Zobrazeno 1 - 10
of 40
pro vyhledávání: '"Raul R. Calvo"'
Autor:
Ashley Nilson, John Hanson, Andres E. Dulcey, Xin Wen, R. Benjamin Free, Raul R. Calvo, Juan J. Marugan, David R. Sibley
Publikováno v:
ASPET 2023 Annual Meeting Abstract - Cellular and Molecular Pharmacology.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::20ac024d7f87744fa2653714e46493a3
https://doi.org/10.1124/jpet.122.194840
https://doi.org/10.1124/jpet.122.194840
Autor:
Shelley K. Ballentine, Mark R. Player, Mary Lou Lubin, Raul R. Calvo, Craig R. Schneider, William H. Parsons, Raymond W. Colburn, Parks Daniel J, Sanath K. Meegalla, Christopher M. Flores
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1903-1907
Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold hypersensitivity. The discovery of a new class of TRPM8 antagonists that shows in vivo efficacy
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::25903ed835bb308ef0a94c28d67b4c5e
https://doi.org/10.1016/j.bmcl.2012.01.060
https://doi.org/10.1016/j.bmcl.2012.01.060
Autor:
Maxwell D. Cummings, Tianbao Lu, Jennifer Lattanze, Juan J. Marugan, Carsten Schubert, Joan Gushue, Holly K. Koblish, Shuyuan Zhao, Kristi A. Leonard, Mark R. Player, Anna C. Maroney, Pierre Raboisson, Raul R. Calvo
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:3115-3120
The 1,4-benzodiazepine-2,5-dione is a suitable template to disrupt the interaction between p53 and Hdm2. The development of an enantioselective synthesis disclosed the stereochemistry of the active enantiomer. An in vitro p53 peptide displacement ass
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::739d721ccb6bdb9dc10b824f6569f129
https://doi.org/10.1016/j.bmcl.2006.03.067
https://doi.org/10.1016/j.bmcl.2006.03.067
Autor:
Pierre Raboisson, Raul R. Calvo, Rose Tominovich, Louis V. LaFrance, Karen L. Milkiewicz, Dana L. Johnson, Anna C. Maroney, Shuyuan Zhao, Robert R. Donatelli, Maxwell D. Cummings, Bruce L. Grasberger, Christopher J. Molloy, Tianbao Lu, Juan J. Marugan, Daniel J. Parks, Kristi A. Leonard, Carol F. Franks, Joan Gushue, Holly K. Koblish
Publikováno v:
Molecular Cancer Therapeutics. 5:160-169
The activity and stability of the p53 tumor suppressor are regulated by the human homologue of the mouse double minute 2 (Hdm2) oncoprotein. It has been hypothesized that small molecules disrupting the Hdm2:p53 complex would allow for the activation
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::30835600d455b26ccf94cf87ed7132f4
https://doi.org/10.1158/1535-7163.mct-05-0199
https://doi.org/10.1158/1535-7163.mct-05-0199
Autor:
Jennifer Lattanze, Tianbao Lu, Karen L. Milkiewicz, Bruce L. Grasberger, Theodore E. Carver, Louis V. LaFrance, Daniel J. Parks, Kannan Ramachandren, Varsha Gupta, Raul R. Calvo, Diane M. Maguire, Eugene C. Petrella, Maxwell D. Cummings
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:765-770
A library of 1,4-benzodiazepine-2,5-diones was screened for binding to the p53-binding domain of HDM2 using Thermofluor ® , a miniaturized thermal denaturation assay. The hits obtained were shown to bind to HDM2 in the p53-binding pocket using a flu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eed49474f88d1fb7a63d4bf5e23b6ee3
https://doi.org/10.1016/j.bmcl.2004.11.009
https://doi.org/10.1016/j.bmcl.2004.11.009
Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells
Autor:
