Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Felix Vajdos"'
Autor:
Felix Vajdos, Matt Griffor, Eric Marr, Matt Wessel, Jitesh Jani, Susan LaGreca, Erika Schmitt, Nandini Patel, Michael Luzzio, Martin Berliner, Marianne Lorenzen, Luis Martinez-Alsina, Lili Yao, Kevin Coleman, John Kath, Jing Lin, Earling Emerson, Daniel Richter, Christofer Autry, Catherine Hulford, Beth Cooper, Pamela Whalen, Ethan Ung, Walter Gregory Roberts
Supplementary Data from Antitumor Activity and Pharmacology of a Selective Focal Adhesion Kinase Inhibitor, PF-562,271
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::39af3a013b36f2e7c2d2dc161c618128
https://doi.org/10.1158/0008-5472.22377182.v1
https://doi.org/10.1158/0008-5472.22377182.v1
Autor:
Martin E. Dowty, James F. Smith, Tsung H. Lin, Brian S. Gerstenberger, Matthew C. Griffor, Brett D. Hollingshead, Roger S. Gifford, Martin Hegen, Felix Vajdos, John D. Knafels, Andrew Fensome, Mary Ellen Banker, James D. Clark
Publikováno v:
Scientific Reports, Vol 10, Iss 1, Pp 1-9 (2020)
Scientific Reports
Scientific Reports
Translation of modulation of drug target activity to therapeutic effect is a critical aspect for all drug discovery programs. In this work we describe the profiling of a non-receptor tyrosine-protein kinase (TYK2) inhibitor which shows a functionally
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2666dee375aa129903ab5f908c84a04a
http://link.springer.com/article/10.1038/s41598-020-65762-y
http://link.springer.com/article/10.1038/s41598-020-65762-y
Autor:
Brett D. Hollingshead, Fabien Vincent, Tsung H. Lin, John I. Trujillo, Betsy Pierce, Andrew Fensome, Brian S. Gerstenberger, Martin E. Dowty, Matthew Frank Brown, Xin Yang, David C. Limburg, Martin Hegen, John D. Knafels, Felix Vajdos, Andrew C. Flick, Mary Ellen Banker, Raman Sharma, Li Xing, Jason Jussif, Catherine M. Ambler, Ivan Viktorovich Efremov, James D. Clark, Liying Zhang, Peter T. Symanowicz, Eddine Saiah, Jill Chrencik, Jean-Baptiste Telliez, Xiaojing Yang, Eric P. Arnold, Ariamala Gopalsamy, Zhao-Kui Wan, Matthew Merrill Hayward, David W. Lin
Publikováno v:
Journal of Medicinal Chemistry. 61:8597-8612
Cytokine signaling is an important characteristic of autoimmune diseases. Many pro-inflammatory cytokines signal through the Janus kinase (JAK)/Signal transducer and activator of transcription (STAT) pathway. JAK1 is important for the γ-common chain
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4d4f153dbb8b5bb68fb24a9742305143
https://doi.org/10.1021/acs.jmedchem.8b00917
https://doi.org/10.1021/acs.jmedchem.8b00917
Autor:
Felix Vajdos, Eric Benvenuti, Leanne M. Buzon, Brian T. O’Neill, Gabriela Barreiro, David Riddell, Kevin Atchison, Charles E. Nolan, Ashley Robshaw, Eric F. Johnson, Kevin D. Parris, Shawn D. Doran, Michael Aaron Brodney, Xinjun Hou, Luis Martinez-Alsina, Kimberly Lapham, Mei-Hui Hsu, Elizabeth Mary Beck, Christopher Ryan Butler, Kevin Ogilvie, Cathleen Gonzales, Lorraine F. Lanyon, Christopher John Helal
Publikováno v:
Journal of Medicinal Chemistry
A growing subset of β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) utilizes an anilide chemotype that engages a key residue (Gly230) in the BACE1 binding site. Although the anilide moiety affords excellent potency, it s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ded625eb28a2c9b897d6055a57557a14
https://doi.org/10.1021/acs.jmedchem.6b01451
https://doi.org/10.1021/acs.jmedchem.6b01451
Autor:
David C. Limburg, Andrew Fensome, Fabien Vincent, Betsy Pierce, Martin E. Dowty, Mary Ellen Banker, Raman Sharma, Xin Yang, Ariamala Gopalsamy, Roger S. Gifford, Brian S. Gerstenberger, Andrew C. Flick, Eric P. Arnold, Jason Jussif, Ivan Viktorovich Efremov, Xiaojing Yang, Martin Hegen, Zhao-Kui Wan, Felix Vajdos, Catherine M. Ambler, James D. Clark, Tsung H. Lin, John I. Trujillo, Li Xing
Publikováno v:
Bioorganic & Medicinal Chemistry. 28:115481
Herein, we disclose a new series of TYK2/ JAK1 inhibitors based upon a 3.1.0 azabicyclic substituted pyrimidine scaffold. We illustrate the use of structure-based drug design for the initial design and subsequent optimization of this series of compou
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dc4d8bef6390fa6ece1b44635a741fad
https://doi.org/10.1016/j.bmc.2020.115481
https://doi.org/10.1016/j.bmc.2020.115481
Autor:
