Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Michael R Gehring"'
Autor:
Paul G. Richardson, Xiaoyun Meng, Karen A. Maegley, A.E. Stewart, Pei-Pei Kung, Jose L Montano, Ya-Li Deng, Jinqiao Wan, Michael R. Gehring, Jordan L. Meier, Brigitte S Naughton, Stephan Grant, Dou Dengfeng, Chakrapani Subramanyam, Anthony R. Harris, Samantha Elizabeth Greasley, Barry A. Morgan, Wen Yan, Xuemin Cheng, Prakash B. Palde, William K Sonnenburg, Junli Feng, Chen Qiuxia, Thomas A Paul, Gary M. Gallego, Sylvie K. Sakata, Sergei Timofeevski, Patrick Bingham, Benjamin J. Burke, Alex Shaginian
Publikováno v:
ACS Med Chem Lett
[Image: see text] Two novel compounds were identified as Naa50 binders/inhibitors using DNA-encoded technology screening. Biophysical and biochemical data as well as cocrystal structures were obtained for both compounds (3a and 4a) to understand thei
Autor:
Tanya Michelle Jewell, Robert Steven Kania, Anand Sistla, Bennett Michael John, Michael R. Gehring, Evan Smith, Zehnder Luke Raymond, Shinji Yamazaki, Karen A. Maegley, Elena Z. Dovalsantos, Ben Burke, Fen Wang, Sacha Ninkovic, Jeff Wang, Joe Zhongxiang Zhou, Pei-Pei Kung, Min-Jean Yin, Michael J. Hickey, Martin James Wythes, Jerry Meng, Buwen Huang, Ping Kang, John F. Braganza, Ketan S. Gajiwala, Tatlock John H, Pramod P. Mehta
Publikováno v:
Journal of Medicinal Chemistry. 54:3368-3385
A novel class of heat shock protein 90 (Hsp90) inhibitors was discovered by high-throughput screening and was subsequently optimized using a combination of structure-based design, parallel synthesis, and the application of medicinal chemistry princip
Autor:
Pramod P. Mehta, Tod Smeal, Min-Jean Yin, Gerrit Los, Michael R. Gehring, Shinji Yamazaki, Marlena Walls, Leslie Nguyen, Andrea Shen, Pei-Pei Kung
Publikováno v:
Cancer Letters. 300:30-39
Hsp90 is required for conformational maturation and stability of numerous key signaling proteins (clients) involved in cell proliferation and transformation. Here we describe two novel Hsp90 inhibitors, PF-4470296 and PF-3823863, demonstrate a differ
Publikováno v:
Biochemistry. 49:8488-8498
The mammalian target of rapamycin (mTOR) is a Ser/Thr protein kinase and a major controller of cell growth. In cells, mTOR forms two distinct multiprotein complexes, mTORC1 and mTORC2. The mTORC1 complex can phosphorylate 4EBP1 and S6K1, two key regu
Autor:
Pramod P, Mehta, Pei-Pei, Kung, Shinji, Yamazaki, Marlena, Walls, Andrea, Shen, Leslie, Nguyen, Michael R, Gehring, Gerrit, Los, Tod, Smeal, Min-Jean, Yin
Publikováno v:
Cancer Letters. 422:132
Autor:
Jennifer A. Digits, Jeff Elleraas, Gang Zhang, Ketan S. Gajiwala, Pei-Pei Kung, Michael J. Hickey, Min-Jean Yin, Michael Zientek, Buwen Huang, Caroline Rodgers, Shinji Yamazaki, Michael R. Gehring, Joe Zhongxiang Zhou, Jay F. Davies, Judith Skaptason, Jeff Wang, David Neul, Pramod P. Mehta
Publikováno v:
Journal of Medicinal Chemistry. 53:499-503
The discovery and optimization of potency and metabolic stability of a novel class of dihyroxyphenylisoindoline amides as Hsp90 inhibitors are presented. Optimization of a screening hit using structure-based design and modification of log D and chemi
Autor:
Ping Kang, Pei-Pei Kung, Jeff Wang, Michael R. Gehring, Monica Jo Patten, Michael J. Hickey, Ketan S. Gajiwala, Buwen Huang, Sujin Cho-Schultz, Sutton Scott Channing, Pramod P. Mehta, Jeff Elleraas
Publikováno v:
Journal of Combinatorial Chemistry. 11:860-874
As part of an oncology chemistry program directed toward discovery of orally bioavailable inhibitors of the 90 kDa heat shock protein (Hsp90), several solution-phase libraries were designed and prepared. A 2 x 89 library of racemic resorcinol amides
Publikováno v:
Metabolic Engineering. 7:38-44
In this paper, we described the optimization of a generic binding assay to measure ligand–receptor interactions for peroxisome proliferator-activated receptors (PPARs). The assay is based on scintillation proximity assay, in which a protein is coat
Autor:
Michele Ann Mctigue, Michael R Gehring, Chris Pinko, J. Ernest Villafranca, Chen-Chen Kan, Camran V Parast, Krzysztof Appelt, Richard E. Showalter, Barbara Mroczkowski, John A Wickersham, Anna Tempczyk-Russell
Publikováno v:
Structure. 7:319-330
Background: Angiogenesis is involved in tumor growth, macular degeneration, retinopathy and other diseases. Vascular endothelial growth factor (VEGF) stimulates angiogenesis by binding to specific receptors (VEGFRs) on the surface of vascular endothe
Publikováno v:
bchm. 379:185-192
Human pro-matrix metalloproteinase 3 (proMMP-3) lacking the N-terminal 34 amino acids and the C-terminal hemopexin-like domain was expressed in E. coli and used to investigate the process of proenzyme activation and its interaction with an endogenous