Search Results - "Marugan, Juan Jose"

Agonist-specific voltage-dependent gating of lysosomal two-pore Na + channels by Zhang, Xiaoli, Chen, Wei, Li, Ping, Calvo, Raul, Southall, Noel, Hu, Xin, Bryant-Genevier, Melanie, Feng, Xinghua, Geng, Qi, Gao, Chenlang, Yang, Meimei, Tang, Kaiyuan, Ferrer, Marc, Marugan, Juan Jose, Xu, Haoxing

“…Mammalian two-pore-channels (TPC1, 2; ) are ubiquitously- expressed, PI(3,5)P -activated, Na -selective channels in the endosomes and lysosomes that regulate…”
Get full text

Inhibition of PIP4Kγ ameliorates the pathological effects of mutant huntingtin protein by Al-Ramahi, Ismael, Giridharan, Sai Srinivas Panapakkam, Chen, Yu-Chi, Patnaik, Samarjit, Safren, Nathaniel, Hasegawa, Junya, de Haro, Maria, Wagner Gee, Amanda K, Titus, Steven A, Jeong, Hyunkyung, Clarke, Jonathan, Krainc, Dimitri, Zheng, Wei, Irvine, Robin F, Barmada, Sami, Ferrer, Marc, Southall, Noel, Weisman, Lois S, Botas, Juan, Marugan, Juan Jose

“…The discovery of the causative gene for Huntington's disease (HD) has promoted numerous efforts to uncover cellular pathways that lower levels of mutant…”
Get full text

Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites by Dorjsuren, Dorjbal, Eastman, Richard T., Wicht, Kathryn J., Jansen, Daniel, Talley, Daniel C., Sigmon, Benjamin A., Zakharov, Alexey V., Roncal, Norma, Girvin, Andrew T., Antonova-Koch, Yevgeniya, Will, Paul M., Shah, Pranav, Sun, Hongmao, Klumpp-Thomas, Carleen, Mok, Sachel, Yeo, Tomas, Meister, Stephan, Marugan, Juan Jose, Ross, Leila S., Xu, Xin, Maloney, David J., Jadhav, Ajit, Mott, Bryan T., Sciotti, Richard J., Winzeler, Elizabeth A., Waters, Norman C., Campbell, Robert F., Huang, Wenwei, Simeonov, Anton, Fidock, David A.

“…The spread of Plasmodium falciparum parasites resistant to most first-line antimalarials creates an imperative to enrich the drug discovery pipeline,…”
Get full text

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…”
Get full text

Probing the hydrophobic pocket of farnesyltransferase : Aromatic substitution of CAAX peptidomimetics leads to highly potent inhibitors by YIMIN QIAN, MARUGAN, J. J, FOSSUM, R. D, VOGT, A, SEBTI, S. M, HAMILTON, A. D

“…Cysteine farnesylation at the carboxylate terminal tetrapeptide CAAX of Ras protein is catalyzed by farnesyltransferase. This lipid modification is necessary…”
Get full text

Identification, design and synthesis of novel pyrazolopyridine influenza virus nonstructural protein 1 antagonists by Patnaik, Samarjit, Basu, Dipanwita, Southall, Noel, Dehdashti, Seameen, Wan, Kanny K., Zheng, Wei, Ferrer, Marc, Taylor, Mercedes, Engel, Daniel A., Marugan, Juan Jose

“…Novel pyrazolopyridine NS1-antagonists for influenza A. Reduces viral titer by 128-fold at 10 μM. Inhibits cytopathic effects of a seasonal influenza A strain…”
Get full text

Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis by Frankowski, Kevin J, Wang, Chen, Patnaik, Samarjit, Schoenen, Frank J, Southall, Noel, Li, Dandan, Teper, Yaroslav, Sun, Wei, Kandela, Irawati, Hu, Deqing, Dextras, Christopher, Knotts, Zachary, Bian, Yansong, Norton, John, Titus, Steve, Lewandowska, Marzena A, Wen, Yiping, Farley, Katherine I, Griner, Lesley Mathews, Sultan, Jamey, Meng, Zhaojing, Zhou, Ming, Vilimas, Tomas, Powers, Astin S, Kozlov, Serguei, Nagashima, Kunio, Quadri, Humair S, Fang, Min, Long, Charles, Khanolkar, Ojus, Chen, Warren, Kang, Jinsol, Huang, Helen, Chow, Eric, Goldberg, Esthermanya, Feldman, Coral, Xi, Romi, Kim, Hye Rim, Sahagian, Gary, Baserga, Susan J, Mazar, Andrew, Ferrer, Marc, Zheng, Wei, Shilatifard, Ali, Aubé, Jeffrey, Rudloff, Udo, Marugan, Juan Jose, Huang, Sui

“…Metastasis remains a leading cause of cancer mortality due to the lack of specific inhibitors against this complex process. To identify compounds selectively…”
Get more information

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…”
Get full text

Agonist-specific voltage-dependent gating of lysosomal two-pore Na.sup.+ channels by Zhang, Xiaoli, Chen, Wei, Li, Ping, Calvo, Raul, Southall, Noel, Hu, Xin, Bryant-Genevier, Melanie, Feng, Xinghua, Geng, Qi, Gao, Chenlang, Yang, Meimei, Tang, Kaiyuan, Ferrer, Marc, Marugan, Juan Jose, Xu, Haoxing

“…Mammalian two-pore-channels (TPC1, 2; TPCN1, TPCN2) are ubiquitously- expressed, PI(3,5)P.sub.2-activated, Na.sup.+-selective channels in the endosomes and…”
Get full text

