Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Klaus Michelsen"'
Autor:
Eris Bame, Hao Tang, Jeremy C Burns, Million Arefayene, Klaus Michelsen, Bin Ma, Isaac Marx, Robin Prince, Allie M Roach, Urjana Poreci, Douglas Donaldson, Patrick Cullen, Fergal Casey, Jing Zhu, Thomas M Carlile, Dipen Sangurdekar, Baohong Zhang, Patrick Trapa, Joseph Santoro, Param Muragan, Alex Pellerin, Stephen Rubino, Davide Gianni, Bekim Bajrami, Xiaomei Peng, Alex Coppell, Katherine Riester, Shibeshih Belachew, Devangi Mehta, Mike Palte, Brian T Hopkins, Matthew Scaramozza, Nathalie Franchimont, Michael Mingueneau
Publikováno v:
Clinical & Translational Immunology, Vol 10, Iss 6, Pp n/a-n/a (2021)
Abstract Objectives Bruton's tyrosine kinase (BTK) plays a non‐redundant signaling role downstream of the B‐cell receptor (BCR) in B cells and the receptors for the Fc region of immunoglobulins (FcR) in myeloid cells. Here, we characterise BIIB09
Externí odkaz:
https://doaj.org/article/960649d0c0f948e3add268a6d5cc0401
Autor:
Jeffrey R. Simard, Klaus Michelsen, Yan Wang, Chunhua Yang, Beth Youngblood, Barbara Grubinska, Kristin Taborn, Daniel J. Gillie, Kevin Cook, Kyu Chung, Alexander M. Long, Brian E. Hall, Paul L. Shaffer, Robert S. Foti, Jacinthe Gingras
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 383:56-69
Ion channels are targets of considerable therapeutic interest to address a wide variety of neurologic indications, including pain perception. Current pharmacological strategies have focused mostly on small molecule approaches that can be limited by s
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f4587f1dc532b800a2152c9df3276069
https://doi.org/10.1124/jpet.121.001026
https://doi.org/10.1124/jpet.121.001026
Autor:
Ermira Pazolli, Randy Kipp, Alessandro Boezio, Hakan Gunaydin, Amanda Iskandar, Matthew Zubrowski, Bret Williams, Kelley Shortsleeves, Alexandre Larivee, Tom McLean, Klaus Michelsen, Hongtao Zeng, Jonathan LaRochelle, Joe Manna, Lucian DiPietro, Andre Lescarbeau, Mary Mader, Bindu Bennet, Jeremy Wilbur, Qi Wang, Levi Pierce, Iain Martin, James Watters, Pascal Fortin, Donald Bergstrom
Publikováno v:
Cancer Research. 82:P5-16
Inhibition of CDK4/6 combined with the estrogen receptor (ER) degrader fulvestrant significantly improves progression free survival and overall survival in advanced hormone receptor positive (HR+) breast cancer patients and is now the standard of car
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::68ddad78553bc15ede0b650a5dff37d3
https://doi.org/10.1158/1538-7445.sabcs21-p5-16-10
https://doi.org/10.1158/1538-7445.sabcs21-p5-16-10
Autor:
Bin Ma, Doug Marcotte, Murugan Paramasivam, Klaus Michelsen, Ti Wang, Andrea Bertolotti-Ciarlet, John Howard Jones, Ben Moree, Margaret Butko, Joshua Salafsky, Xin Sun, Timothy McKee, Laura F Silvian
Publikováno v:
PLoS ONE, Vol 11, Iss 11, p e0165983 (2016)
MLKL is a pore forming pseudokinase involved in the final stage of necroptosis, a form of programmed cell death. Its phosphorylation by RIPK3 is necessary for triggering necroptosis but not for triggering apoptosis, which makes it a unique target for
Externí odkaz:
https://doaj.org/article/67003a59dd434add954b7cdabddde7a6
Autor:
E Allen Sickmier, Robert J M Kurzeja, Klaus Michelsen, Mukta Vazir, Evelyn Yang, Andrew S Tasker
Publikováno v:
PLoS ONE, Vol 11, Iss 9, p e0163366 (2016)
Panitumumab and cetuximab target the epidermal growth factor receptor for the treatment of metastatic colorectal cancer. These therapies provide a significant survival benefit to patients with metastatic colorectal cancer with wild-type RAS. A single
Externí odkaz:
https://doaj.org/article/9714291c953e4ed38fccb50a2c3b5208
Autor:
Jing Zhu, Xiaomei Peng, Alex Pellerin, Brian T. Hopkins, Dipen Sangurdekar, Michael Mingueneau, Urjana Poreci, Eris Bame, Joseph C Santoro, Prince Robin, Katherine Riester, Mike Palte, Allie M Roach, Klaus Michelsen, Bin Ma, Hao Tang, Million Arefayene, Stephen J Rubino, Devangi Mehta, Fergal Casey, Patrick Cullen, Patrick Trapa, Bekim Bajrami, Thomas M. Carlile, Davide Gianni, Marx Isaac, Douglas Donaldson, Baohong Zhang, Jeremy C. Burns, Param Muragan, Alex Coppell, Shibeshih Belachew, Nathalie Franchimont, Matthew Scaramozza
