Search Results - "Calvo, Raul R."

Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo by Koblish, Holly K, Zhao, Shuyuan, Franks, Carol F, Donatelli, Robert R, Tominovich, Rose M, LaFrance, Louis V, Leonard, Kristi A, Gushue, Joan M, Parks, Daniel J, Calvo, Raul R, Milkiewicz, Karen L, Marugán, Juan José, Raboisson, Pierre, Cummings, Maxwell D, Grasberger, Bruce L, Johnson, Dana L, Lu, Tianbao, Molloy, Christopher J, Maroney, Anna C

“…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…”
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Discovery and Cocrystal Structure of Benzodiazepinedione HDM2 Antagonists That Activate p53 in Cells by Grasberger, Bruce L, Lu, Tianbao, Schubert, Carsten, Parks, Daniel J, Carver, Theodore E, Koblish, Holly K, Cummings, Maxwell D, LaFrance, Louis V, Milkiewicz, Karen L, Calvo, Raul R, Maguire, Diane, Lattanze, Jennifer, Franks, Carol F, Zhao, Shuyuan, Ramachandren, Kannan, Bylebyl, Gwendolyn R, Zhang, Marie, Manthey, Carl L, Petrella, Eugene C, Pantoliano, Michael W, Deckman, Ingrid C, Spurlino, John C, Maroney, Anna C, Tomczuk, Bruce E, Molloy, Christopher J, Bone, Roger F

“…HDM2 binds to an α-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to…”
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Discovery of vinylcycloalkyl-substituted benzimidazole TRPM8 antagonists effective in the treatment of cold allodynia by Calvo, Raul R., Meegalla, Sanath K., Parks, Daniel J., Parsons, William H., Ballentine, Shelley K., Lubin, Mary Lou, Schneider, Craig, Colburn, Raymond W., Flores, Christopher M., Player, Mark R.

“…Thermosensitive transient receptor potential melastatin 8 (TRPM8) antagonists are considered to be potential therapeutic agents for the treatment of cold…”
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Benzo[d]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans-2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]‑1H‑benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep) by Parsons, William H, Calvo, Raul R, Cheung, Wing, Lee, Yu-Kai, Patel, Sharmila, Liu, Jian, Youngman, Mark A, Dax, Scott L, Stone, Dennis, Qin, Ning, Hutchinson, Tasha, Lubin, Mary Lou, Zhang, Sui-Po, Finley, Michael, Liu, Yi, Brandt, Michael R, Flores, Christopher M, Player, Mark R

“…Reported herein is the design, synthesis, and pharmacologic characterization of a class of TRPV1 antagonists constructed on a benzo­[d]­imidazole platform that…”
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1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2–p53 interaction: discovery and SAR by Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., Gupta, Varsha, Lattanze, Jennifer, Ramachandren, Kannan, Carver, Theodore E., Petrella, Eugene C., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Lu, Tianbao

“…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…”
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Direct design of a potent non-peptide fibrinogen receptor antagonist based on the structure and conformation of a highly constrained cyclic RGD peptide by Ku, Thomas W, Ali, Fadia E, Barton, Linda S, Bean, John W, Bondinell, William E, Burgess, Joelle L, Callahan, James F, Calvo, Raul R, Chen, Lichong

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Enhanced pharmacokinetic properties of 1,4-benzodiazepine-2,5-dione antagonists of the HDM2-p53 protein–protein interaction through structure-based drug design by Parks, Daniel J., LaFrance, Louis V., Calvo, Raul R., Milkiewicz, Karen L., José Marugán, Juan, Raboisson, Pierre, Schubert, Carsten, Koblish, Holly K., Zhao, Shuyuan, Franks, Carol F., Lattanze, Jennifer, Carver, Theodore E., Cummings, Maxwell D., Maguire, Diane, Grasberger, Bruce L., Maroney, Anna C., Lu, Tianbao

“…Guided by structure-based drug design, modification of the BDP lead compound 1 resulted in the discovery of 19, a potent and orally bioavailable antagonist of…”
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Discovery of piperidine carboxamide TRPV1 antagonists by Cheung, Wing S., Calvo, Raul R., Tounge, Brett A., Zhang, Sui-Po, Stone, Dennis R., Brandt, Michael R., Hutchinson, Tasha, Flores, Christopher M., Player, Mark R.