Identification of novel short chain 4-substituted indoles as potent αvβ3 antagonist using structure-based drug design by RABOISSON, Pierre, DESJARLAIS, Renee L, REED, Rolanda, LATTANZE, Jennifer, CHAIKIN, Margery, MANTHEY, Carl L, TOMCZUK, Bruce E, MARUGAN, Juan José

Get full text

Abstract 5368: Metarrestin effectively disassembles PNCs and inhibits metastasis by Wang, Chen, Frankowski, Kevin, Yaroslav, Teper, Patnaik, Samarjit, Schoenen, Frank, Southall, Noel, Sun, Wei, Titus, Steve, Griner, Lesley, Dextras, Christopher, Sultan, Jamey, Kandela, Irawati, Lewandowska, Marzena, Wen, Yi-Ping, Norton, John, Kang, Jin Sol, Mazar, Andrew, Zhang, Wei, Aubé, Jeffrey, Ferrer, Marc, Rudloff, Udo, Marugan, Juan Jose, Huang, Sui

“…The perinucleolar compartment (PNC) is a nuclear body that forms specifically in highly malignant cancer cells. PNC prevalence is shown to reflect metastatic…”
Get full text

Structure-based design, synthesis, and biological evaluation of novel 1,4-diazepines as HDM2 antagonists by Raboisson, Pierre, Marugán, Juan José, Schubert, Carsten, Koblish, Holly K., Lu, Tianbao, Zhao, Shuyuan, Player, Mark R., Maroney, Anna C., Reed, Rolanda L., Huebert, Norman D., Lattanze, Jennifer, Parks, Daniel J., Cummings, Maxwell D.

“…Novel 1,4-diazepine-2,5-diones that act as antagonists of the HDM2–p53 interaction are reported. Crystallographic analysis of ligands bound to HDM2 suggested…”
Get full text

Novel 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists with improved cellular activity by Leonard, Kristi, Marugan, Juan Jose, Raboisson, Pierre, Calvo, Raul, Gushue, Joan M., Koblish, Holly K., Lattanze, Jennifer, Zhao, Shuyuan, Cummings, Maxwell D., Player, Mark R., Maroney, Anna C., Lu, Tianbao

“…The disruption of the p53-Hdm2 protein–protein interaction induces cell growth arrest and apoptosis. We have identified the 1,4-benzodiazepine-2,5-dione…”
Get full text

A novel series of arylsulfonylthiophene-2-carboxamidine inhibitors of the complement component C1s by Subasinghe, Nalin L., Travins, Jeremy M., Ali, Farah, Huang, Hui, Ballentine, Shelley K., Marugán, Juan José, Khalil, Ehab, Hufnagel, Heather R., Bone, Roger F., DesJarlais, Renee L., Crysler, Carl S., Ninan, Nisha, Cummings, Maxwell D., Molloy, Christopher J., Tomczuk, Bruce E.

“…Inhibiting the classical pathway of complement activation by attenuating the proteolytic activity of the serine protease C1s is a potential strategy for the…”
Get full text

Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists by Marugan, Juan Jose, Leonard, Kristi, Raboisson, Pierre, Gushue, Joan M., Calvo, Raul, Koblish, Holly K., Lattanze, Jennifer, Zhao, Shuyuan, Cummings, Maxwell D., Player, Mark R., Schubert, Carsten, Maroney, Anna C., Lu, Tianbao

“…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…”
Get full text

Design, synthesis, and biochemical evaluation of novel α vβ 3 integrin ligands by Marugan, Juan Jose, Haslow, Kristin D, Crysler, Carl

“…Synthesis and activity of oxyguanidine–indoles as α vβ 3 ligands is reported. Studies on integrin α vβ 3 have implicated this receptor in a number of…”
Get full text

Pharmacokinetics of TDP223206 following intravenous and oral administration to intact rats and intravenous administration to bile duct-cannulated rats by Chen, Yanmin, Cheng, Deping, Marugan, Juan Jose, Manthey, Carl, Tomczuk, Bruce, Huebert, Norman

“…The pharmacokinetics of TDP223206 was studied following single intravenous and oral administrations in rats. A mixture of TDP223206 and 14C‐TDP223206 were…”
Get full text

Design, Synthesis, and Biological Evaluation of Novel Potent and Selective αvβ3/αvβ5 Integrin Dual Inhibitors with Improved Bioavailability. Selection of the Molecular Core by Marugán, Juan José, Manthey, Carl, Anaclerio, Beth, Lafrance, Lou, Lu, Tianbao, Markotan, Tom, Leonard, Kristi A, Crysler, Carl, Eisennagel, Stephen, Dasgupta, Malini, Tomczuk, Bruce

“…A novel series of potent and selective αvβ3/αvβ5 dualinhibitors was designed, synthesized, and evaluated against several integrins. These compounds were…”
Get full text

Non-peptidic αvβ3 antagonists containing indol-1-yl propionic acids by Leonard, Kristi, Pan, Wenxi, Anaclerio, Beth, Gushue, Joan M., Guo, Zihong, DesJarlais, Renee L., Chaikin, Marge A., Lattanze, Jennifer, Crysler, Carl, Manthey, Carl L., Tomczuk, Bruce E., Marugan, Juan Jose

“…[Display omitted] We describe the synthesis and structure/activity relationship of RGD mimetics that are potent inhibitors of the integrin αvβ3. Indol-1-yl…”
Get full text

Design, synthesis, and biochemical evaluation of novel αvβ3 integrin ligands by MARUGAN, Juan Jose, HASLOW, Kristin D, CRYSLER, Carl

Get full text