Discovery of Thieno[3,2‑d]pyrimidine-6-carboxamides as Potent Inhibitors of SIRT1, SIRT2, and SIRT3
Disch, Jeremy S, Evindar, Ghotas, Chiu, Cynthia H, Blum, Charles A, Dai, Han, Jin, Lei, Schuman, Eli, Lind, Kenneth E, Belyanskaya, Svetlana L, Deng, Jianghe, Coppo, Frank, Aquilani, Leah, Graybill, Todd L, Cuozzo, John W, Lavu, Siva, Mao, Cheney, Vlasuk, George P, Perni, Robert B
Published in Journal of medicinal chemistry (09.05.2013)
Published in Journal of medicinal chemistry (09.05.2013)
Get full text
Journal Article
Discovery of oxazolo[4,5- b]pyridines and related heterocyclic analogs as novel SIRT1 activators
Bemis, Jean E., Vu, Chi B., Xie, Roger, Nunes, Joseph J., Ng, Pui Yee, Disch, Jeremy S., Milne, Jill C., Carney, David P., Lynch, Amy V., Jin, Lei, Smith, Jesse J., Lavu, Siva, Iffland, Andre, Jirousek, Michael R., Perni, Robert B.
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Published in Bioorganic & medicinal chemistry letters (15.04.2009)
Get full text
Journal Article
Bispecific Estrogen Receptor α Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening
Disch, Jeremy S, Duffy, Jennifer M, Lee, Esther C. Y, Gikunju, Diana, Chan, Betty, Levin, Benjamin, Monteiro, Michael I, Talcott, Sarah A, Lau, Anthony C, Zhou, Fei, Kozhushnyan, Anton, Westlund, Neil E, Mullins, Patrick B, Yu, Yan, von Rechenberg, Moritz, Zhang, Junyi, Arnautova, Yelena A, Liu, Yanbin, Zhang, Ying, McRiner, Andrew J, Keefe, Anthony D, Kohlmann, Anna, Clark, Matthew A, Cuozzo, John W, Huguet, Christelle, Arora, Shilpi
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
Get full text
Journal Article
Evidence for a Common Mechanism of SIRT1 Regulation by Allosteric Activators
Hubbard, Basil P., Gomes, Ana P., Dai, Han, Li, Jun, Case, April W., Considine, Thomas, Riera, Thomas V., Lee, Jessica E., Yen E, Sook, Lamming, Dudley W., Pentelute, Bradley L., Schuman, Eli R., Stevens, Linda A., Ling, Alvin J. Y., Armour, Sean M., Michan, Shaday, Zhao, Huizhen, Jiang, Yong, Sweitzer, Sharon M., Blum, Charles A., Disch, Jeremy S., Ng, Pui Yee, Howitz, Konrad T., Rolo, Anabela P., Hamuro, Yoshitomo, Moss, Joel, Perni, Robert B., Ellis, James L., Vlasuk, George P., Sinclair, David A.
Published in Science (American Association for the Advancement of Science) (08.03.2013)
Published in Science (American Association for the Advancement of Science) (08.03.2013)
Get full text
Journal Article
Discovery of Nanomolar DCAF1 Small Molecule Ligands
Li, Alice Shi Ming, Kimani, Serah, Wilson, Brian, Noureldin, Mahmoud, González-Álvarez, Héctor, Mamai, Ahmed, Hoffer, Laurent, Guilinger, John P., Zhang, Ying, von Rechenberg, Moritz, Disch, Jeremy S., Mulhern, Christopher J., Slakman, Belinda L., Cuozzo, John W., Dong, Aiping, Poda, Gennady, Mohammed, Mohammed, Saraon, Punit, Mittal, Manish, Modh, Pratik, Rathod, Vaibhavi, Patel, Bhashant, Ackloo, Suzanne, Santhakumar, Vijayaratnam, Szewczyk, Magdalena M, Barsyte-Lovejoy, Dalia, Arrowsmith, Cheryl H., Marcellus, Richard, Guié, Marie-Aude, Keefe, Anthony D., Brown, Peter J., Halabelian, Levon, Al-awar, Rima, Vedadi, Masoud
Published in Journal of medicinal chemistry (13.04.2023)
Published in Journal of medicinal chemistry (13.04.2023)
Get full text
Journal Article
Crystallographic structure of a small molecule SIRT1 activator-enzyme complex
Dai, Han, Case, April W., Riera, Thomas V., Considine, Thomas, Lee, Jessica E., Hamuro, Yoshitomo, Zhao, Huizhen, Jiang, Yong, Sweitzer, Sharon M., Pietrak, Beth, Schwartz, Benjamin, Blum, Charles A., Disch, Jeremy S., Caldwell, Richard, Szczepankiewicz, Bruce, Oalmann, Christopher, Yee Ng, Pui, White, Brian H., Casaubon, Rebecca, Narayan, Radha, Koppetsch, Karsten, Bourbonais, Francis, Wu, Bo, Wang, Junfeng, Qian, Dongming, Jiang, Fan, Mao, Cheney, Wang, Minghui, Hu, Erding, Wu, Joe C., Perni, Robert B., Vlasuk, George P., Ellis, James L.
