Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Shannon Rumfelt"'
Autor:
Dah-Ren Hwang, John Castrillon, Shannon Rumfelt, Jennifer R. Allen, Essa Hu, Anissa Abi-Dargham, Carl Davis, Balu Easwaramoorthy, James J. S. Treanor, Hang Chen, Mark Slifstein
Publikováno v:
Nuclear Medicine and Biology. 41:343-349
Introduction Phosphodiesterase 10A (PDE10A) is an intracellular enzyme responsible for the breakdown of cyclic nucleotides which are important secondary messengers in the central nervous system. Inhibition of PDE10A has been identified as a potential
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e513d78ed165d00a8bcf84edd85dfd4d
https://doi.org/10.1016/j.nucmedbio.2014.01.007
https://doi.org/10.1016/j.nucmedbio.2014.01.007
Autor:
Qingyian Liu, Kaustav Biswas, Frank Koegler, Tiffany L. Correll, Toni Williamson, Jodi Bradley, Jennifer R. Allen, Leeanne Zalameda, Darren L. Reid, Michael D. Bartberger, Joe Zhu, Stephen J. Wood, Randy Hungate, Yichin Liu, Frank Chavez, Robert M. Rzasa, Jianhua Zhang, John D. McCarter, Thomas Nixey, Paul H. Wen, Li Zhu, Shannon Rumfelt, Yi Luo, Safura Babu-Khan, Stephen Hitchcock, Ning Chen, Mqhele Ncube, Wenyuan Qian, Frenel Fils Demorin, Dean Hickman, Christopher M. Tegley, Jian J. Chen, Albert Amegadzie, Charles W. Dean, Chester Chenguang Yuan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:6447-6454
γ-Secretase modulators (GSMs) are potentially disease-modifying treatments for Alzheimer's disease. They selectively lower pathogenic Aβ42 levels by shifting the enzyme cleavage sites without inhibiting γ-secretase activity, possibly avoiding know
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9f9717b5fcc1d773beec78fba83ce7ef
https://doi.org/10.1016/j.bmcl.2013.09.041
https://doi.org/10.1016/j.bmcl.2013.09.041
Autor:
Dianna Lester-Zeiner, Christopher Biorn, Essa Hu, Jianxia Shi, James J. S. Treanor, Sharon Zhao, Jennifer R. Allen, Amy Porter, Kristin L. Andrews, Samer Chmait, Shannon Rumfelt, Aaron C. Siegmund, Roxanne Kunz, Ning Chen, Hang Chen, Carl Davis, Ji Ma
Publikováno v:
Journal of Medicinal Chemistry. 56:8781-8792
Our development of PDE10A inhibitors began with an HTS screening hit (1) that exhibited both high p-glycoprotein (P-gp) efflux ratios in rat and human and poor metabolic stability. On the basis of cocrystal structure of 1 in human PDE10A enzyme, we d
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3066fe445a252131b55a29d74d2cd4ef
https://doi.org/10.1021/jm401234w
https://doi.org/10.1021/jm401234w
Autor:
Samer Chmait, Adrie D. Jones, Amy Porter, Kristin L. Andrews, Xiaoning Zhao, Jennifer R. Allen, Shannon Rumfelt, Wenge Zhong, Essa Hu, James R. Falsey, Robert M. Rzasa, Steven W. Louie, James J. S. Treanor, Ning Chen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7371-7375
We report the discovery of a novel series of biaryl ethers as potent and selective PDE10A inhibitors. Structure-activity studies improved the potency and decreased Pgp-mediated efflux found in the initial compound 4. X-ray crystallographic studies re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6c902b8d3ff73465c5b07e532310cd1d
https://doi.org/10.1016/j.bmcl.2012.10.078
https://doi.org/10.1016/j.bmcl.2012.10.078
Autor:
Dah-Ren Hwang, Geraldine Hill Della Puppa, Jamie Wong, Essa Hu, Thomas Nixey, Silke Miller, Hang Chen, Jessica Able, Dianna Lester-Zeiner, James J. S. Treanor, Robert Cho, Santosh Talreja, Roxanne Kunz, Jianxia Shi, Ji Ma, David C. Immke, Jennifer R. Allen, Christopher Biorn, Amy Porter, Klaus Michelsen, Shannon Rumfelt, Stephen Hitchcock
