Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Karin M, Otte"'
Autor:
David A. Candito, Vladimir Simov, Anmol Gulati, Solomon Kattar, Ryan W. Chau, Blair T. Lapointe, Joey L. Methot, Duane E. DeMong, Thomas H. Graham, Ravi Kurukulasuriya, Mitchell H. Keylor, Ling Tong, Gregori J. Morriello, John J. Acton, Barbara Pio, Weiguo Liu, Jack D. Scott, Michael J. Ardolino, Theodore A. Martinot, Matthew L. Maddess, Xin Yan, Hakan Gunaydin, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Hongshi Yu, Ellen C. Minnihan, Charles A. Lesburg, Ping Liu, Jing Su, Laxminarayan G. Hegde, Lily Y. Moy, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul Ciaccio, Jennifer A. Piesvaux, Karin M. Otte, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Santhosh Neelamkavil, Harold B. Wood, Peter H. Fuller, J. Michael Ellis
Publikováno v:
Journal of Medicinal Chemistry. 65:16801-16817
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::365ba0e1a6a6d085b4344b637344b726
https://doi.org/10.1021/acs.jmedchem.2c01605
https://doi.org/10.1021/acs.jmedchem.2c01605
Autor:
David A, Candito, Vladimir, Simov, Anmol, Gulati, Solomon, Kattar, Ryan W, Chau, Blair T, Lapointe, Joey L, Methot, Duane E, DeMong, Thomas H, Graham, Ravi, Kurukulasuriya, Mitchell H, Keylor, Ling, Tong, Gregori J, Morriello, John J, Acton, Barbara, Pio, Weiguo, Liu, Jack D, Scott, Michael J, Ardolino, Theodore A, Martinot, Matthew L, Maddess, Xin, Yan, Hakan, Gunaydin, Rachel L, Palte, Spencer E, McMinn, Lisa, Nogle, Hongshi, Yu, Ellen C, Minnihan, Charles A, Lesburg, Ping, Liu, Jing, Su, Laxminarayan G, Hegde, Lily Y, Moy, Janice D, Woodhouse, Robert, Faltus, Tina, Xiong, Paul, Ciaccio, Jennifer A, Piesvaux, Karin M, Otte, Matthew E, Kennedy, David Jonathan, Bennett, Erin F, DiMauro, Matthew J, Fell, Santhosh, Neelamkavil, Harold B, Wood, Peter H, Fuller, J Michael, Ellis
Publikováno v:
Journal of medicinal chemistry. 65(24)
Inhibition of leucine-rich repeat kinase 2 (LRRK2) kinase activity represents a genetically supported, chemically tractable, and potentially disease-modifying mechanism to treat Parkinson's disease. Herein, we describe the optimization of a novel ser
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::d1e71dbb505d333749f04ff7e2a07818
https://pubmed.ncbi.nlm.nih.gov/36475697
https://pubmed.ncbi.nlm.nih.gov/36475697
Autor:
Frederique M. Poulet, J. Michael Ellis, Matthew E. Kennedy, Carrie G. Markgraf, Lauren M Timmins, Dianne K. Bryce, Sabu Kuruvilla, Janice D Woodhouse, Matthew J. Fell, Karin M. Otte, Christopher Ware, Laxminarayan G Hegde, Matthew L. Maddess, Paul J Ciaccio
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 377:11-19
Gain-of-function mutations in leucine-rich kinase 2 (LRRK2) are associated with increased incidence of Parkinson disease (PD); thus, pharmacological inhibition of LRRK2 kinase activity is postulated as a disease-modifying treatment of PD. Histomorpho
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50f51a63a6fe69d40bfa5ed39544e2dd
https://doi.org/10.1124/jpet.120.000217
https://doi.org/10.1124/jpet.120.000217
Autor:
