Zobrazeno 1 - 10
of 37
pro vyhledávání: '"Luc J. Farmer"'
Autor:
Michael J. Boyd, Nti-Addae Kwame Wiredu, Randy S. Bethiel, John P. Duffy, Joshua R. Leeman, Rene Rijnbrand, Brian Ledford, Deng Hongbo, Christine Memmott, Tiansheng Wang, Randal Byrn, Hamilton B. Bennett, Luc J. Farmer, Jones Steven, Wenxin Gu, Paul S. Charifson, Youssef L. Bennani, Mark W. Ledeboer, Upul K. Bandarage, Marc Jacobs, Michael P. Clark, Emanuele Perola, Colleen O’Brien, Alice Tsai, Shannon Dean
In our efforts to develop novel small-molecule inhibitors for the treatment of influenza, we utilized molecular modeling and the X-ray crystal structure of the PB2 subunit of the influenza polymerase to optimize a series of acyclic β-amino acid inhi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::571e3924c774ac8afe409ad89fb6f678
https://europepmc.org/articles/PMC5304291/
https://europepmc.org/articles/PMC5304291/
Autor:
William Markland, Ernst ter Haar, Darshana Zhaveri, Guy W. Bemis, Thomas Hoock, Martin Connors, Francesco G. Salituro, Shawn D. Britt, Cochran John E, Suganthini Nanthakumar, Edmund Harrington, Jian Wang, Luc J. Farmer, Paul Taslimi
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:6231-6235
A series of SYK inhibitors based on the phenylamino pyrimidine thiazole lead 4 were prepared and evaluated for biological activity. Lead optimization provided compounds with nanomolar Ki’s against SYK and potent inhibition in mast cell degranulatio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d2a734cf4205416eba869a8c2e13177
https://doi.org/10.1016/j.bmcl.2008.09.106
https://doi.org/10.1016/j.bmcl.2008.09.106
Autor:
David Messersmith, Harmon J. Zuccola, Thomas Hoock, Sudipta Mahajan, Christopher Town, M. Woods Wannamaker, Luke Oh, Jian Wang, James J. Black, Bin Fan, Pamela McCarthy, Francesco G. Salituro, Mark N. Namchuk, Christopher L Brummel, Valerie Marone, Warren Dorsch, Randy S. Bethiel, Mark W. Ledeboer, Edmund Harrington, Summer Halas, Dina Shlyakter, Lora Swenson, Cochran John E, Youssef L. Bennani, Arthur Rugg, David Howe, Albert C. Pierce, Shannon Dean, Marina Penney, Hui Huang, Tiansheng Wang, Gabriel Martinez-Botella, James K. Hogan, Ananthsrinivas Chakilam, Shengkai Liao, Michael J. Arnost, Kumkum Saxena, Luc J. Farmer, Scott A. Raybuck, Shi-Kai Tian, Dylan Jacobs, Leena Laitinen, Raymond J. Winquist
Publikováno v:
Journal of medicinal chemistry. 58(18)
While several therapeutic options exist, the need for more effective, safe, and convenient treatment for a variety of autoimmune diseases persists. Targeting the Janus tyrosine kinases (JAKs), which play essential roles in cell signaling responses an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3a57998bf457ae6f3959a86c5e2312bb
https://pubmed.ncbi.nlm.nih.gov/26230873
https://pubmed.ncbi.nlm.nih.gov/26230873
Autor:
Dina Shlyakhter, Sudipta Mahajan, Luke Oh, Francesco G. Salituro, James K. Hogan, Thomas Hoock, Luc J. Farmer
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 353(2)
Cytokines, growth factors, and other chemical messengers rely on a class of intracellular nonreceptor tyrosine kinases known as Janus kinases (JAKs) to rapidly transduce intracellular signals. A number of these cytokines are critical for lymphocyte d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::917e0be8e90db7a494f6f86288a01743
https://pubmed.ncbi.nlm.nih.gov/25762693
https://pubmed.ncbi.nlm.nih.gov/25762693
Autor:
Cynthia A. Gates, John A. Thomson, Kevin M. Cottrell, Yu P. Luong, Scott L. Harbeson, Robert B. Perni, John H. Van Drie, David D. Deininger, Roger D. Tung, Shawn D. Britt, Chao Lin, Janos Pitlik, Luc J. Farmer, John J. Court, Yunyi Wei, John Maxwell, Kai Lin, Bhisetti Govinda Rao, Lawrence F. Courtney, Wayne C. Schairer
Publikováno v:
Letters in Drug Design & Discovery. 2:497-502
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7d420d4ea1640c769a11c7300ffa8634
https://doi.org/10.2174/157018005774479203
https://doi.org/10.2174/157018005774479203
Autor:
Kai Lin, Joseph L. Kim, Yu-Ping Luong, Janos Pitlik, Wayne C. Schairer, Chao Lin, Roger D. Tung, Robert B. Perni, John A. Thomson, John Maxwell, Luc J. Farmer, Kevin M. Cottrell, Murcko Mark A, Lawrence F. Courtney, Cynthia A. Gates, John J. Court, John H. Van Drie, David D. Deininger, Wilson Keith P, B. Govinda Rao, Scott L. Harbeson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1939-1942
We recently described the identification of an optimized α-ketoamide warhead for our series of HCV NS3·4A inhibitors. We report herein a series of HCV protease inhibitors incorporating 3-alkyl-substituted prolines in P2. These compounds show except
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aee870e2ad12957f02ea4352f74bcbb2
https://doi.org/10.1016/j.bmcl.2004.01.078
https://doi.org/10.1016/j.bmcl.2004.01.078
Autor:
Ethan O'malley, Yunyi Wei, Yu-Ping Luong, John H. Van Drie, Lawrence F. Courtney, Scott L. Harbeson, Janos Pitlik, Kai Lin, Roger D. Tung, Young-Choon Moon, Shawn D. Britt, Chao Lin, Luc J. Farmer, B. Govinda Rao, John J. Court, Cynthia A. Gates, John A. Thomson, David D. Deininger, Robert B. Perni, Rhonda B. Levin
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:1441-1446
The α-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3·4A protease inhibitors. Structure–activity relationships and prime side optimization are discussed.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56535e42d42b9915dbd7e2607e21e42a
https://doi.org/10.1016/j.bmcl.2004.01.022
https://doi.org/10.1016/j.bmcl.2004.01.022
Autor:
Rhonda B. Levin, Luc J. Farmer, Robert B. Perni, Joseph L. Kim, Janos Pitlik, B. Govinda Rao, J. A. Landro, Wayne C. Schairer, Roger D. Tung, Shawn D. Britt, Cynthia A. Gates, David D. Deininger, John A. Thomson, John H. Van Drie, Lawrence F. Courtney, John Court, Ethan O'malley, Scott L. Harbeson, Yu-Ping Luong, Yunyi Wei
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:4059-4063
Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91046b82077f4245c43e468a535b331b
https://doi.org/10.1016/j.bmcl.2003.08.050
https://doi.org/10.1016/j.bmcl.2003.08.050
Autor:
Marc Jacobs, Christopher Bral, Youssef L. Bennani, Jianglin Liang, John P. Duffy, Tiansheng Wang, Brian Ledford, Michael J. Boyd, Wenxin Gu, Randal Byrn, Min Jiang, Christine Memmott, Azin Nezami, Ioana Davies, Joshua R. Leeman, Yuegang Zhang, Hamilton B. Bennett, Warren Dorsch, Katrina L. Jackson, Upul K. Bandarage, William P. Taylor, Mark W. Ledeboer, Dylan Jacobs, Francesco G. Salituro, Kennedy Joseph M, Huai Gao, Nti-Addae Kwame Wiredu, Michael P. Clark, Francois Maltais, Emanuele Perola, Murcko Mark A, Deng Hongbo, M. Woods Wannamaker, Ursula A. Germann, Alice Tsai, Rene Rijnbrand, Luc J. Farmer, Colleen F. McNeil, Randy S. Bethiel, Paul S. Charifson, John J. Court, Jones Steven
Publikováno v:
Journal of medicinal chemistry. 57(15)
In our effort to develop agents for the treatment of influenza, a phenotypic screening approach utilizing a cell protection assay identified a series of azaindole based inhibitors of the cap-snatching function of the PB2 subunit of the influenza A vi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e831d7438e6619f14b048a90fd8101c5
https://pubmed.ncbi.nlm.nih.gov/25019388
https://pubmed.ncbi.nlm.nih.gov/25019388
Autor:
James P. Edwards, James W. Kong, Kristen L. Arienti, Keith B. Marschke, Thomas R. Caferro, Robert I. Higuchi, Luc J. Farmer, Robert L. Davis, Todd K. Jones, Josef D. Ringgenberg, Lawrence G. Hamann
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 9:1335-1340
A series of human androgen receptor (hAR) agonists based on 4-alkyl-; 4,4-dialkyl-; and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinoline was synthesized and evaluated in competitive receptor binding assays and an androgen receptor cotransfec
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6263b53da9f5d576664b6452d5408f4
https://doi.org/10.1016/s0960-894x(99)00186-9
https://doi.org/10.1016/s0960-894x(99)00186-9