Zobrazeno 1 - 10
of 31
pro vyhledávání: '"Thorsett Eugene D"'
Autor:
Thorsett, Eugene D., Harris, Elbert E., Peterson, Elwood R., Greenlee, William J., Patchett, Arthur A., Ulm, Edgar H., Vassil, Theodore C.
Publikováno v:
Proceedings of the National Academy of Sciences of the United States of America, 1982 Apr 01. 79(7), 2176-2180.
Externí odkaz:
https://www.jstor.org/stable/11590
Autor:
Thorsett, Eugene D, Latimer, Lee H
Publikováno v:
In Current Opinion in Chemical Biology 2000 4(4):377-382
Autor:
Jay S. Tung, Michael A. Pleiss, Albert W. Garofalo, Erich Goldbach, Cheryl A. Bales, David W. G. Wone, James E. Audia, Stephen Sohn, Darren B. Dressen, Thomas Edward Mabry, Angela Phuc, Nissen Jeffrey S, Thorsett Eugene D, Folmer Beverly K, Jing Wu, Harry F. Dovey, Ashley C. Guinn, Lee H. Latimer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:3051-3053
Potent, small molecule A beta inhibitors have been prepared that incorporate an alanine core bracketed by an N-terminal arylacetyl group and various C-terminal amino alcohols. The compounds exhibit stereospecific inhibition as demonstrated in an in v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e54cab507103921c3382fac6a78953b0
https://doi.org/10.1016/s0960-894x(02)00684-4
https://doi.org/10.1016/s0960-894x(02)00684-4
Autor:
Judevin Lugar, Kevin P. Quinn, Anna Liao, Darren B. Dressen, Linda Chen, Thomas N. Thompson, Elizabeth J. Holsztynska, Francine S. Farouz, Whitney Dunn, Christopher Vandevert, Ying-Zi Xu, Michael Jefferies, Thorsett Eugene D, Mark Dreyer, Michael A. Pleiss, Ted Yednock, Andrei W. Konradi, Stephen B. Freedman, Linda Mutter, Semko Christopher M
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(6)
A series of N-(pyrimidin-4-yl)-phenylalanine VLA-4 antagonists is described. Optimization of substituents at the 2 and 5 positions of the pyrimidine ring gave 14, a very potent VLA-4 inhibitor which is orally active in a sheep asthma model.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::982509e7bd4eb62add7249a723781903
https://pubmed.ncbi.nlm.nih.gov/21316228
https://pubmed.ncbi.nlm.nih.gov/21316228
Autor:
Semko, Christopher M., Chen, Linda, Dressen, Darren B., Dreyer, Mark L., Dunn, Whitney, Farouz, Francine S., Freedman, Stephen B., Holsztynska, Elizabeth J., Jefferies, Michael, Konradi, Andrei W., Liao, Anna, Lugar, Judevin, Mutter, Linda, Pleiss, Michael A., Quinn, Kevin P., Thompson, Thomas, Thorsett, Eugene D., Vandevert, Christopher, Xu, Ying-Zi, Yednock, Ted A.
Publikováno v:
In Bioorganic & Medicinal Chemistry Letters 2011 21(6):1741-1743
Autor:
Joseph B. Moon, Donna J. Paddock, Louis Brogley, and Sukanto Sinha, Nancy Jewett, Timothy E. Benson, Michael S. Dappen, John A. Tucker, Thomas L. Emmons, Roy K. Hom, Michel Maillard, Alfredo G. Tomasselli, Thorsett Eugene D, Shumeye Mamo, D. Bryan Prince, Varghese John, D. Danielle Woods, Michael J. Bienkowski
Publikováno v:
Journal of medicinal chemistry. 50(4)
The design and synthesis of a novel series of potent and cell permeable peptidomimetic inhibitors of the human beta-secretase (BACE) are described. These inhibitors feature a hydroxyethyl secondary amine isostere and a novel aromatic ring replacement
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::52cd1c1f1ac700a20d12b3fb48c9bf8c
https://pubmed.ncbi.nlm.nih.gov/17300163
https://pubmed.ncbi.nlm.nih.gov/17300163
Autor:
Nancy Jewett, Jay S Tung, Larry Fang, David L. Davis, Joseph B. Moon, Roy K. Hom, Donald E Walker, Shumeye Mamo, Varghese John, Thorsett Eugene D, Andrea Gailunas
Publikováno v:
Journal of medicinal chemistry. 47(1)
The hydroxyethylene (HE) transition state isostere was developed as a scaffold to provide potent, small molecule inhibitors of human beta-secretase (BACE). The previous work on the statine series proved critical to the discovery of HE structure-activ
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::65ab54da9c2e698e556dab7a00c45b1e
https://pubmed.ncbi.nlm.nih.gov/14695829
https://pubmed.ncbi.nlm.nih.gov/14695829
Autor:
John P. Anderson, Shumeye Mamo, David L. Davis, Roy K. Hom, Ashley C. Guinn, Thorsett Eugene D, Donald Walker, Jay S. Tung, Sukanto Sinha, Varghese John, J. Knops, Larry Fang, Nancy Jewett, Andrea Gailunas
Publikováno v:
Journal of medicinal chemistry. 46(10)
We describe the development of statine-based peptidomimetic inhibitors of human beta-secretase (BACE). The conversion of the peptide inhibitor 1 into cell-permeable peptidomimetic inhibitors of BACE was achieved through an iterative strategy of conce
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2726c906c9e75d647f93b7ef28c0d02
https://pubmed.ncbi.nlm.nih.gov/12723942
https://pubmed.ncbi.nlm.nih.gov/12723942
Autor:
David L. Davis, Nancy Jewett, Thorsett Eugene D, Roy K. Hom, Sukanto Sinha, Varghese John, John P. Anderson, Shumeye Mamo, Jay S. Tung, Donald Walker
Publikováno v:
Journal of medicinal chemistry. 45(2)
By use of the effectively cleaved beta-secretase (BACE) substrate (1), incorporation of a statine in P(1) resulted in a weak inhibitor 13 of the enzyme. Further substitution of P(1)'-Asp by P(1)'-Val in 13 results in a potent inhibitor 22 of BACE. Re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05d50ed2fca50aa92ed78b745c2770f1
https://pubmed.ncbi.nlm.nih.gov/11784130
https://pubmed.ncbi.nlm.nih.gov/11784130
Publisher Summary This chapter discusses the status of the active Alzheimer's disease (AD) therapeutic approaches as well as some areas that are only beginning to see medicinal chemistry activity. Though the exact pathogenic mechanisms of AD remain e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::76c85a00bd6dbd9f97e276a43bbaa6f6
https://doi.org/10.1016/s0065-7743(08)60891-x
https://doi.org/10.1016/s0065-7743(08)60891-x