Tianbao Lu, Jennifer Lattanze, Ingrid Deckman, Marie Zhang, Bruce L. Grasberger, Carl L. Manthey, and Christopher J. Molloy, John C. Spurlino, Diane M. Maguire, Eugene C. Petrella, Kannan Ramachandren, Holly K. Koblish, Shuyuan Zhao, Bruce E. Tomczuk, Gwendolyn R. Bylebyl, Louis V. LaFrance, Carsten Schubert, Daniel J. Parks, Karen L. Milkiewicz, Carol F. Franks, Theodore E. Carver, Roger F. Bone, Anna C. Maroney, Maxwell D. Cummings, Raul R. Calvo, W. Michael Avondale Pantoliano
Publikováno v:
Journal of Medicinal Chemistry. 48:909-912
HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepined
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9ad2c720d92aeda8d7b96e67eadcedf4
https://doi.org/10.1021/jm049137g
https://doi.org/10.1021/jm049137g
Autor:
Irene N. Uzinskas, Kyung O. Johanson, William F. Huffman, R. D. Cousins, William E. Bondinell, Stephen T. Ross, M.W. Lark, Keith W. Ward, Chuan-Kui Yuan, Kevin L. Salyers, Dirk A. Heerding, S M Hwang, Joseph W. Venslavsky, J. Samanen, Karl F. Erhard, Raul R. Calvo, M. Gowen, Pradip K. Bhatnagar, James F. Callahan, Manley Peter J, Doreen Alberts, Brian R. Smith, Kenneth A. Newlander, W.H. Miller, R. C. Haltiwanger, Richard M. Keenan, George B. Stroup, David J. Rieman, Chet Kwon, Leonard M. Azzarano, Ian E. James
Publikováno v:
Journal of Medicinal Chemistry. 43:22-26
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::921ed25c145b5edbd1b8a614916fc7cc
https://doi.org/10.1021/jm990446u
https://doi.org/10.1021/jm990446u
Autor:
Thomas W. Ku, Dalia R. Jakas, William H. Miller, Valerie A. Reader, James F. Callahan, Catherine C.K. Yuan, Brian R. Smith, Dennis T. Takata, Raul R. Calvo, Thomas T. Nguyen, Bondinell William E, Fadia E. Ali, Russell D. Cousins, S M Hwang, Chet Kwon, Steven T. Ross, Irene N. Uzinskas, David J. Rieman, M. Amparo Lago, Richard M. Keenan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 8:3165-3170
In a 3-oxo-1,4-benzodiazepine-2-acetic acid series of vitronectin receptor (alpha v beta 3) antagonists containing a benzimidazole as a novel arginine mimetic, we examined the effects of benzimidazole modifications and amide substitutions on both act
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::08fa8760f29ac2a671d601214e0654b9
https://doi.org/10.1016/s0960-894x(98)00555-1
https://doi.org/10.1016/s0960-894x(98)00555-1
Autor:
James F. Callahan, Fadia E. Ali, S M Hwang, Catherine E. Peishoff, Chuan-Kui Yuan, Chet Kwon, Angela S. Wong, Kenneth D. Kopple, Richard M. Keenan, William F. Huffman, Raul R. Calvo, James Samanen, William H. Miller
Publikováno v:
Journal of Medicinal Chemistry. 40:2289-2292
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::55a449785e2ab209401f4c2b15ab7c84
https://doi.org/10.1021/jm970205r
https://doi.org/10.1021/jm970205r
Autor:
Philip L. Smith, Andrew J. Nichols, Tobias Oregon Yellin, Kenneth A. Newlander, Raul R. Calvo, James Samanen, Irene N. Uzinskas, Bondinell William E, Chao-Pin Lee, Michael W. Parker, Dalia R. Jakas
Publikováno v:
Advanced Drug Delivery Reviews. 23:133-142
A series of potent, high affinity GPIIb/IIIa antagonists were evaluated for intestinal permeability in vitro using rabbit intestinal strips mounted in the Ussing Chamber. In this series of compounds, structural modifications were found to impact inte
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::350bdbddf76768ec56b4c8776c870467
https://doi.org/10.1016/s0169-409x(96)00431-0
https://doi.org/10.1016/s0169-409x(96)00431-0