Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Nino Campobasso"'
Autor:
Peter A. Jones, Ashley K. Wiseman, Helai P. Mohammad, Christopher S. Kershaw, Bryan W. King, Ian D. Waddell, Thau F. Ho, Stephen B. Baylin, Morris Muliaditan, Marcus Bantscheff, Elisabeth A. Minthorn, Thilo Werner, Alan P. Graves, Wendy A. Kellner, Phil Chapman, Mehul Patel, Anthony J. Jurewicz, Allan M. Jordan, Emma E. Fairweather, Rab K. Prinjha, Nino Campobasso, Anna Rutkowska, H. Christian Eberl, Ryan G. Kruger, Charles F. McHugh, Michael T. McCabe, Kristin M. Goldberg, Jon Paul Jaworski, Christopher L. Carpenter, Michael Steidel, Stuart Paul Romeril, Dirk A. Heerding, Lourdes Rueda, David T. Fosbenner, Amy N. Taylor, Jacques Briand, Shawn W. Foley, Arthur Groy, Andrew B. Benowitz, Xiaodong Cheng, Donald J. Ogilvie, Paola Grandi, Cunyu Zhang, Mei Li, Sarath Pathuri, Aidan G. Gilmartin, Christian S. Sherk, Juan I. Luengo, Mark Cockerill, Ali Raoof, Alexandra Stowell, Kathryn Keenan, Melissa B. Pappalardi, Makda Mebrahtu, Kristen Wong, Xing Zhang, Jessica L. Handler, Roger J. Butlin, John R. Horton, Susan Merrihew, Charlotte Burt, Dean E. McNulty
Publikováno v:
Nature Cancer. 2:1002-1017
DNA methylation, a key epigenetic driver of transcriptional silencing, is universally dysregulated in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine analogs decitabine or azacytidine, has demonstrated clinical ben
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e44c950954b0f6c38dfa2b274f54f21b
https://doi.org/10.1038/s43018-021-00249-x
https://doi.org/10.1038/s43018-021-00249-x
Autor:
Jared T. Spletstoser, Jason Dreabit, Andrew N. Knox, Andrew Benowitz, Nino Campobasso, Paris Ward, Guanglei Cui, Thomas Lewandowski, Lynn McCloskey, Kelly M. Aubart
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 29:2410-2414
The discovery of a novel series of peptide deformylase inhibitors incorporating a piperazic acid amino acid found in nature is described. These compounds demonstrated potent in vitro enzymatic potency and antimicrobial activity. Crystal structure ana
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d179b77d42efa2e2549141d20562468
https://doi.org/10.1016/j.bmcl.2019.05.028
https://doi.org/10.1016/j.bmcl.2019.05.028
Autor:
Stéphane Sautet, Emilie Jigorel, Nicolas Faucher, Jamel Meslamani, Lara Kathryn Leister, Pascal Grondin, Julie A. Cox, Bryan W. King, Pamela Nassau, Gemma Victoria White, Brad J. Geddes, Alain Claude-Marie Daugan, Helen H. Sun, Michael T. Ouellette, Pauline Lamoureux, Elizabeth J. Rivera, Scott B. Berger, James H. Thorpe, Philip A. Harris, J. Mosley, Susan E. Hutchinson, Frédéric Donche, John Bertin, Sandra J. Hoffman, Natalie Wellaway, Patrick M. Eidam, Paris Ward, Florent Potvain, Clark A. Sehon, Sebastien Andre Campos, Robert W. Marquis, Peter J. Gough, Mukesh K. Mahajan, Veronique Beneton, Jae U. Jeong, Michelle C. Schaeffer, John D. Lich, Allison M. Beal, Rakesh Nagilla, James Michael Woolven, Bonnie L. Hoffman, Anderson Niall Andrew, Marie-Hélène Fouchet, Deepak Bandyopadhyay, Carol A. Capriotti, Rachel D. Totoritis, Joshua N. Finger, Kishore K. Pasikanti, David D. Wisnoski, Sze-Ling Ng, Nino Campobasso, Nicolas George, Michael Reilly
Publikováno v:
Journal of Medicinal Chemistry. 62:5096-5110
RIP1 kinase regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including inflammatory and neurological diseases. Currently, RIP1 kinase inhibitors have advanced into early clinical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::49ff65b82b2e1feff6acc28b9dcac4dc
https://doi.org/10.1021/acs.jmedchem.9b00318
https://doi.org/10.1021/acs.jmedchem.9b00318
Autor:
Laurie K. Overton, J. David Taylor, D.D. McKee, Nino Campobasso, Robert T. Nolte, Robert A. Reid, Kenneth H. Pearce, George B. Barrett, Robert T. Gampe
Publikováno v:
Acta Crystallogr F Struct Biol Commun
Furin, also called proprotein convertase subtilisin/kexin 3 (PCSK3), is a calcium-dependent serine endoprotease that processes a wide variety of proproteins involved in cell function and homeostasis. Dysregulation of furin has been implicated in nume
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9931dc871f96ee114123ac981f3ab45b
https://doi.org/10.1107/s2053230x19001419
https://doi.org/10.1107/s2053230x19001419
Autor:
Paul Scott-Stevens, Qin Donghui, Allen Oliff, Andrew N. Hobbs, Yoshiaki Washio, Josh Cottom, Jennifer A. Borthwick, Julia Coggins, Robert J. Young, Biju Mangatt, Jordi Munoz-Muriedas, Paris Ward, Siegfried B. Christensen, Helen L. Evans, Jingsong Yang, Nino Campobasso, Graham L. Simpson, Julien Chabanet, Xuan Hong, Sophie M. Bertrand, Susan Chen, Helen C. Dawson
Publikováno v:
Journal of Medicinal Chemistry. 62:2154-2171
Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was hypothesized that transient activation of c-Abl kinase via displacement of the N-terminal autoinhibito
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::64687f04df163cae0b9f2c6dc35de00e
https://doi.org/10.1021/acs.jmedchem.8b01872
https://doi.org/10.1021/acs.jmedchem.8b01872
Autor:
Lisa E.J. Douglas, James A. Reihill, Melisa W.Y. Ho, Jeffrey M. Axten, Nino Campobasso, Jessica L. Schneck, Alan R. Rendina, Keith M. Wilcoxen, S. Lorraine Martin
Publikováno v:
Douglas, L E J, Reihill, J A, Ho, M W Y, Axten, J M, Campobasso, N, Schneck, J L, Rendina, A R, Wilcoxen, K M & Martin, S L 2022, ' A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airways disease ', Cell Chemical Biology, vol. 29, no. 6, pp. P947-957.E8 . https://doi.org/10.1016/j.chembiol.2022.02.001
In cystic fibrosis (CF), excessive furin activity plays a critical role in the activation of the epithelial sodium channel (ENaC), dysregulation of which contributes to airways dehydration, ineffective mucociliary clearance (MCC) and mucus obstructio
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec7020648ac8f44c37c8cfe5b454e467
https://doi.org/10.1016/j.chembiol.2022.02.001
https://doi.org/10.1016/j.chembiol.2022.02.001
Autor:
Xiaoyang Dong, Anna Vossenkämper, Attiq Rahman, Viera Kasparcova, Robert Singhaus, Joshua N. Finger, Bryan W. King, Patrick M. Eidam, Michael Reilly, David D. Wisnoski, Scott B. Berger, John D. Lich, James Kang, Michael T. Ouellette, Lauren Dare, Philip A. Harris, Julie A. Cox, Nathan A. Miller, John Bertin, Michelle C. Schaeffer, Deepak Bandyopadhyay, Daohua Zhang, Alan R. Rendina, Clark A. Sehon, Sandra J. Hoffman, Peter J. Gough, Rachel D. Totoritis, Thomas T. MacDonald, Yunfeng Lan, Paris Ward, Barbara A. Swift, Robert W. Marquis, Lara Kathryn Leister, Rakesh Nagilla, Elizabeth J. Rivera, Helen H. Sun, Carol A. Capriotti, Nino Campobasso, Ruth Lehr, Christina S. Pao, Jae U. Jeong
Publikováno v:
Journal of Medicinal Chemistry. 60:1247-1261
RIP1 regulates necroptosis and inflammation and may play an important role in contributing to a variety of human pathologies, including immune-mediated inflammatory diseases. Small-molecule inhibitors of RIP1 kinase that are suitable for advancement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cc6dda831a1761e39a5fe91326c033a4
https://doi.org/10.1021/acs.jmedchem.6b01751
https://doi.org/10.1021/acs.jmedchem.6b01751
Autor:
Mary Ann Hardwicke, Hong Lin, Karl F. Erhard, John D. Martin, Ren Xie, Kaushik Raha, Rosanna Tedesco, Jin Zeng, Yanqiu Qian, Patricia M. Kratz, Yong Jiang, Ted Cecconie, Stan F. Martens, Angela Smallwood, Patrick McDevitt, James F. Mack, Baoguang Zhao, Stephenie B. Chen, Anthony J. Jurewicz, Juan I. Luengo, Mark J. Schulz, Nino Campobasso, Catherine A. Oleykowski, Lawrence M. Szewczuk, Alan R. Rendina, Cynthia M. Rominger, Benjamin J. Schwartz, Leng Nickels, Junya Qu, Jacques Briand
Publikováno v:
ACS Medicinal Chemistry Letters. 7:217-222
A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the HK2 enzyme could adopt an "in
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aec5386353626ba6f7f23a2d64607cd6
https://doi.org/10.1021/acsmedchemlett.5b00214
https://doi.org/10.1021/acsmedchemlett.5b00214
Autor:
Martha Alicia De La Rosa, Kurt Weaver, Lisa M. Shewchuk, Rachel D. Totoritis, John Seal, David Favre, Guofeng Zhang, Makda Mebrahtu, Tia Lewis, Marcel Muelbaier, Richard M. Dunham, Giovanna Bergamini, Jeffrey Guss, Alan R. Rendina, Nino Campobasso, Wieslaw M. Kazmierski, Douglas W. Thomson, Robert Midgett, Katrin Strohmer, Anna Rutkowska-Klute, Rosalie Matico, Thomas Consler, Cunyu Zhang, David Taylor, Sabrina Bédard, Rodrigo F Ortiz-Meoz, Liping Wang
Indoleamine-2,3-dioxygenase 1 (IDO1) is a heme-containing enzyme that catalyzes the rate-limiting step in the kynurenine pathway of tryptophan (TRP) metabolism. As an inflammation-induced immunoregulatory enzyme, pharmacological inhibition of IDO1 ac
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d6eedaf9b8c5819ab8c1e04bab343a2
https://doi.org/10.1101/324947
https://doi.org/10.1101/324947
Autor:
Nino Campobasso, Donald Huddler
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:3771-3776
Hydrogen deuterium exchange mass spectrometry (HDX-MS) has become an increasingly routine technology for probing the solution structure and dynamics of proteins. HDX-MS measures the exchange of deuterium with the amide proton on the protein backbone
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c14963cf5cc01f3a694e00ef99deeb7b
https://doi.org/10.1016/j.bmcl.2015.07.007
https://doi.org/10.1016/j.bmcl.2015.07.007