Martin Hegen, David C. Wood, Patrik Rhönnstad, Felix Vajdos, Atli Thorarensen, Mark E. Schnute, Timothy Braden, Kimberly Crouse, Maria Sjöberg, John I. Trujillo, Ravi G. Kurumbail, Bolette Husman, Konrad F. Koehler, Mattias Wennerstål, Tomas Bonn, Joakim Löfstedt, Eva Backström-Rydin, Bo Carlsson, Aron Sundell, Ming Z. Chen, Steven E. Heasley, John David Trzupek, Annika Goos-Nilsson, Carol A. Menard, Peter Harris, James R. Kiefer, Martin Bengtsson, Leon P. Collis, Michael J. Prinsen, Philippe Nuhant, Jennifer Alley, Scott A. Long, Alexander E. Hromockyj, Andrew C. Flick, Johnny Sandberg, Christoph W. Zapf, Edouard Zamaratski, Xiao Hu, Lee Napierata, Björn Kauppi, Nicole Caspers, Kimberly F. Fennell, Robert E. Kyne, Gabriel Berstein, Neelu Kaila, Lars Kruger, Wei Li, Li Xing, Ray Unwalla, Elisabet Kallin, Matthew J. Pelc, Susan Fish, James Robert Blinn, Hjalmar Gullberg, Marvin J. Meyers, Scot Richard Mente, Chulho Choi, Falgun Shah, Mathias Färnegårdh, Dean Messing, Peter G. Jones, Yajuan Zhao, Alexandria P. Taylor, Maria Sandström, Charles W. Bolten, Daniel Nöteberg, Robin A. Weinberg, Tomasz Janosik, John D. Knafels, Anna Wilhelmsson
Publikováno v:
Journal of medicinal chemistry. 61(23)
The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b335f732a3ffd4d00a80bd0f813c732
https://pubmed.ncbi.nlm.nih.gov/30130103
https://pubmed.ncbi.nlm.nih.gov/30130103
Autor:
Eddie Yang, Jennifer L. Liras, Christine C. Orozco, Christopher W. am Ende, Matthew A. Movsesian, Jayvardhan Pandit, John M. Humphrey, Stephen Jenkinson, Frank S. Menniti, Thomas Allen Chappie, Spiros Liras, Stacey L. Becker, Felix Vajdos, Fabrice Vandeput
Publikováno v:
Journal of medicinal chemistry. 61(10)
We disclose the discovery and X-ray cocrystal data of potent, selective quinazoline inhibitors of PDE1. Inhibitor (S)-3 readily attains free plasma concentrations above PDE1 IC50 values and has restricted brain access. The racemic compound 3 inhibits
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aad70863e6c50adf198b09386b95c77c
https://pubmed.ncbi.nlm.nih.gov/29718668
https://pubmed.ncbi.nlm.nih.gov/29718668
Autor:
Christopher John Helal, Kevin Atchison, Christopher Ryan Butler, Cathleen Gonzales, Ricardo Lira, Shawn D. Doran, Feng Pan, Felix Vajdos, Alison H. Varghese, Gabriela Barreiro, Michael Aaron Brodney, Jinlong Wang, Elizabeth Mary Beck, Luis Martinez-Alsina, Yong Zhang, Kevin D. Parris, David Riddell, Joseph Michael Young, Leanne M. Buzon, Ashley Robshaw, Kevin Ogilvie, Jason K. Dutra, Brian T. O’Neill, John C. Murray, Charles E. Nolan
Publikováno v:
Journal of Medicinal Chemistry. 58:2678-2702
The identification of centrally efficacious β-secretase (BACE1) inhibitors for the treatment of Alzheimer's disease (AD) has historically been thwarted by an inability to maintain alignment of potency, brain availability, and desired absorption, dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::455eb0d85337e81623d88cc6b235a8b0
https://doi.org/10.1021/jm501833t
https://doi.org/10.1021/jm501833t
Autor:
Louis Leung, Jonathan Langille, John I. Trujillo, Paul B. Balbo, Jason Jussif, Jill Chrencik, Martin Hegen, Felix Vajdos, Atli Thorarensen, Sarah Soucy, Adam M. Gilbert, Jean-Baptiste Telliez, Tsung Lin, Ray Unwalla, Matthew Merrill Hayward, Justin I. Montgomery, Sidney Liang, Fabien Vincent, Robert M. Czerwinski, Ye Che, Martin E. Dowty, Mary Ellen Banker, Xin Yang, Matthew Frank Brown, Agustin Casimiro-Garcia, Jotham Wadsworth Coe, Brian Juba
Publikováno v:
Journal of medicinal chemistry. 60(5)
Significant work has been dedicated to the discovery of JAK kinase inhibitors resulting in several compounds entering clinical development and two FDA approved NMEs. However, despite significant effort during the past 2 decades, identification of hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c5195e7072387df8494062118b596b7
https://pubmed.ncbi.nlm.nih.gov/28139931
https://pubmed.ncbi.nlm.nih.gov/28139931
Autor:
Laurel Sweet, Carine Beysen, William P. Esler, David Price, Alan M. Mathiowetz, David A. Griffith, Daniel W. Kung, Scott W. Bagley, Scott M. Turner, Gabriele E. Sonnenberg, Eric Ravussin, Santos Carvajal-Gonzalez, Felix Vajdos, Chris Limberakis, James A. Southers, Paul A. Amor, Shawn D. Doran, Kirk McPherson
Publikováno v:
Journal of Medicinal Chemistry
Acetyl-CoA carboxylase (ACC) inhibitors offer significant potential for the treatment of type 2 diabetes mellitus (T2DM), hepatic steatosis, and cancer. However, the identification of tool compounds suitable to test the hypothesis in human trials has
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e1aef7fc28748a6cde4608945069cb34
http://europepmc.org/articles/PMC4281100
http://europepmc.org/articles/PMC4281100