Nicolas Solban, Alexander Pasternak, Qinglin Pu, Amy C. Doty, David Jonathan Bennett, Charles A. Lesburg, Wensheng Yu, Prasanthi Geda, Nunzio Sciammetta, J. Richard Miller, Hua Zhou, Xuelei Song, Yongxin Han, Lars Neumann, David L. Sloman, Mangeng Cheng, Heidi Ferguson, Karin M. Otte, Liangqin Guo, Hongjun Zhang, Alfred Lammens, Xavier Fradera, Meredeth A. McGowan
Publikováno v:
ACS Med Chem Lett
[Image: see text] Indoleamine-2,3-dioxygenase 1 (IDO1) inhibition and its combination with immune checkpoint inhibitors like pembrolizumab have drawn considerable attention from both academia and the pharmaceutical industry. Here, we describe the dis
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7bc457a333eeebf89280777405619540
https://doi.org/10.1021/acsmedchemlett.0c00195
https://doi.org/10.1021/acsmedchemlett.0c00195
Autor:
Derun Li, David L. Sloman, Abdelghani Achab, Hua Zhou, Meredeth A. McGowan, Catherine White, Craig Gibeau, Hongjun Zhang, Qinglin Pu, Indu Bharathan, Brett Hopkins, Kun Liu, Heidi Ferguson, Xavier Fradera, Charles A. Lesburg, Theodore A. Martinot, Ji Qi, Zhiguo J. Song, Jingjun Yin, Huangguang Zhang, Licheng Song, Baoqiang Wan, Suzanne DAddio, Nicolas Solban, J. Richard Miller, Beata Zamlynny, Alan Bass, Elizabeth Freeland, Bridget Ykoruk, Catherine Hilliard, Jude Ferraro, Jin Zhai, Ian Knemeyer, Karin M. Otte, Stella Vincent, Nunzio Sciammetta, Alexander Pasternak, David Jonathan Bennett, Yongxin Han
Publikováno v:
Journal of medicinal chemistry. 65(8)
3,3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and cyclobutane functionalities. We report the discovery of a novel class of oxetane indole-amine 2,3-dioxygenase (IDO1) inhibitors suitable for Q3W (once every 3 weeks) o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f65de888aa90fb7088ca022d5b5ddf12
https://pubmed.ncbi.nlm.nih.gov/35239336
https://pubmed.ncbi.nlm.nih.gov/35239336
Autor:
Mitchell H. Keylor, Anmol Gulati, Solomon D. Kattar, Rebecca E. Johnson, Ryan W. Chau, Kaila A. Margrey, Michael J. Ardolino, Cayetana Zarate, Kelsey E. Poremba, Vladimir Simov, Gregori J. Morriello, John J. Acton, Barbara Pio, Xin Yan, Rachel L. Palte, Spencer E. McMinn, Lisa Nogle, Charles A. Lesburg, Donovon Adpressa, Shishi Lin, Santhosh Neelamkavil, Ping Liu, Jing Su, Laxminarayan G. Hegde, Janice D. Woodhouse, Robert Faltus, Tina Xiong, Paul J. Ciaccio, Jennifer Piesvaux, Karin M. Otte, Harold B. Wood, Matthew E. Kennedy, David Jonathan Bennett, Erin F. DiMauro, Matthew J. Fell, Peter H. Fuller
Publikováno v:
Journal of medicinal chemistry. 65(1)
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder whose current therapies are limited in scope and efficacy. In this repor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6720c280fccf3e18653a864a196348ad
https://pubmed.ncbi.nlm.nih.gov/34967623
https://pubmed.ncbi.nlm.nih.gov/34967623
Autor:
Theodore A. Martinot, Xavier Fradera, Meredeth A. McGowan, Wensheng Yu, Heidi Ferguson, Purakattle J Biju, H. Zhou, Nicolas Solban, Qinglin Pu, Yongxin Han, Xiao Wang, Kun Liu, Ravi Kurukulasuriya, Yu-hong Lam, Abdelghani Achab, Karin M. Otte, Michael J. Ardolino, Amy C. Doty, Charles A. Lesburg, J. Richard Miller, Yongqi Deng, Mangeng Cheng, Hongjun Zhang, Ian Knemeyer, Nunzio Sciammetta, David Jonathan Bennett