Published in Nature communications (02.07.2015)
Published in Nature communications (02.07.2015)
Get full text
Journal Article
Discovery of a selective c-MET inhibitor with a novel binding mode
Collie, Gavin W., Barlind, Louise, Bazzaz, Sana, Börjesson, Ulf, Dale, Ian L., Disch, Jeremy S., Habeshian, Sevan, Jetson, Rachael, Khurana, Puneet, Madin, Andrew, Michaelides, Iacovos N., Peng, Ling, Snijder, Arjan, Stubbs, Christopher J.
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
Published in Bioorganic & medicinal chemistry letters (01.11.2022)
Get full text
Journal Article
Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes
Choy, Wendy, Sinclair, David A, Lambert, Philip D, Gagne, David J, Lynch, Amy V, Milne, Jill C, Bemis, Jean E, Boss, Olivier, Perni, Robert B, Schenk, Simon, Carney, David P, Yang, Hongying, Ng, Pui Yee, Iffland, Andre, Smith, Jesse J, Elliott, Peter J, Vu, Chi B, Xie, Roger, Galonek, Heidi, Israelian, Kristine, Lavu, Siva, Medvedik, Oliver, Olefsky, Jerrold M, Disch, Jeremy S, Nunes, Joseph J, Jirousek, Michael R, Westphal, Christoph H, Jin, Lei
Published in Nature (29.11.2007)
Published in Nature (29.11.2007)
Get full text
Journal Article
A Target Class Ligandability Evaluation of WD40 Repeat-Containing Proteins
Ackloo, Suzanne, Li, Fengling, Szewczyk, Magda, Seitova, Almagul, Loppnau, Peter, Zeng, Hong, Xu, Jin, Ahmad, Shabbir, Arnautova, Yelena A, Baghaie, A J, Beldar, Serap, Bolotokova, Albina, Centrella, Paolo A, Chau, Irene, Clark, Matthew A, Cuozzo, John W, Dehghani-Tafti, Saba, Disch, Jeremy S, Dong, Aiping, Dumas, Antoine, Feng, Jianwen A, Ghiabi, Pegah, Gibson, Elisa, Gilmer, Justin, Goldman, Brian, Green, Stuart R, Guié, Marie-Aude, Guilinger, John P, Harms, Nathan, Herasymenko, Oleksandra, Houliston, Scott, Hutchinson, Ashley, Kearnes, Steven, Keefe, Anthony D, Kimani, Serah W, Kramer, Trevor, Kutera, Maria, Kwak, Haejin A, Lento, Cristina, Li, Yanjun, Liu, Jenny, Loup, Joachim, Machado, Raquel A C, Mulhern, Christopher J, Perveen, Sumera, Righetto, Germanna L, Riley, Patrick, Shrestha, Suman, Sigel, Eric A, Silva, Madhushika, Sintchak, Michael D, Slakman, Belinda L, Taylor, Rhys D, Thompson, James, Torng, Wen, Underkoffler, Carl, von Rechenberg, Moritz, Walsh, Ryan T, Watson, Ian, Wilson, Derek J, Wolf, Esther, Yadav, Manisha, Yazdi, Aliakbar K, Zhang, Junyi, Zhang, Ying, Santhakumar, Vijayaratnam, Edwards, Aled M, Barsyte-Lovejoy, Dalia, Schapira, Matthieu, Brown, Peter J, Halabelian, Levon, Arrowsmith, Cheryl H
Published in Journal of medicinal chemistry (04.11.2024)
Published in Journal of medicinal chemistry (04.11.2024)
Get full text
Journal Article
Generating Selective Leads for Mer Kinase InhibitorsExample of a Comprehensive Lead-Generation Strategy