Publikováno v:
Clinical & Translational Immunology
Clinical & Translational Immunology, Vol 10, Iss 6, Pp n/a-n/a (2021)
Clinical & Translational Immunology, Vol 10, Iss 6, Pp n/a-n/a (2021)
Objectives Bruton's tyrosine kinase (BTK) plays a non‐redundant signaling role downstream of the B‐cell receptor (BCR) in B cells and the receptors for the Fc region of immunoglobulins (FcR) in myeloid cells. Here, we characterise BIIB091, a nove
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::188cf6754afaaa237193991f00885497
https://doi.org/10.1002/cti2.1295
https://doi.org/10.1002/cti2.1295
Autor:
Ermira Pazolli, Randy Kipp, Alessandro Boezio, Hakan Gunaydin, Amanda Iskandar, Matthew Zubrowski, Bret Williams, Kelley Shortsleeves, Alexandre Larivee, Tom McLean, Klaus Michelsen, Hongtao Zeng, Jonathan LaRochelle, Joe Manna, Lucian DiPietro, Mary Mader, Bindu Bennet, Jeremy Wilbur, Qi Wang, Levi Pierce, Iain Martin, James Watters, Pascal Fortin, Donald Bergstrom
Publikováno v:
Molecular Cancer Therapeutics. 20:P251-P251
Phosphoinositide 3-kinase alpha (PI3Kα) is the most frequently mutated kinase in solid tumors. Traditionally, the development of PI3Kα inhibitors has focused on the active, or orthosteric site. The therapeutic index of orthosteric inhibitors is lim
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::567d8dac909432d6fd3f2fd9a69edd1f
https://doi.org/10.1158/1535-7163.targ-21-p251
https://doi.org/10.1158/1535-7163.targ-21-p251
Autor:
Shuyan Yi, Sonya G. Lehto, Stefan I. McDonough, Klaus Michelsen, Erin F. DiMauro, Hao Chen, Maosheng Zhang, Stephen Schneider, Shawn Ayube, Jason A. Luther, Matthew H. Plant, Xin Huang, David J. Matson, Jeffrey R. Simard, Howard Bregman, Jacinthe Gingras, Paul L. Shaffer, Yohannes Teffera
Publikováno v:
Nature Structural & Molecular Biology. 24:108-113
Current therapies to treat persistent pain and neuropathic pain are limited by poor efficacy, side effects and risk of addiction. Here, we present a novel class of potent selective, central nervous system (CNS)-penetrant potentiators of glycine recep
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e4d3f9eaf357c8330409b932db69a7e
https://doi.org/10.1038/nsmb.3329
https://doi.org/10.1038/nsmb.3329
Autor:
Michael D. Bartberger, Michael Croghan, Carolyn Moyer, David Lloyd, Rod Cupples, Seifu Tadesse, Nobuko Nishimura, Ke Kong, Gwyneth Van, Christopher H. Fotsch, Randall W. Hungate, David J. St. Jean, Kevin Yang, Kate Ashton, Mark H. Norman, Samer Chmait, Longbin Liu, Lewis D. Pennington, Fang-Tsao Hong, Matthew P. Bourbeau, Clarence Hale, Jiandong Zhang, Aaron C. Siegmund, Jie Chen, Christopher M. Tegley, Steven R. Jordan, Kristin L. Andrews, Klaus Michelsen, Guomin Yao, Glenn Sivits, Andreas Reichelt, Joan Helmering
Publikováno v:
Journal of Medicinal Chemistry. 58:9663-9679
The HTS-based discovery and structure-guided optimization of a novel series of GKRP-selective GK-GKRP disrupters are revealed. Diarylmethanesulfonamide hit 6 (hGK-hGKRP IC50 = 1.2 μM) was optimized to lead compound 32 (AMG-0696; hGK-hGKRP IC50 = 0.0
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2c946578bf834df571e0f47d51f90f41
https://doi.org/10.1021/acs.jmedchem.5b01367
https://doi.org/10.1021/acs.jmedchem.5b01367
Autor:
Kate S, Ashton, Kristin L, Andrews, Marian C, Bryan, Marion C, Bryan, Jie, Chen, Kui, Chen, Michelle, Chen, Samer, Chmait, Michael, Croghan, Rod, Cupples, Christopher, Fotsch, Joan, Helmering, Steve R, Jordan, Robert J M, Kurzeja, Klaus, Michelsen, Lewis D, Pennington, Steve F, Poon, Glenn, Sivits, Gwyneth, Van, Steve L, Vonderfecht, Robert C, Wahl, Jiandong, Zhang, David J, Lloyd, Clarence, Hale, David J, St Jean
Publikováno v:
Journal of Medicinal Chemistry. 57:309-324
Small molecule activators of glucokinase have shown robust efficacy in both preclinical models and humans. However, overactivation of glucokinase (GK) can cause excessive glucose turnover, leading to hypoglycemia. To circumvent this adverse side effe
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::688eef24bebd019f68813ef22be87641
https://doi.org/10.1021/jm4016735
https://doi.org/10.1021/jm4016735