“…A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential receptor vanilloid 1 (TRPV1), an emerging target…”
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Substituted 1,4-Benzodiazepine-2,5-diones as α-Helix Mimetic Antagonists of the HDM2-p53 Protein-Protein Interaction by Cummings, Maxwell D., Schubert, Carsten, Parks, Daniel J., Calvo, Raul R., LaFrance, Louis V., Lattanze, Jennifer, Milkiewicz, Karen L., Lu, Tianbao

“…Small molecule antagonists of protein–protein interactions represent a particular challenge for pharmaceutical discovery. One approach to finding molecules…”
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Discovery of Potent Nonpeptide Vitronectin Receptor (αVβ3) Antagonists by Keenan, Richard M, Miller, William H, Kwon, Chet, Ali, Fadia E, Callahan, James F, Calvo, Raul R, Hwang, Shing-Mei, Kopple, Kenneth D, Peishoff, Catherine E, Samanen, James M, Wong, Angela S, Yuan, Chuan-Kui, Huffman, William F

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Conformational Preferences in a Benzodiazepine Series of Potent Nonpeptide Fibrinogen Receptor Antagonists by Keenan, Richard M, Callahan, James F, Samanen, James M, Bondinell, William E, Calvo, Raul R, Chen, Lichong, DeBrosse, Charles, Eggleston, Drake S, Haltiwanger, R. Curtis, Hwang, Shing Mei, Jakas, Dalia R, Ku, Thomas W, Miller, William H, Newlander, Kenneth A, Nichols, Andrew, Parker, Michael F, Southhall, Linda S, Uzinskas, Irene, Vasko-Moser, Janice A, Venslavsky, Joseph W, Wong, Angela S, Huffman, William F

“…Previously, we reported the direct design of highly potent nonpeptide 3-oxo-1,4-benzodiazepine fibrinogen receptor antagonists from a constrained,…”
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Conformationally Constrained Peptides and Semipeptides Derived from RGD as Potent Inhibitors of the Platelet Fibrinogen Receptor and Platelet Aggregation by Ali, Fadia E, Bennett, Donald B, Calvo, Raul R, Elliott, John D, Hwang, Shing-Mei, Ku, Thomas W, Lago, M. Amparo, Nichols, Andrew J, Romoff, Todd T

“…Structure-activity studies have been pursued on cyclo-S,S-[Ac-Cys-(N alpha-Me)Arg-Gly-Asp-Pen]-NH2, 2 (SK&F 106760), a potent inhibitor of platelet…”
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Enantiospecific synthesis of SB 214857, a potent, orally active, nonpeptide fibrinogen receptor antagonist by Miller, William H., Ku, Thomas W., Ali, Fadia E., Bondinell, William E., Calvo, Raul R., Davis, Larry D., Erhard, Karl F., Hall, Leon B., Huffman, William F., Keenan, Richard M., Kwon, Chet, Newlander, Kenneth A., Ross, Stephen T., Samanen, James M., Takata, Dennis T., Yuan, Chuan-Kui

“…An enantiospecific synthesis of SB 214857, a potent, nonpeplide fibrinogen receptor antagonist, is reported. The synthetic route employs as a key step an…”
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Benzo[ d ]imidazole Transient Receptor Potential Vanilloid 1 Antagonists for the Treatment of Pain: Discovery of trans -2-(2-{2-[2-(4-Trifluoromethyl-phenyl)-vinyl]-1 H -benzimidazol-5-yl}-phenyl)-propan-2-ol (Mavatrep) by Parsons, William H., Calvo, Raul R., Cheung, Wing, Lee, Yu-Kai, Patel, Sharmila, Liu, Jian, Youngman, Mark A., Dax, Scott L., Stone, Dennis, Qin, Ning, Hutchinson, Tasha, Lubin, Mary Lou, Zhang, Sui-Po, Finley, Michael, Liu, Yi, Brandt, Michael R., Flores, Christopher M., Player, Mark R.