Publikováno v:
ACS Med Chem Lett
[Image: see text] Checkpoint inhibitors have demonstrated unprecedented efficacy and are evolving to become standard of care for certain types of cancers. However, low overall response rates often hamper the broad utility and potential of these break
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c30fa3b8f261ace5c7d56e064b7047fa
https://doi.org/10.1021/acsmedchemlett.9b00344
https://doi.org/10.1021/acsmedchemlett.9b00344
Optimization of brain-penetrant picolinamide derived leucine-rich repeat kinase 2 (LRRK2) inhibitors
Autor:
Blair T. Lapointe, Jack D. Scott, Xin Cindy Yan, Haiqun Tang, Janice D Woodhouse, Kaleen Konrad Childers, Robert Faltus, Erin F. DiMauro, Solomon Kattar, Charles S. Yeung, Ravi Kurukulasuriya, Vladimir Simov, Hakan Gunaydin, Anmol Gulati, Joey L. Methot, Rachel L. Palte, Ellen C. Minnihan, Greg Morriello, J. Michael Ellis, Harold B. Wood, Santhosh Neelamkavil, Karin M. Otte, Michael J. Ardolino, Barbara Pio, Ping Liu, Laxminarayan G Hegde, Matthew J. Fell, Vanessa L. Rada, Peter Fuller, Paul J Ciaccio
Publikováno v:
RSC Med Chem
The discovery of potent, kinome selective, brain penetrant LRRK2 inhibitors is the focus of extensive research seeking new, disease-modifying treatments for Parkinson's disease (PD). Herein, we describe the discovery and evolution of a picolinamide-d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c8d45ea7dd7adda70471298a4476afa
https://europepmc.org/articles/PMC8292993/
https://europepmc.org/articles/PMC8292993/
Autor:
Karin M. Otte, Nunzio Sciammetta, Heidi Ferguson, Xavier Fradera, Theo Martinot, Amy C. Doty, Charles A. Lesburg, Yongqi Deng, Derun Li, Yongxin Han, Stella H. Vincent, Kun Liu, J. Richard Miller, Wensheng Yu, David L. Sloman, Ian Knemeyer, David Jonathan Bennett
Publikováno v:
Bioorganicmedicinal chemistry letters. 49
A series of IDO1 inhibitors containing a decahydroquinoline, decahydro-1,6-naphthyridine, or octahydro-1H-pyrrolo[3,2-c]pyridine scaffold were identified with good cellular and human whole blood activity against IDO1. These inhibitors contain multipl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa3cf00999a6352aade5315c15461ced
https://pubmed.ncbi.nlm.nih.gov/34391891
https://pubmed.ncbi.nlm.nih.gov/34391891
Autor:
Derun Li, Hongjun Zhang, Hua Zhou, Xuelei Song, Theodore A. Martinot, Prasanthi Geda, Brett A. Hopkins, Jeanine E. Ballard, Stella H. Vincent, Yongxin Han, Nicolas Solban, Karin M. Otte, Mangeng Cheng, J. Richard Miller, Qinglin Pu, Indu Bharathan, Charles A. Lesburg, Ryan D. Cohen, Ian Knemeyer, David Jonathan Bennett, Xavier Fradera, Alfred Lammens, Nadya Smotrov
Publikováno v:
ACS Med Chem Lett
[Image: see text] Herein the discovery of potent IDO1 inhibitors with low predicted human dose is discussed. Metabolite identification (MetID) and structural data were used to strategically incorporate cyclopropane rings into this tetrahydronaphthyri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83daf5d6fb5e002887daecc8d7be71ff
https://pubmed.ncbi.nlm.nih.gov/34531952
https://pubmed.ncbi.nlm.nih.gov/34531952