Zobrazeno 1 - 10
of 30
pro vyhledávání: '"Matthew P. Bourbeau"'
Autor:
Brian Belmontes, Jodi Moriguchi, Grace Chung, Jan Sun, Maria Stefania S. Ninniri, Kelly Hanestad, Kui Chen, John D. McCarter, Upendra P. Dahal, Sudipa Ghimire-Rijal, Yue Hao, Christopher P. Mohr, Xinchao Yu, Matthew G. Rees, Melissa Ronan, Jennifer Roth, Sheroy Minocherhomji, Jennifer R. Allen, Matthew P. Bourbeau, Paul E. Hughes, Nuria A Tamayo, Marc N. Payton
Publikováno v:
Cancer Research. 83:516-516
Chromosomal instability (CIN) is a hallmark of human cancers and is caused by persistent errors in chromosome segregation during mitosis. Aggressive types of human cancer such as high-grade serous ovarian cancer and triple-negative breast cancer have
Autor:
Nuria A. Tamayo, Matthew P. Bourbeau, Jennifer R. Allen, Kate S. Ashton, Jian Jeffrey Chen, Matthew R. Kaller, Thomas T. Nguyen, Nobuko Nishimura, Liping H. Pettus, Mary Walton, Brian Belmontes, Jodi Moriguchi, Kui Chen, John D. McCarter, Kelly Hanestad, Grace Chung, Maria Stefania S. Ninniri, Jan Sun, Leszek Poppe, Chris Spahr, John Hui, Lei Jia, Tian Wu, Upendra P. Dahal, Katheryne Z. Edson, Marc Payton
Publikováno v:
Journal of medicinal chemistry. 65(6)
Chromosomal instability (CIN) is a hallmark of cancer that results from errors in chromosome segregation during mitosis. Targeting of CIN-associated vulnerabilities is an emerging therapeutic strategy in drug development. KIF18A, a mitotic kinesin, h
Autor:
Jan Sun, Brain Belmontes, Jodi Moriguchi, Grace Chung, Kui Chen, John D. McCarter, Upendra P. Dahal, Andrew S. Boghossian, Matthew G. Rees, Melissa M. Ronan, Jennifer A. Roth, Sheroy Minocherhomji, Matthew P. Bourbeau, Jennifer R. Allen, Angela Coxon, Paul E. Hughes, Nuria Tamayo, Marc N. Payton
Publikováno v:
Cancer Research. 82:LB202-LB202
KIF18A is a mitotic kinesin that localizes to the plus-end tips of kinetochore microtubule (MT) spindle fibers during metaphase, where it regulates chromosome alignment, and promotes the viability of chromosomally unstable cancer cells. KIF18A is ove
Autor:
Paul H. Wen, Stephen J. Wood, Qingyian Liu, Aaron C. Siegmund, Liping H. Pettus, Adrian Nanez, Matthew P. Bourbeau, Jennifer R. Allen, Michael D. Bartberger, Douglas A. Whittington, Jodi Bradley, James R. Manning, Kui Chen, Dean Hickman, Michael E. Johnson
Publikováno v:
Journal of medicinal chemistry. 63(5)
β-Site amyloid precursor protein cleaving enzyme 1 (BACE1) is an aspartyl protease that plays a key role in the production of amyloid β (Aβ) in the brain and has been extensively pursued as a target for the treatment of Alzheimer's disease (AD). B
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
Autor:
Wenyuan Qian, Michael J. Frohn, Michael D. Bartberger, Stephen J. Wood, Albert Amegadzie, Aaron C. Siegmund, Ning Chen, Jennifer R. Allen, Dean Hickman, Helming Tan, Paul H. Wen, Longbin Liu, Matthew P. Bourbeau, Douglas A. Whittington
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 30:127240
The (Z)-fluoro-olefin amide bioisosteric replacement is an effective tool for addressing various shortcomings of the parent amide. In an effort to fine tune ADME properties of BACE1 preclinical candidate AM-6494, a series of structurally distinct (Z)
Publikováno v:
Journal of Medicinal Chemistry. 58:525-536
The development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease has been pursued by the pharmaceutical industry for some time. A number of recent disclosures describing potent ACC inhibitors have been reported by mul
Autor:
James Meyer, Kevin Salyers, Minghan Wang, Matthew P. Bourbeau, Yang Xu, Melissa Graham, Christopher H. Fotsch, John G. Allen, Wei Gu, Michael D. Bartberger, Mark R. Fielden, Murielle M. Véniant, Ki-Won Kim, James Busby, Aaron C. Siegmund, Renee Komorowski, Hong Shu
Publikováno v:
Journal of Medicinal Chemistry. 56:10132-10141
Acetyl-CoA carboxylase (ACC) is a target of interest for the treatment of metabolic syndrome. Starting from a biphenyloxadiazole screening hit, a series of piperazine oxadiazole ACC inhibitors was developed. Initial pharmacokinetic liabilities of the
Autor:
Matthew P. Bourbeau, Rider James Thomas, Douglas Hoffman, Xin Huang, Randall W. Hungate, Holger Monenschein, Qingping Zeng, Daniel J. Freeman, Shiwen Zhang, Andrew Tasker, Matthew R. Lee, Celia Dominguez, Elizabeth Tominey, Chun Li, Xiaoling Zhang, Vellarkad N. Viswanadhan, G. Erich Wohlhieter, Guomin Yao, Harvey Yamane, Julie A. Lofgren
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1652-1656
A series of 2-aminothiadiazole of inhibitors of AKT1 is described. SAR relationships are discussed, along with selectivity for protein kinase A (PKA) and cyclin-dependent kinase 2 (CDK2). Moderate selectivity observed in several compounds for AKT1 ve
Autor:
Fang-Tsao Hong, Christopher H. Fotsch, Xianghong Wang, Qingping Zeng, John G. Allen, G. Erich Wohlhieter, Chun Li, Yihong Zhou, Guomin Yao, Seifu Tadesse, Matthew P. Bourbeau, Chester Chenguang Yuan, Sekhar Surapaneni, Matthew R. Lee, Gary L. Skiles, Raju Subramanian, Xiaochun Zhu
Publikováno v:
Chemical Research in Toxicology. 23:653-663
A 2-aminothiazole derivative 1 was developed as a potential inhibitor of the oncology target AKT, a serine/threonine kinase. When incubated in rat and human liver microsomes in the presence of NADPH, 1 underwent significant metabolic activation on it