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The use of rabbit intestinal permeability as an in vitro assay in the search for orally active GPIIb/IIIa antagonists by Samanen, James M., Lee, Chao-Pin, Smith, Philip L., Bondinell, William E., Calvo, Raul R., Jakas, Dalia R., Newlander, Kenneth A., Parker, Michael, Uzinskas, Irene, Yellin, Tobias O., Nichols, Andrew J.

“…A series of potent, high affinity GPIIb/IIIa antagonists were evaluated for intestinal permeability in vitro using rabbit intestinal strips mounted in the…”
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Angiotensin converting enzyme inhibitors. 10. Aryl sulfonamide substituted N-[1-carboxy-3-phenylpropyl]-L-alanyl-L-proline derivatives as novel antihypertensives by Mencel, James J, Regan, John R, Barton, Jeffrey, Menard, Paul R, Bruno, Joseph G, Calvo, Raul R, Kornberg, Brian E, Schwab, Alfred, Neiss, Edward S, Suh, John T

“…Compounds 1a-g consisting of enalaprilat covalently bonded to aryl sulfonamides, including several known thiazide diuretics, were synthesized and tested for…”
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Discovery of Orally Active Nonpeptide Vitronectin Receptor Antagonists Based on a 2-Benzazepine Gly-Asp Mimetic by Miller, William H, Alberts, Doreen P, Bhatnagar, Pradip K, Bondinell, William E, Callahan, James F, Calvo, Raul R, Cousins, Russell D, Erhard, Karl F, Heerding, Dirk A, Keenan, Richard M, Kwon, Chet, Manley, Peter J, Newlander, Kenneth A, Ross, Stephen T, Samanen, James M, Uzinskas, Irene N, Venslavsky, Joseph W, Yuan, Catherine C.-K, Haltiwanger, R. Curtis, Gowen, Maxine, Hwang, Shing-Mei, James, Ian E, Lark, Michael W, Rieman, David J, Stroup, George B, Azzarano, Leonard M, Salyers, Kevin L, Smith, Brian R, Ward, Keith W, Johanson, Kyung O, Huffman, William F

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Research Article: Substituted 1,4-Benzodiazepine-2,5-diones as alpha -Helix Mimetic Antagonists of the HDM2-p53 Protein-Protein Interaction by Cummings, Maxwell D, Schubert, Carsten, Parks, Daniel J, Calvo, Raul R, LaFrance, Louis V, Lattanze, Jennifer, Milkiewicz, Karen L, Lu, Tianbao

“…Small molecule antagonists of protein-protein interactions represent a particular challenge for pharmaceutical discovery. One approach to finding molecules…”
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Potent, Selective, Orally Active 3-Oxo-1,4-benzodiazepine GPIIb/IIIa Integrin Antagonists by Samanen, James M, Ali, Fadia E, Barton, Linda S, Bondinell, William E, Burgess, Joelle L, Callahan, James F, Calvo, Raul R, Chen, Wenting, Chen, Lichong, Erhard, Karl, Feuerstein, Giora, Heys, Richard, Hwang, Shing-Mei, Jakas, Dalia R, Keenan, Richard M, Ku, Thomas W, Kwon, Chet, Lee, Chao-Pin, Miller, William H, Newlander, Kenneth A, Nichols, Andrew, Parker, Michael, Peishoff, Catherine E, Rhodes, Gerald, Ross, Steven, Shu, Arthur, Simpson, Richard, Takata, Dennis, Yellin, Tobias O, Uzsinskas, Irene, Venslavsky, Joseph W, Yuan, Chuan-Kui, Huffman, William F

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Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (αvβ3) antagonists by Keenan, Richard M., Miller, William H., Lago, M.Amparo, Ali, Fadia E., Bondinell, William E., Callahan, James F., Calvo, Raul R., Cousins, Russell D., Hwang, Shing-Mei, Jakas, Dalia R., Ku, Thomas W., Kwon, Chet, Nguyen, Thomas T., Reader, Valerie A., Rieman, David J., Ross, Steven T., Takata, Dennis T., Uzinskas, Irene N., Yuan, Catherine C.K., Smith, Brian R.

“…In a 3-oxo-1,4-benzodiazepine-2-acetic acid series of vitronectin receptor (αvβ3) antagonists containing a benzimidazole as a novel arginine mimetic, we…”
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