Zobrazeno 1 - 10
of 27
pro vyhledávání: '"E. A. Kallel"'
Autor:
Sean Ekins, Jair Lage de Siqueira-Neto, Laura-Isobel McCall, Malabika Sarker, Maneesh Yadav, Elizabeth L Ponder, E Adam Kallel, Danielle Kellar, Steven Chen, Michelle Arkin, Barry A Bunin, James H McKerrow, Carolyn Talcott
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 9, Iss 6, p e0003878 (2015)
BACKGROUND:Chagas disease is a neglected tropical disease (NTD) caused by the eukaryotic parasite Trypanosoma cruzi. The current clinical and preclinical pipeline for T. cruzi is extremely sparse and lacks drug target diversity. METHODOLOGY/PRINCIPAL
Externí odkaz:
https://doaj.org/article/b9e8a9fd005b4febbb1b946f9673640a
Autor:
Kenneth Steadman, Gregory S. Parker, Geoffray Leriche, Sarah Fish, Julia Toth, Mary E. Spalding, Elizabeth Daniele, Aleksandar Jamborcic, Xiaoming Li, E Adam Kallel, Farhana Barmare, Kenneth Chng, Erika Green, Michael Hocker, Elliot Imler, Yi Zhang, Peggy A. Thompson, Simon Bailey
Publikováno v:
Cancer Research. 82:421-421
Prostate cancer is the second most common cause of cancer related deaths in men in the United States. Pathogenesis is driven by the androgen receptor (AR), which has led to front-line treatment modalities that are based on androgen deprivation therap
Autor:
Peggy A. Thompson, Pengyu Yang, Xiaoming Li, Stephen Chien, Mary E. Spalding, Alejandro Dearie, Elizabeth Daniele, Linette Yang, E Adam Kallel, Aleksandar Jamborcic, Julia Toth, Gregory Parker, Simon Bailey
Publikováno v:
Cancer Research. 82:1111-1111
Targeted protein degradation (TPD) using the endogenous Ubiquitin Proteasome System (UPS) is a rapidly growing drug discovery strategy to eliminate pathogenic proteins. Molecular glues are small molecules that promote a novel interaction between a pr
Autor:
Eric Brown, E. Adam Kallel, Donald D. Lorimer, Arshil Master, Ken McCormack, Alexandra Fetsko, David M. Dranow, Nadezda V. Sokolova, Rana Sidhu, Alexander N. Freiberg, Vidyasagar Reddy Gantla, Plewe Michael Bruno, Jameson Bullen, Greg Henkel, Junru Wang, Shibani Naik, Birte Kalveram, Hayden Smutney, Lihong Zhang
Publikováno v:
ACS Med Chem Lett
[Image: see text] We identified and explored the structure–activity-relationship (SAR) of an adamantane carboxamide chemical series of Ebola virus (EBOV) inhibitors. Selected analogs exhibited half-maximal inhibitory concentrations (EC(50) values)
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 26:3010-3013
The unusual activity differences of carbon linked versus oxygen linked 2-substituted piperazines as α7 nicotinic acetylcholine receptor agonists led to a conformational study of several examples. The conformational preferences of which are absent fr
Autor:
Jyun-Hung Chen, Thomas R. Caferro, Charlotte Pooley Deckhut, Lin Zhi, Christopher M. Tegley, Keith B. Marschke, Anthony W. Thompson, James P. Edwards, E. Adam Kallel, Marquis L. Cummings, Francisco J. López, William T. Schrader, Robert I. Higuchi, Mark E. Adams, Donald S. Karanewsky
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:5442-5446
A series of androgen receptor modulators based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones was synthesized and evaluated in an androgen receptor transcriptional activation assay. The most potent analogues from the series exhibited single-digit nanomolar
Autor:
Jeffrey N. Miner, Deepa Rungta, Lino J. Valdez, Yongkai Li, Andrew Hudson, William W. Lamph, Jean Yen, Dean P. Phillips, and Andrés Negro-Vilar, Lin Zhi, Angie Vassar, Catalina Cuervo, Reid P. Bissonnette, Keith B. Marschke, E. Adam Kallel, Mark E. Adams, Catherine J. Gharbaoui, Robert I. Higuchi, Dale E. Mais, Steven L. Roach
Publikováno v:
Journal of Medicinal Chemistry. 50:4699-4709
Structure-activity relationship studies centered around 3'-substituted (Z)-5-(2'-(thienylmethylidene))1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-chromeno[3,4-f]quinolines are described. A series of highly potent and efficacious selective glu
Autor:
James H. McKerrow, Steven Chen, Danielle Kellar, Jair L. Siqueira-Neto, Michelle R. Arkin, Laura-Isobel McCall, Maneesh K. Yadav, E. Adam Kallel, Carolyn L. Talcott, Barry A. Bunin, Elizabeth L. Ponder, Sean Ekins, Malabika Sarker
Publikováno v:
PLoS Neglected Tropical Diseases
PLoS Neglected Tropical Diseases, Vol 9, Iss 6, p e0003878 (2015)
PLoS Neglected Tropical Diseases, Vol 9, Iss 6, p e0003878 (2015)
Background Chagas disease is a neglected tropical disease (NTD) caused by the eukaryotic parasite Trypanosoma cruzi. The current clinical and preclinical pipeline for T. cruzi is extremely sparse and lacks drug target diversity. Methodology/Principal
Autor:
Kai-ni Liang, E. Adam Kallel, Feng Wang, He Li, Arjan van Oeveren, Mei Hong, Jeffrey N. Miner, Zhi Lin, Tao Jiang, Xiao-qin Liu
Publikováno v:
Acta Crystallographica Section F Structural Biology and Crystallization Communications. 62:1067-1071
The androgen receptor (AR) is a ligand-inducible steroid hormone receptor that mediates androgen action, determining male sexual phenotypes and promoting spermatogenesis. As the androgens play a dominant role in male sexual development and function,
Publikováno v:
Journal of the American Chemical Society. 125:5839-5848
The allowed conrotatory cyclobutene ring-opening has a distinctly nonplanar carbon skeleton. Classic experiments by Brauman and Archie, and by Freedman et al., placed the allowed/forbidden gap at greater than 15 kcal/mol. Wolfgang Roth proposed that