Zobrazeno 1 - 10
of 80
pro vyhledávání: '"Xavier, Fradera"'
Autor:
Nairie Michaelian, Anastasiia Sadybekov, Élie Besserer-Offroy, Gye Won Han, Harini Krishnamurthy, Beata A. Zamlynny, Xavier Fradera, Phieng Siliphaivanh, Jeremy Presland, Kerrie B. Spencer, Stephen M. Soisson, Petr Popov, Philippe Sarret, Vsevolod Katritch, Vadim Cherezov
Publikováno v:
Nature Communications, Vol 12, Iss 1, Pp 1-12 (2021)
Human leukotriene B4 receptors (BLT1 and BLT2) are members of the GPCR superfamily that respond to a potent pro-inflammatory lipid and chemoattractant LTB4. Here authors determined a crystal structure of the human BLT1 in complex with a selective ant
Externí odkaz:
https://doaj.org/article/718b186632fa46f2ad43c9c7ad152fa9
Autor:
Prasanthi Geda, Mark A. McCoy, Liping Yang, Chaomin Li, Armetta D. Hill, Xavier Fradera, Marianne L. Spatz, Matthew Ernst Voss, Carolyn Michele Cammarano, Pierre Daublain, Xiao Wang, Christopher F. Thompson, B. Wesley Trotter, C. Gary Marshall, Michael H. Reutershan, Peter Goldenblatt, Latha G. Nair, Manami Shizuka, Tammie C. Yeh, John G. Cryan, Isabelle Dussault, Michelle Martinez, Mingmei Cai, Raymond A. Kemper, Binyuan Sun, Michelle R. Machacek, Dietrich Steinhuebel, Giovanna Scapin, Michael D. Altman, Stephane L. Bogen, Matthew Christopher, Dapeng Chen, Victoria Kutilek, Weidong Pan
Publikováno v:
Journal of Medicinal Chemistry. 64:16213-16241
Identification of low-dose, low-molecular-weight, drug-like inhibitors of protein-protein interactions (PPIs) is a challenging area of research. Despite the challenges, the therapeutic potential of PPI inhibition has driven significant efforts toward
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::a9f003ba884dc7f950fc132b2a33cadf
https://doi.org/10.1021/acs.jmedchem.1c01524
https://doi.org/10.1021/acs.jmedchem.1c01524
Autor:
Joey L. Methot, David A Candito, Sheila Ranganath, Zangwei Xu, Xavier Fradera, Abdelghani Achab, Erin F. DiMauro, Haiyan Xu, Samuel M. Levi, Brandon A. Vara, Brian M. Lacey, Mark Bittinger, Jennifer Piesvaux, Dustin M Smith, Alexander Pasternak, Jongwon Lim, David Jonathan Bennett, J. Richard Miller, Charles A. Lesburg, Shuhei Kawamura
Publikováno v:
ACS Med Chem Lett
[Image: see text] Hematopoietic progenitor kinase 1 (HPK1), a serine/threonine kinase, is a negative immune regulator of T cell receptor (TCR) and B cell signaling that is primarily expressed in hematopoietic cells. Accordingly, it has been reported
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3974d15fa6854f44fa7ca9ad4baa4e1b
https://doi.org/10.1021/acsmedchemlett.1c00096
https://doi.org/10.1021/acsmedchemlett.1c00096
Autor:
Chunhui Huang, Christian Fischer, Michelle R. Machacek, Stephane Bogen, Tesfaye Biftu, Xianhai Huang, Michael H. Reutershan, Ryan Otte, Qingmei Hong, Zhicai Wu, Yang Yu, Min Park, Lei Chen, Purakkattle Biju, Ian Knemeyer, Ping Lu, Christopher J. Kochansky, Michael Brendan Hicks, Yong Liu, Roy Helmy, Xavier Fradera, Anthony Donofrio, Josh Close, Matthew L. Maddess, Catherine White, David L. Sloman, Nunzio Sciammetta, Jun Lu, Craig Gibeau, Vladimir Simov, Hongjun Zhang, Peter Fuller, David Witter
Publikováno v:
ACS Med Chem Lett
[Image: see text] Mutant isocitrate dehydrogenase 1 (IDH1) has been identified as an attractive oncology target for which >70% of grade II and III gliomas and ∼10% of acute myeloid leukemia (AML) harbor somatic IDH1 mutations. These mutations confe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::13ecfd534a4182e5c705a82b16c3ffcc
https://europepmc.org/articles/PMC9014435/
https://europepmc.org/articles/PMC9014435/
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:
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:
Xavier Fradera, Michael H. Reutershan, Michelle R. Machacek, B. Wesley Trotter, Mark A. McCoy
Publikováno v:
Chembiochem : a European journal of chemical biology. 23(6)
We present an automated NMR-guided docking workflow that can be used to generate models of protein-ligand complexes based on data from NOE NMR experiments. The first step is to generate a number of intermolecular distance constraints from experimenta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0be041247caf23dd8a9121996305af82
https://pubmed.ncbi.nlm.nih.gov/35104390
https://pubmed.ncbi.nlm.nih.gov/35104390
Autor:
Michael H, Reutershan, Michelle R, Machacek, Michael D, Altman, Stephane, Bogen, Mingmei, Cai, Carolyn, Cammarano, Dapeng, Chen, Matthew, Christopher, John, Cryan, Pierre, Daublain, Xavier, Fradera, Prasanthi, Geda, Peter, Goldenblatt, Armetta D, Hill, Raymond A, Kemper, Victoria, Kutilek, Chaomin, Li, Michelle, Martinez, Mark, McCoy, Latha, Nair, Weidong, Pan, Christopher F, Thompson, Giovanna, Scapin, Manami, Shizuka, Marianne L, Spatz, Dietrich, Steinhuebel, Binyuan, Sun, Matthew E, Voss, Xiao, Wang, Liping, Yang, Tammie C, Yeh, Isabelle, Dussault, C Gary, Marshall, B Wesley, Trotter
Publikováno v:
Journal of medicinal chemistry. 64(21)
Identification of low-dose, low-molecular-weight, drug-like inhibitors of protein-protein interactions (PPIs) is a challenging area of research. Despite the challenges, the therapeutic potential of PPI inhibition has driven significant efforts toward
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::7c70be0458a74b9595c42b9269bd0b63
https://pubmed.ncbi.nlm.nih.gov/34714078
https://pubmed.ncbi.nlm.nih.gov/34714078
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
Autor:
Sam Kattar, Jason D. Katz, Peter Goldenblatt, Kenneth E. Wilson, Augustin, Matthew Christopher, Abdelghani Achab, Charles A. Lesburg, H. Zhou, Shrenik K. Shah, Xavier Fradera, Yudith Garcia, Joey L. Methot, Altman, McGowan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2575-2580
PI3Kδ mediates key immune cell signaling pathways and is a target of interest for multiple indications in immunology and oncology. Here we report a structure-based scaffold-hopping strategy for the design of chemically diverse PI3Kδ inhibitors. Usi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6b939d5f9d279a3d02ee126d137ba8e4
https://doi.org/10.1016/j.bmcl.2019.08.004
https://doi.org/10.1016/j.bmcl.2019.08.004