Zobrazeno 1 - 10
of 320
pro vyhledávání: '"Stephen W Fesik"'
Autor:
Andrew J. Siladi, Jing Wang, Andrea C. Florian, Lance R. Thomas, Joy H. Creighton, Brittany K. Matlock, David K. Flaherty, Shelly L. Lorey, Gregory C. Howard, Stephen W. Fesik, April M. Weissmiller, Qi Liu, William P. Tansey
Publikováno v:
Scientific Reports, Vol 12, Iss 1, Pp 1-11 (2022)
Abstract WDR5 nucleates the assembly of histone-modifying complexes and acts outside this context in a range of chromatin-centric processes. WDR5 is also a prominent target for pharmacological inhibition in cancer. Small-molecule degraders of WDR5 ha
Externí odkaz:
https://doaj.org/article/4970649d70db445fb70eaa8e823937b6
Publikováno v:
Molecular & Cellular Oncology, Vol 7, Iss 2 (2020)
The oncoprotein transcription factor MYC is overexpressed in most cancers and is responsible for hundreds of thousands of cancer deaths worldwide every year. MYC is also a highly validated – but currently undruggable – anti-cancer target. We rece
Externí odkaz:
https://doaj.org/article/2a2e594b9e5d48a3bc01fda6686bdc6c
Autor:
Joachim Bröker, Alex G. Waterson, Chris Smethurst, Dirk Kessler, Jark Böttcher, Moriz Mayer, Gerhard Gmaschitz, Jason Phan, Andrew Little, Jason R. Abbott, Qi Sun, Michael Gmachl, Dorothea Rudolph, Heribert Arnhof, Klaus Rumpel, Fabio Savarese, Thomas Gerstberger, Nikolai Mischerikow, Matthias Treu, Lorenz Herdeis, Tobias Wunberg, Andreas Gollner, Harald Weinstabl, Andreas Mantoulidis, Oliver Krämer, Darryl B. McConnell, Stephen W. Fesik
Publikováno v:
Journal of Medicinal Chemistry. 65:14614-14629
Autor:
Erin R. Aho, Jing Wang, Rocco D. Gogliotti, Gregory C. Howard, Jason Phan, Pankaj Acharya, Jonathan D. Macdonald, Ken Cheng, Shelly L. Lorey, Bin Lu, Sabine Wenzel, Audra M. Foshage, Joseph Alvarado, Feng Wang, J. Grace Shaw, Bin Zhao, April M. Weissmiller, Lance R. Thomas, Christopher R. Vakoc, Matthew D. Hall, Scott W. Hiebert, Qi Liu, Shaun R. Stauffer, Stephen W. Fesik, William P. Tansey
Publikováno v:
Cell Reports, Vol 26, Iss 11, Pp 2916-2928.e13 (2019)
Summary: The chromatin-associated protein WDR5 is a promising target for pharmacological inhibition in cancer. Drug discovery efforts center on the blockade of the “WIN site” of WDR5, a well-defined pocket that is amenable to small molecule inhib
Externí odkaz:
https://doaj.org/article/624392b24e9c465daac627e90b1195e5
Autor:
Stephen W. Fesik, Alex G. Waterson, Olivia W. Rossanese, Michael C. Burns, Denis T. Akan, Jennifer E. Howes
Treatment with 1 does not cause total protein levels of SPRY2, SPRY4, DUSP4 and DUSP16 to increase. HeLa cells were treated with 50 μM 1 over a time course of up to 180 minutes. EGF (50 ng/mL for 5 minutes) was used as a positive control. HCT 116 ly
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::09fd5e2be2439e67e9c2690aad808a50
https://doi.org/10.1158/1535-7163.22505280.v1
https://doi.org/10.1158/1535-7163.22505280.v1
Autor:
Stephen W. Fesik, Alex G. Waterson, Olivia W. Rossanese, Michael C. Burns, Denis T. Akan, Jennifer E. Howes
Oncogenic mutation of RAS results in aberrant cellular signaling and is responsible for more than 30% of all human tumors. Therefore, pharmacologic modulation of RAS has attracted great interest as a therapeutic strategy. Our laboratory has recently
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::e86b5dbecdff349cba3b81582433effa
https://doi.org/10.1158/1535-7163.c.6538014.v1
https://doi.org/10.1158/1535-7163.c.6538014.v1
Autor:
Michael R. Savona, Stephen W. Fesik, Edward T. Olejniczak, Gregory D. Ayers, Leah J. Hogdal, John Sensintaffar, Stephen A. Strickland, Kelli L. Boyd, Londa Fuller, Maria Pia Arrate, Agnieszka E. Gorska, Taekyu Lee, Melissa A. Fischer, Haley E. Ramsey
Supplementary figures and table
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75a65705db4645e57301fe7bf49f1478
https://doi.org/10.1158/2159-8290.22534147.v1
https://doi.org/10.1158/2159-8290.22534147.v1
Autor:
Stephen W. Fesik, Alex G. Waterson, Olivia W. Rossanese, Michael C. Burns, Denis T. Akan, Jennifer E. Howes
Protein kinase inhibition profile for 1. Compound 1 was tested against a panel of 342 kinases at a single dose concentration of 20 μM. Columns labeled 'Data 1' and 'Data 2' indicate data from technical replicates. Control compound staurosporine was
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2653646ab1837d21a94eae4544aacb91
https://doi.org/10.1158/1535-7163.22505259
https://doi.org/10.1158/1535-7163.22505259
Autor:
Michael R. Savona, Stephen W. Fesik, Edward T. Olejniczak, Gregory D. Ayers, Leah J. Hogdal, John Sensintaffar, Stephen A. Strickland, Kelli L. Boyd, Londa Fuller, Maria Pia Arrate, Agnieszka E. Gorska, Taekyu Lee, Melissa A. Fischer, Haley E. Ramsey
Suppression of apoptosis by expression of antiapoptotic BCL2 family members is a hallmark of acute myeloblastic leukemia (AML). Induced myeloid leukemia cell differentiation protein (MCL1), an antiapoptotic BCL2 family member, is commonly upregulated
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7f6e8f2266d8ea8d3407f3dac4b6921b
https://doi.org/10.1158/2159-8290.c.6547384
https://doi.org/10.1158/2159-8290.c.6547384
Autor:
Alex R. Shoemaker, Steven W. Elmore, Saul H. Rosenberg, Stephen W. Fesik, David J. Frost, Christin Tse, Joy Bauch, Sanjay R. Chemburkar, Baole Wang, Sally Schlessinger, Marion Refici, Anatol Oleksijew, Kelly Foster, Michael J. Mitten, Yu Xiao, Scott Ackler
Supplementary Fig. S1 from ABT-263 and rapamycin act cooperatively to kill lymphoma cells in vitro and in vivo
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc855370bebdfa4ee58ecc2565eb8e85
https://doi.org/10.1158/1535-7163.22483001.v1
https://doi.org/10.1158/1535-7163.22483001.v1