Zobrazeno 1 - 10
of 11
pro vyhledávání: '"Jennifer Dao"'
Autor:
Alan C. Cheng, Elizabeth M. Doherty, Sheree Johnstone, Erin F. DiMauro, Jennifer Dao, Abhinav Luthra, Jay Ye, Jie Tang, Thomas Nixey, Xiaoshan Min, Philip Tagari, Les P. Miranda, Zhulun Wang
Publikováno v:
Scientific Reports, Vol 8, Iss 1, Pp 1-9 (2018)
Abstract Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of “chemibodies” as small molecule-antibody hybrids that offer dual re
Externí odkaz:
https://doaj.org/article/03c054e59aee48aa9fd15ab0e960b901
Autor:
David Powers, Katja Labitzke, Mark J. Rose, Kristin L. Andrews, Richard Kendall, Kenneth R. Dellamaggiore, Shon Booker, Peter Jaeckel, Silvia Materna-Reichelt, Mark H. Norman, Young-Ah Chung, Holger Beckmann, Paul L. Shaffer, Pedro J. Beltran, Hao Chen, Alexander M. Long, Petia Mitchell, Adrian L. Smith, Jennifer Dao, J. Russell Lipford, Noel D'angelo, Steven F. Bellon, Michelle Wu
Publikováno v:
Journal of Medicinal Chemistry. 58:1426-1441
The structure-based design and optimization of a novel series of selective PERK inhibitors are described resulting in the identification of 44 as a potent, highly selective, and orally active tool compound suitable for PERK pathway biology exploratio
Autor:
Kathleen S. Keegan, Hong Shu, Michael D. Bartberger, Julie M. Bailis, Guomin Yao, Jennifer Dao, Matthew R. Kaller, Andreas Reichelt, John G. Allen, Margaret F. Weidner
Publikováno v:
European Journal of Medicinal Chemistry. 80:364-382
The Cell division cycle 7 (Cdc7) protein kinase is essential for DNA replication and maintenance of genome stability. We systematically explored thiazole-based compounds as inhibitors of Cdc7 kinase activity in cancer cells. Our studies resulted in t
Autor:
Jennifer Dao, Erin F. DiMauro, Elizabeth M. Doherty, Jie Tang, Philip Tagari, Alan C. Cheng, Jing Ye, Les P. Miranda, Xiaoshan Min, Thomas Nixey, Zhulun Wang, Abhinav Luthra, Sheree Johnstone
Publikováno v:
Acta Crystallographica Section A Foundations and Advances. 75:a220-a220
Small molecules and antibodies each have advantages and limitations as therapeutics. Here, we present for the first time to our knowledge, the structure-guided design of "chemibodies" as small molecule-antibody hybrids that offer dual recognition of
Autor:
Christopher M. Tegley, Philip Tagari, José M. Morachis, Jeffery K. Lewis, Violeta Yu, Robert J.M. Kurzeja, Jennifer Dao, Henrike Veith
Publikováno v:
Analytical Biochemistry. 384:213-223
The human hypoxia-inducible factor prolyl hydroxylases 1, 2, and 3 (HIF-PHD1, -2, and -3) are thought to act as proximal sensors of cellular hypoxia by virtue of their mechanism-based dependence on molecular oxygen. These 2-oxoglutarate (2-OG) and no
Autor:
Jennifer E. Golden, Randall W. Hungate, Alexander J. Pickrell, Gloria Biddlecome, Roland Burli, Mike Frohn, Jennifer Dao, Norma Rogers, Vellarkad N. Viswanadhan, Jennifer R. Allen, Kristine M. Muller, Sean Yoder
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5023-5026
We report the structure-based design and synthesis of a novel series of aza-benzimidazoles as PHD2 inhibitors. These efforts resulted in compound 22, which displayed highly potent inhibition of PHD2 function in vitro.
Autor:
Randall W. Hungate, Jennifer Dao, Christopher M. Tegley, Sean Yoder, Catherine H. Chang, Tanya Peterkin, Roland Burli, Henrike Veith, Jennifer R. Allen, Philip Tagari, Norma Rogers, Kaustav Biswas, Vellarkad N. Viswanadhan, Michael J. Frohn, Gloria Biddlecome
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3925-3928
Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors.
Autor:
Christopher M. Tegley, Chi-Hwei Lin, Xianghong Wang, Tae-Seong Kim, Tony I. Lee, Jennifer Dao, Christopher Mohr, Sandra Ross, Andrew Hague, Andrew Tasker, Steven R. Jordan, Philip Tagari, Brian Lian, Carol Mayeda, Teresa L. Burgess, Vellarkad N. Viswanadhan, Janet Cheetham, Yi-xin Qian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:87-90
A series of (4-piperidinylphenyl)aminoethyl amides based on dipeptide anilines were synthesized and tested against cathepsin K, cathepsin L and cathepsin B. These new non-covalent inhibitors exhibited single-digit nM inhibition of the cysteine protea
Autor:
Elizabeth R. Gillard, Chuck A. Turkowski, Rishi K. Goel, Jennifer Dao, Faizi A. Jamal, Margarita C. Currás, Arshad M. Khan, Stefany D. Wolfsohn, B. Glenn Stanley
Publikováno v:
American Journal of Physiology-Regulatory, Integrative and Comparative Physiology. 276:R880-R891
Cells within the lateral hypothalamic area (LHA) are important in eating control. Glutamate or its analogs, kainic acid (KA) and N-methyl-d-aspartate (NMDA), elicit intense eating when microinjected there, and, conversely, LHA-administered NMDA recep
Publikováno v:
Brain research. Molecular brain research. 70(2)
NMDA receptor activation produces a characteristic pattern of neuronal firing in magnocellular neuroendocrine cells (MNCs) of the supraoptic nucleus of the hypothalamus (SON) which has been associated with greater hormone release in vivo and in vitro