Zobrazeno 1 - 10
of 56
pro vyhledávání: '"Kevin J. Tomaselli"'
Autor:
Kevin J. Tomaselli
Publikováno v:
The Scientific World Journal, Vol 1, Pp 104-104 (2001)
Externí odkaz:
https://doaj.org/article/e8419997f4584bdc9e473e100a4665cf
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
Autor:
Shinichi Kitada, Jacqueline M. O'Connor, John C. Reed, Wendt Michael D, Andrew M. Petros, Alexander R. Shoemaker, Anatol Oleksijew, David J. Augeri, Craig B. Thompson, Kunzer Aaron R, Jürgen Dinges, Thomas L. Deckwerth, Stanley J. Korsmeyer, Saul H. Rosenberg, Stephen K. Tahir, Barbara A. Belli, Paul Nimmer, Baole Wang, Shi Chung Ng, Steven W. Elmore, Anthony Letai, Wang Shen, Haichao Zhang, Tilman Oltersdorf, Stephen W. Fesik, Milan Bruncko, David G. Nettesheim, Robert C. Armstrong, Michael J. Mitten, Kevin J. Tomaselli, Mary K. Joseph, Philip J. Hajduk, Chi Li
Publikováno v:
Nature. 435:677-681
Proteins in the Bcl-2 family are central regulators of programmed cell death, and members that inhibit apoptosis, such as Bcl-X(L) and Bcl-2, are overexpressed in many cancers and contribute to tumour initiation, progression and resistance to therapy
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
Autor:
Edward D. Robinson, Silvio Roggo, Joe C. Wu, Robert J. Ternansky, Jose-Luis Diaz, Teresa Aja, Kevin J. Tomaselli, Steven P. Meduna, Vincent J. Kalish, Donald S. Karanewsky, Robert O. Sayers, Albert Schmitz, Brett R. Ullman, Julia Herrmann, Kip Nalley, Thomas L. Deckwerth
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3623-3626
Various aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum
Autor:
Teresa Aja, André Sauter, Donald S. Karanewsky, Markus Rudin, Rachel May, Peter R. Allegrini, Bastian Hengerer, Robert O. Sayers, Christoph Wiessner, Steve Linton, Albert Schmitz, Giorgio Rovelli, Kevin J. Tomaselli, Patricia C. Contreras, Joe C. Wu, Silvio Roggo, Kip Nalley, Lisa M. Adams, Thomas L. Deckwerth
Publikováno v:
Drug Development Research. 52:579-586
Apoptotic cell death occurs in the injured and diseased central nervous system. It is mediated by a family of caspases, which are activated by the lethal stimulus and cleave multiple protein substrates that are critical for cell viability. Previous s
Autor:
Anu Srinivasan, Lawrence C. Fritz, Joseph F. Krebs, Kevin J. Tomaselli, Joe C. Wu, Angela M. Wong
Publikováno v:
Biochemistry. 39:16056-16063
Heavy membrane preparations from 697 lymphoblastoid cells contain a tightly bound caspase zymogen. This heavy membrane-bound procaspase can be efficiently liberated from membrane preparations using detergents. Alternatively, the procaspase can be rap
Autor:
Nancy A. Thornberry, Michael A. Moskowitz, Hideaki Hara, Shin Jung Kang, Anu Srinivasan, Kevin J. Tomaselli, Sepideh Amin-Hanjani, Junying Yuan, Zhihong Huang, Erin P. Peterson, Shobu Namura, Suyue Wang
Publikováno v:
The Journal of Cell Biology
Caspase-11, a member of the murine caspase family, has been shown to be an upstream activator of caspase-1 in regulating cytokine maturation. We demonstrate here that in addition to its defect in cytokine maturation, caspase-11–deficient mice have
Autor:
Christian Leist, Kim Hoang, Anu Srinivasan, Donald S. Karanewsky, Tam Vu, Lawrence C. Fritz, Robert C. Armstrong, Joe C. Wu, Bryan Pham, Teresa Aja, Rob Sayers, Albert Schmitz, Angela M. Wong, Joseph F. Krebs, Aileen Aboy, Kevin J. Tomaselli
Publikováno v:
The Journal of Cell Biology
The mechanism by which membrane-bound Bcl-2 inhibits the activation of cytoplasmic procaspases is unknown. Here we characterize an intracellular, membrane-associated form of procaspase-3 whose activation is controlled by Bcl-2. Heavy membranes isolat
Autor:
Michael A. Moskowitz, Anu Srinivasan, Klaus Fink, Shobu Namura, Matthias Endres, Kevin J. Tomaselli, Jinmin Zhu, Junying Yuan
Publikováno v:
The Journal of Neuroscience. 18:3659-3668
We examined the expression, activation, and cellular localization of caspase-3 (CPP32) using immunohistochemistry, immunoblots, and cleavage of the fluorogenic substrateN-benzyloxycarbonyl-Asp-Glu-Val-Asp-7-amino-4-trifluoromethyl coumarin (zDEVD-afc