Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Steven D. Linton"'
Autor:
Kevin J. Tomaselli, Julia Herrmann, Robert O. Sayers, Joe C. Wu, Lalitha Kodandapani, Kathy G. Jahangiri, Craig D. Fisher, David T. Winn, Edward D. Robinson, Steven P. Meduna, Robert J. Ternansky, Pauline Yeo, Karen L. Valentino, Jose-Luis Diaz, Vincent J. Kalish, Steven D. Linton, Kristen Sebring, Robert A. Armstrong, Joseph F. Krebs, Niel C. Hoglen, Alfred P. Spada, Brad P. Hirakawa, Ning Chen, Brett R. Ullman, Brett Weylan Ching, Cheng-zhi Zhang, Xu Bai, Xin Gu, Kip Nalley, Long-Shiuh Chen, Patricia L. Gladstone, Jeff McQuiston, Teresa Aja, Todd Groessl, Donald S. Karanewsky, Suzanne Weeks, Lawrence C. Fritz, Patricia C. Contreras
Publikováno v:
Journal of Medicinal Chemistry. 48:6779-6782
A series of oxamyl dipeptides were optimized for pan caspase inhibition, anti-apoptotic cellular activity and in vivo efficacy. This structure-activity relationship study focused on the P4 oxamides and warhead moieties. Primarily on the basis of in v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bc05f6b9f812322c1ff557485178cfdb
https://doi.org/10.1021/jm050307e
https://doi.org/10.1021/jm050307e
Autor:
Robert Smidt, Silvio Roggo, Julia Herrmann, Edward D. Robinson, Kathy G. Jahangiri, Teresa Aja, Kip Nalley, Thomas L. Deckwerth, Giorgio Rovelli, Kevin J. Tomaselli, Joe C. Wu, Bastian Hengerer, Steven P. Meduna, André Sauter, Jose-Luis Diaz, Joerg Kallen, Albert Schmitz, Donald S. Karanewsky, Brett R. Ullman, Steven D. Linton, Christoph Wiessner, Robert J. Ternansky, Peter R. Allegrini, Robert O. Sayers
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 14:2685-2691
Structural modifications were made to a previously described acyl dipeptide caspase inhibitor, leading to the oxamyl dipeptide series. Subsequent SAR studies directed toward the warhead, P2, and P4 regions of this novel peptidomimetic are described h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6fb680f6d4dacf778afb32ec56f318e3
https://doi.org/10.1016/j.bmcl.2003.12.106
https://doi.org/10.1016/j.bmcl.2003.12.106
Autor:
Robert Smidt, Jose-Luis Diaz, Lalitha Kodandapani, Joe C. Wu, Brian Pham, Donald S. Karanewsky, Kevin J. Tomaselli, Robert J. Ternansky, Lawrence C. Fritz, Steven D. Linton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 12:2969-2971
Parallel synthesis was used to explore the SAR of a peptidomimetic caspase inhibitor. The most potent compound had nanomolar activity against caspases 1, 3, 6, 7, and 8.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7078d5ac5fc6e3546ebfe8dd175cdeef
https://doi.org/10.1016/s0960-894x(02)00629-7
https://doi.org/10.1016/s0960-894x(02)00629-7
Publikováno v:
Tetrahedron Letters. 34:2577-2580
The first total synthesis of (+)-porothramycin B ( 1b is described. Our synthetic pathway can be readily applied to the synthesis of other members of the pyrrolo[1,4]benzodiazepine antibiotics.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::7191456e5ba8f93e7a326947c552c58b
https://doi.org/10.1016/s0040-4039(00)77629-5
https://doi.org/10.1016/s0040-4039(00)77629-5
Publikováno v:
ChemInform. 24
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c04d4d62a09cd1843c7de8432a746867
https://doi.org/10.1002/chin.199339300
https://doi.org/10.1002/chin.199339300
Autor:
Donald S. Karanewsky, Kevin J. Tomaselli, Bryan Pham, Joseph F. Krebs, Steven D. Linton, Xu Bai, Joe Wu
Publikováno v:
ChemInform. 30
A systematic study of interleukin-1β converting enzyme (ICE, caspase-1) and caspase-3 (CPP32, apopain) inhibitors incorporating a P2–P3 conformationally constrained dipeptide mimetic is reported. Depending on the nature of the P4 substituent, high
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::f8b26ecd63c52afb7c27a4f432df7c02
https://doi.org/10.1002/chin.199906175
https://doi.org/10.1002/chin.199906175
Autor:
Steven D. Linton, Tom O'Brien
Publikováno v:
Design of Caspase Inhibitors as Potential Clinical Agents
Presents the Therapeutic Potential for Caspase Inhibitors: Present and FutureCaspases represent one of the most specific protease families described to date. These extremely important enzymes are crucial to the destruction of aberrant cells - the bod
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8c83c69bc3e29c13b5c8d573f2c6bdcd
https://doi.org/10.1201/9781420045413
https://doi.org/10.1201/9781420045413
Publikováno v:
Tetrahedron Letters. 31:5989-5992
The first total synthesis of (±)-renieramycin A ( 1a ) is described. The stereochemistry of the angelate side chain was unequivocally determined by X-ray crystallographic analysis of the penultimate intermediate.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::32f1d1c44e77e975b912042ec0195351
https://doi.org/10.1016/s0040-4039(00)98010-9
https://doi.org/10.1016/s0040-4039(00)98010-9
Autor:
Steven D. Linton
Publikováno v:
Current topics in medicinal chemistry. 5(16)
Caspase inhibition has been demonstrated to be therapeutically effective in moderating excessive programmed cell death, or apoptosis. Publications detailing programs in the pharmaceutical industry have been more frequent in recent years, ranging from
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e3efe82d3f403e0001020d0060451620
https://pubmed.ncbi.nlm.nih.gov/16375749
https://pubmed.ncbi.nlm.nih.gov/16375749
Autor:
Teresa Aja, Kevin J. Tomaselli, Edward D. Robinson, Joe C. Wu, Steven D. Linton, Xin Gu, Robert O. Sayers, Steven P. Meduna, Kip Nalley, Lalitha Kodandapani, Silvio Roggo, Vincent J. Kalish, Jose-Luis Diaz, Donald S. Karanewsky, Ning Chen, Albert Schmitz, Julia Herrmann, Brett R. Ullman, Joseph J. Krebs, Robert J. Ternansky
Publikováno v:
Bioorganicmedicinal chemistry letters. 15(15)
Various heterocyclic hetero-methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A study of their structure-activity relationship (SAR) related to caspase-1, -3, -6, and -8 is reported. Their efficacy in a cellular model of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d20fa9b2635d713c24eee1115cb07fa3
https://pubmed.ncbi.nlm.nih.gov/15964758
https://pubmed.ncbi.nlm.nih.gov/15964758