Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Stephan C. Schürer"'
Publikováno v:
Cell Reports Medicine
Cell Reports Medicine, Vol 1, Iss 7, Pp 100128-(2020)
Cell Reports Medicine, Vol 1, Iss 7, Pp 100128-(2020)
Summary The approval of the first kinase inhibitor, Gleevec, ushered in a paradigm shift for oncological treatment—the use of genomic data for targeted, efficacious therapies. Since then, over 48 additional small-molecule kinase inhibitors have bee
Autor:
Scott A. Oakes, Markus A. Seeliger, Bradley J. Backes, Likun Wang, B. Gayani K. Perera, Stephan C. Schürer, Barun Bhhatarai, Feroz R. Papa, Dustin J. Maly, Sanjay B. Hari
Publikováno v:
Nature chemical biology
Under endoplasmic reticulum stress, unfolded protein accumulation leads to activation of the endoplasmic reticulum transmembrane kinase/endoRNase (RNase) IRE1α. IRE1α oligomerizes, autophosphorylates and initiates splicing of XBP1 mRNA, thus trigge
Autor:
Stephan C. Schürer, Saurabh Mehta, Nagi G. Ayad, Stewart W. J. Ember, Bryce K. Allen, Ernst Schönbrunn
Publikováno v:
Scientific Reports
Inhibition of cancer-promoting kinases is an established therapeutic strategy for the treatment of many cancers, although resistance to kinase inhibitors is common. One way to overcome resistance is to target orthogonal cancer-promoting pathways. Bro
Autor:
Claudia Ruiz, Michael D. Cameron, Stephan C. Schürer, Evelyn Griffin, Yangbo Feng, Philip LoGrasso, Toshihiro Inoue, Thomas Schröter, P. Vasanth Rao, Amiee Weiser, Li Lin, Yan Yin
Publikováno v:
Journal of Medicinal Chemistry. 51:6642-6645
The identification of a new class of potent and selective ROCK-II inhibitors is presented. Compound 5 (SR-3677) had an IC 50 of approximately 3 nM in enzyme and cell based assays and had an off-target hit rate of 1.4% against 353 kinases, and inhibit
Autor:
Clara Penas, Stephan C. Schürer, Nagi G. Ayad, William R. Roush, Jitendra Kumar Mishra, Spencer D. Wood
Ubiquitin mediated proteolysis is required for transition from one cell cycle phase to another. For instance, the mitosis inhibitor Wee1 is targeted for degradation during S phase and G2 to allow mitotic entry. Wee1 is an essential tyrosine kinase re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::659e5c792b9f063a0c56b271a1d613fd
Autor:
Maike Thamsen, Deborah Caswell, Likun Wang, Dustin J. Maly, Kurt F. Weiberth, Hector Macias, Sanjay B. Hari, Scott A. Oakes, Aeid Igbaria, Barun Bhhatarai, Shuhei Morita, Eric S. Wang, Michael S. German, Micah J. Gliedt, Bradley J. Backes, Kris Prado, Erik L. Snapp, Arinjay K. Mitra, Douglas B. Gould, Rajarshi Ghosh, Feroz R. Papa, B. Gayani K. Perera, Stephan C. Schürer, Marcel V. Alavi
Publikováno v:
Cell, vol 158, iss 3
SummaryDepending on endoplasmic reticulum (ER) stress levels, the ER transmembrane multidomain protein IRE1α promotes either adaptation or apoptosis. Unfolded ER proteins cause IRE1α lumenal domain homo-oligomerization, inducing trans autophosphory
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::56b7569da9f8dea1aed176e2d9eaf89f
https://escholarship.org/uc/item/59n5c159
https://escholarship.org/uc/item/59n5c159
Autor:
Peter Hodder, William R. Roush, Judith A. Steen, Franck Madoux, Vimal Ramachandran, Stephan C. Schürer, Ruchi Chauhan, Ronald J. Rahaim, Scott Simanski, Choogon Lee, Nagi G. Ayad, Omar S. Barnaby, Clara Penas
Publikováno v:
The Journal of biological chemistry. 289(27)
Eukaryotic mitotic entry is controlled by Cdk1, which is activated by the Cdc25 phosphatase and inhibited by Wee1 tyrosine kinase, a target of the ubiquitin proteasome pathway. Here we use a reporter of Wee1 degradation, K328M-Wee1-luciferase, to scr
Publikováno v:
Journal of chemical information and modeling. 52(12)
Protein kinases remain among the most versatile and prospective therapeutic drug targets with currently 15 distinct compounds approved for use in humans and numerous clinical development programs. The vast majority of kinase inhibitors bind at the AT
Autor:
Thomas Schröter, Yan Yin, Michael D. Cameron, Stephan C. Schürer, Derek R. Duckett, Wayne Grant, Philip LoGrasso, Claudia Ruiz, Yangbo Feng, Jennifer Pocas, Li Lin, Weimin Chen
Publikováno v:
Bioorganicmedicinal chemistry letters. 19(23)
A series of benzothiazole derivatives as ROCK inhibitors have been discovered. Compounds with good biochemical and cellular potency, and sufficient kinase selectivity have been identified.
Autor:
Yen Ting Chen, Michael D. Cameron, Thomas D. Bannister, Evelyn Griffin, Claudia Ruiz, Stephan C. Schürer, Derek R. Duckett, Thomas Schröter, Yangbo Feng, Philip LoGrasso, Li Lin, Amiee Weiser
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(24)
Inhibition of Rho kinase (ROCK) is an attractive strategy for the treatment of diseases such as hypertension, glaucoma, and cancer. Here we report chroman-3-amides as highly potent ROCK inhibitors with sufficient kinase selectivity, excellent cell ac