Publikováno v:
Journal of Medicinal Chemistry. 55:4776-4787
A radiolabeled tracer for imaging therapeutic targets in the brain is a valuable tool for lead optimization in CNS drug discovery and for dose selection in clinical development. We report the rapid identification of a novel phosphodiesterase 10A (PDE
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::626c862c5f50bd2845e3c603ba24a357
https://doi.org/10.1021/jm3002372
https://doi.org/10.1021/jm3002372
Autor:
Jeffrey H. Kogan, Samer Chmait, Chun Li, Essa Hu, Michelle Lindstrom, Jiandong Zhang, Kristin L. Andrews, Roland Burli, Roxanne Kunz, Stephen Hitchcock, James J. S. Treanor, Ning Chen, Shannon Rumfelt
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:2262-2265
We report the discovery of 6,7-dimethoxy-4-(pyridin-3-yl)cinnolines as novel inhibitors of phosphodiesterase 10A (PDE10A). Systematic examination and analyses of structure–activity-relationships resulted in single digit nM potency against PDE10A. X
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::865cbcb6f0a332d88ba4d4befabc0a9d
https://doi.org/10.1016/j.bmcl.2012.01.086
https://doi.org/10.1016/j.bmcl.2012.01.086
Autor:
Hu Ye, Tim Kazules, Ji Ma, Dianna Lester-Zeiner, Essa Hu, Santosh Talreja, Carl Davis, Charlie Glaus, Oliver R. Thiel, Ning Chen, Geraldine Hill Della Puppa, James J. S. Treanor, Shannon Rumfelt, Hui Hannah Dou, Roxanne Kunz, David C. Immke, Jessica Able, Jennifer R. Allen, Silke Miller, Xiaoning Zhao, Hang Chen, Jianxia Shi, Jamie Wong, Toni Williamson, Christopher Biorn, Amy Porter, Klaus Michelsen, Ada Chen
Publikováno v:
The Journal of pharmacology and experimental therapeutics. 352(2)
Phosphodiesterase 10A (PDE10A) inhibitors have therapeutic potential for the treatment of psychiatric and neurologic disorders, such as schizophrenia and Huntington's disease. One of the key requirements for successful central nervous system drug dev
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d2114c0263395e74897b10174822cf2a
https://pubmed.ncbi.nlm.nih.gov/25502803
https://pubmed.ncbi.nlm.nih.gov/25502803
Autor:
Roland Burli, Matthew H. Plant, Randall W. Hungate, Roxanne Kunz, Douglas A. Whittington, Yang Xu, Shannon Rumfelt, Gordon Ng, Violeta Yu, Michael Schrag, Ning Chen, Yen Nguyen, Yanyan Tudor, Andrew Tasker, Kristin Meagher, Essa Hu, Dawei Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5115-5117
Deregulation of the receptor tyrosine kinase c-Kit is associated with an increasing number of human diseases, including certain cancers and mast cell diseases. Interference of c-Kit signaling with multi-kinase inhibitors has been shown clinically to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdd2f15cb2f6855f01eb5d331d0b8302
https://doi.org/10.1016/j.bmcl.2008.07.111
https://doi.org/10.1016/j.bmcl.2008.07.111
Autor:
Essa Hu, James J. S. Treanor, Michelle Lindstrom, Shannon Rumfelt, Kristin L. Andrews, Stephen Hitchcock, Chun Li, Roxanne Kunz
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(22)
We report our successful effort to increase the PDE3 selectivity of PDE10A inhibitor pyridyl cinnoline 1 using a combination of computational modeling and structural-activity relationship investigations. An analysis of the PDE3 catalytic domain compa
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::126d4d25ed148a833fd16e6ee1fedab0
https://pubmed.ncbi.nlm.nih.gov/23044369
https://pubmed.ncbi.nlm.nih.gov/23044369