Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Deborah H. Slee"'
Autor:
Vivek Gupta, Deborah H. Slee, Ming Chen, John A. Muraski, Samir Mitragotri, Sunny Kumar, Aaron C. Anselmo
Publikováno v:
Journal of Controlled Release. 199:190-197
Cyclosporine A (CsA) is used for the treatment of psoriasis; however systemic administration of CsA is potentially life threatening and there are long-term side effects. Topical application of CsA has the potential to overcome this hurdle; however, i
Autor:
Deborah H. Slee, Ming Chen, Samir Mitragotri, John A. Muraski, Michael Zakrewsky, Aaron C. Anselmo, Vivek Gupta
Publikováno v:
Journal of Controlled Release. 179:33-41
Short-interfering RNAs (siRNAs) offer a potential tool for the treatment of skin disorders. However, applications of siRNA for dermatological conditions are limited by their poor permeation across the stratum corneum of the skin and low penetration i
Autor:
Marion Lanier, Xiaohu Zhang, John E. Tellew, Zhiyong Luo, Mark Santos, Raymond S. Gross, Deborah H. Slee, Emily Lin, Sandra M. Lechner, Jaimie K. Rueter, María I. Crespo, Jose-Luis Diaz, Yongsheng Chen, Siobhan Malany, Manisha Moorjani, John Saunders, John P. Williams, Binh G. Vong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:5402-5405
In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In additi
Publikováno v:
Neuropsychopharmacology. 34:106-125
Beginning with the discovery of the structure of deoxyribose nucleic acid in 1953, by James Watson and Francis Crick, the sequencing of the entire human genome some 50 years later, has begun to quantify the classes and types of proteins that may have
Autor:
Yongsheng Chen, Mark Santos, Emily Lin, Stacy Markison, John E. Tellew, Sandra M. Lechner, Maria Prat, Xiaohu Zhang, John Saunders, Silvia Gual, Marion Lanier, Marı´a I. Crespo, John P. Williams, Raymond S. Gross, Tanya Joswig, Jaimie K. Rueter, Deborah H. Slee, Siobhan Malany, Jose-Luis Diaz, Manisha Moorjani, Julio C. Castro-Palomino
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:1778-1783
A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM), selectivity (A(1)/A(2A) > 100), and efficacy (MED 10 mg/kg p.o.) in the rat haloperidol-indu
Autor:
Deborah H. Slee, Susan K. Sullivan, Neil J. Ashweek, Marion Lanier, Yun-Fei Zhu, Jaimie K. Rueter, Miklos Feher, Colin J. Loweth, Michael S. Brown, John P. Williams
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:5590-5603
The present article describes a selection of a new class of small molecule antagonists for the h-GnRH receptor, their preparation, and evaluation in vitro. Three computational methods were combined into a consensus score, to rank order virtual templa
Autor:
William Charles Ripka, Scott W. Nelson, Kevin M. Short, Michael J. Newman, Richard B. Honzatko, Karl Norvell, Frank U. Axe, Kristen L. Arienti, Deborah H. Slee, Tassie L. Collins, Todd K. Jones, Jun-young Choe, Herbert J. Fromm, Rachel Denise Anne Kimmich, Suzanne J. Romano
Publikováno v:
Journal of Biological Chemistry. 278:51176-51183
A highly constrained pseudo-tetrapeptide (OC252-324) further defines a new allosteric binding site located near the center of fructose-1,6-bisphosphatase. In a crystal structure, pairs of inhibitory molecules bind to opposite faces of the enzyme tetr
Autor:
Alexander Wlodawer, Alla Gustchina, Deborah H. Slee, Ian R. Ollmann, Chi-Huey Wong, Karen Laslo, Jukka Kervinen, John H. Elder, Alexander Zdanov
Publikováno v:
Journal of the American Chemical Society. 117:11867-11878
Autor:
Deborah H. Slee, Truc N. Nguyen, Mary Kish, Michael J. Newman, Stephen J. Mcconnell, Katy Lundeen, Abhijit S. Bhat
Publikováno v:
Journal of Medicinal Chemistry. 46:1120-1122
The regulation of lipid metabolism and it's effect on glucose control and diabetes has received intense interest. Hormone-sensitive lipase (HSL) is a vital enzyme in lipid metabolism. A series of novel pyrrolopyrazinediones has been discovered that d
Autor:
Emily Lin, Zhiyong Luo, Dimitri E. Grigoriadis, Marion Lanier, Xiaohu Zhang, Romano Di Fabio, Yves St. Denis, John E. Tellew, Enza Di Modugno, John Saunders, Deborah H. Slee, John P. Williams, Sam R. J. Hoare, Manisha Moorjani
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(24)
Antagonists of the corticotropin-releasing factor (CRF) neuropeptide may prove effective in treating stress and anxiety related disorders. In an effort to identify antagonists with improved physico-chemical properties a new series of CRF1 antagonists