. Richard Baker, Helen E. Sanger, Xushan Wang, David B. Shaw, Lourdes Prieto, Mark G. Bures, Joan H. Carter, Lisa M. Broad, Kelly L. Knopp, Helene Rudyk, David L. McKinzie, David Edward Tupper, Christopher David Beadle, John T. Catlow, Carlos Lamas, Alicia Marcos
Publikováno v:
Journal of Medicinal Chemistry. 58:1776-1794
As part of our ongoing research to identify novel agents acting at metabotropic glutamate 2 (mGlu2) and 3 (mGlu3) receptors, we have previously reported the identification of the C4α-methyl analog of mGlu2/3 receptor agonist 1 (LY354740). This molec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::527bce29ceb86979086e1027b9d87633
https://doi.org/10.1021/jm501612y
https://doi.org/10.1021/jm501612y