Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Stephan C. Schürer"'
Autor:
A Masson, SO Abdul-Hay, Juliette Bertrand, Umberto Crisafulli, Michael P. McGuire, Franck Madoux, Terrone R. Rosenberry, Michael D. Cameron, Caitlyn L. Topper, Caroline R. Thompson, Thomas D. Bannister, Thomas R. Caulfield, Peter Hodder, Malcolm A. Leissring, H Wang, Erin A. Howard, Stephan C. Schürer
Publikováno v:
ACS Chem Biol
Many therapeutically important enzymes are present in multiple cellular compartments, where they can carry out markedly different functions, thus there is a need for pharmacological strategies to selectively manipulate distinct pools of target enzyme
Autor:
Omar Moukha-Chafiq, Yali Dou, Chenzhong Liao, Vibha Pathak, Garrett S. Gibbons, Robert C. Reynolds, Amarraj Chakraborty, Stephan C. Schürer, Timothy S. Snowden, Afoma C. Umeano, Sierrah M. Grigsby, Zaneta Nikolovska-Coleska, Bini Mathew, Young Tae Lee
Publikováno v:
Eur J Med Chem
Disruptor of Telomeric Silencing 1-Like (DOT1L), the sole histone H3 lysine 79 (H3K79) methyltransferase, is required for leukemogenic transformation in a subset of leukemias bearing chromosomal translocations of the Mixed Lineage Leukemia (MLL) gene
Autor:
Ronald J. Rahaim, Yoshihiko Noguchi, Yangbo Feng, Shima Nakanishi, Lin Li, Konstantin Licht, Laura H. Rosenberg, Weimin Chen, John L. Cleveland, Stephan C. Schürer, William R. Roush, Jun Yong Choi, Michael D. Cameron, Mathieu Bibian, Derek R. Duckett
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:4374-4380
The development of a series of potent and highly selective casein kinase 1δ/e (CK1δ/e) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highl
Autor:
Mohd Hafeez Faridi, Ruth Day, Vineet Gupta, Darren Stoub, Constantinos J. Barth, Stephan C. Schürer, Dony Maiguel
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6902-6906
We report the identification of novel small molecule agonists of integrin CD11b/CD18, which increased, in a dose-dependent manner, the adhesion of the integrin CD11b/CD18 expressing cells to two physiologically relevant ligands: Fibrinogen and iC3b.
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:
Timothy P. Spicer, Peter Hodder, Pedro J. Gonzalez-Cabrera, Steven J. Brown, Peter Chase, Jacqueline Chapman, Hugh Rosen, Marie Therese Schaeffer, Euijung Jo, Stephan C. Schürer
Publikováno v:
ACS Chemical Biology. 3:486-498
We have studied the sphingosine 1-phosphate (S1P) receptor system to better understand why certain molecular targets within a closely related family are much more tractable when identifying compelling chemical leads. Five medically important G-protei
Publikováno v:
F1000Research
Kinases regulate cell growth, movement, and death. Deregulated kinase activity is a frequent cause of disease. The therapeutic potential of kinase inhibitors has led to large amounts of published structure activity relationship (SAR) data. Bioactivit
Autor:
Maria Laura Cremona, Ai Yamamoto, Udo Többen, Dusica Vidovic, Yuli Xie, Nathalie Aulner, Donald W. Landry, Caty Chung, Lars Branden, Gangli Gong, Katherine M. Myers, Alison Rinderspacher, Stephan C. Schürer, Yidong Liu, Monique Andersen, Shi Xian Deng
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:1715-1717
A quinazoline that decreases polyglutamine aggregate burden in a cell-based assay was identified from a high-throughput screen of a chemical-compound library, provided by the NIH Molecular Libraries Small Molecule Repository (MLSMR). A structure and
Autor:
Sarwat Chowdhury, Peter Chase, Thomas D. Bannister, Timothy P. Spicer, Peter Hodder, Daniel W. Zaharevitz, Melissa Crisp, Yuanjun He, Vincent W. Yang, Franck Madoux, Agnieszka Bialkowska, Chenlu Tian, Stephan C. Schürer
The transcription factor Krüppel-like factor 5 (KLF5) is primarily expressed in the proliferative zone of the mammalian intestinal epithelium, where it regulates cell proliferation. Studies showed that inhibition of KLF5 expression reduces prolifera
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87d3a6e19206e2ede64d0fad7896c49b
https://europepmc.org/articles/PMC3213326/
https://europepmc.org/articles/PMC3213326/
Autor:
Deborah H. Smith, Alison Rinderspacher, Shi Xian Deng, Dusica Vidovic, Torkel Vang, Stephan C. Schürer, Tomas Mustelin, Robert C. Rickert, Yidong Liu, Donald W. Landry, Yuli Xie, Gangli Gong, Wallace Liu, Lutz Tautz, Caty Chung, Shuangding Wu
Publikováno v:
Journal of medicinal chemistry. 54(2)
The lymphoid tyrosine phosphatase (Lyp, PTPN22) is a critical negative regulator of T cell antigen receptor (TCR) signaling. A single-nucleotide polymorphism (SNP) in the ptpn22 gene correlates with the incidence of various autoimmune diseases, inclu