Nissink, J. Willem M, Bazzaz, Sana, Blackett, Carolyn, Clark, Matthew A, Collingwood, Olga, Disch, Jeremy S, Gikunju, Diana, Goldberg, Kristin, Guilinger, John P, Hardaker, Elizabeth, Hennessy, Edward J, Jetson, Rachael, Keefe, Anthony D, McCoull, William, McMurray, Lindsay, Olszewski, Allison, Overman, Ross, Pflug, Alexander, Preston, Marian, Rawlins, Philip B, Rivers, Emma, Schimpl, Marianne, Smith, Paul, Truman, Caroline, Underwood, Elizabeth, Warwicker, Juli, Winter-Holt, Jon, Woodcock, Simon, Zhang, Ying
Published in Journal of medicinal chemistry (25.03.2021)
Published in Journal of medicinal chemistry (25.03.2021)
Get full text
Journal Article
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds
Ramos, Ashley L., Goedken, Eric R., Frank, Kristine E., Argiriadi, Maria A., Bazzaz, Sana, Bian, Zhiguo, Brown, Jesse T. C., Centrella, Paolo A., Chen, Hui-Ju, Disch, Jeremy S., Donner, Pamela L., Duignan, David B., Gikunju, Diana, Greszler, Stephen N., Guié, Marie-Aude, Habeshian, Sevan, Hartl, Hajnalka E., Hein, Christopher D., Hutchins, Charles W., Jetson, Rachael, Keefe, Anthony D., Khan, Hasan, Li, Huan-Qiu, Olszewski, Allison, Ortiz Cardona, Benjamin J., Osuma, Augustine, Panchal, Sanjay C., Phelan, Ryan, Qiu, Wei, Shotwell, J. Brad, Shrestha, Anurupa, Srikumaran, Myron, Su, Zhi, Sun, Chaohong, Upadhyay, Anup K., Wood, Michael D., Wu, Haihong, Zhang, Ruijie, Zhang, Ying, Zhao, Gang, Zhu, Haizhong, Webster, Matthew P.
Published in Journal of medicinal chemistry (25.04.2024)
Published in Journal of medicinal chemistry (25.04.2024)
Get full text
Journal Article
Discovery of Imidazo[1,2-b]thiazole Derivatives as Novel SIRT1 Activators
Vu, Chi B, Bemis, Jean E, Disch, Jeremy S, Ng, Pui Yee, Nunes, Joseph J, Milne, Jill C, Carney, David P, Lynch, Amy V, Smith, Jesse J, Lavu, Siva, Lambert, Philip D, Gagne, David J, Jirousek, Michael R, Schenk, Simon, Olefsky, Jerrold M, Perni, Robert B
Published in Journal of medicinal chemistry (12.03.2009)
Published in Journal of medicinal chemistry (12.03.2009)
Get full text
Journal Article
Carboxamide SIRT1 inhibitors block DBC1 binding via an acetylation-independent mechanism
Hubbard, Basil P, Loh, Christine, Gomes, Ana P, Li, Jun, Lu, Quinn, Doyle, Taylor LG, Disch, Jeremy S, Armour, Sean M, Ellis, James L, Vlasuk, George P, Sinclair, David A
Published in Cell cycle (Georgetown, Tex.) (15.07.2013)
Published in Cell cycle (Georgetown, Tex.) (15.07.2013)
Get full text
Journal Article
Bispecific Estrogen Receptor a Degraders Incorporating Novel Binders Identified Using DNA-Encoded Chemical Library Screening
Disch, Jeremy S., Duffy, Jennifer M., Lee, Esther C. Y., Gikunju, Diana, Chan, Betty, Levin, Benjamin, Monteiro, Michael, Talcott, Sarah A., Lau, Anthony C., Zhou, Fei, Kozhushnyan, Anton, Westlund, Neil E., Mullins, Patrick B., Yu, Yan, von Rechenberg, Moritz, Zhang, Junyi, Arnautova, Yelena A., Liu, Yanbin, Zhang, Ying, McRiner, Andrew J., Keefe, Anthony D., Kohlmann, Anna, Clark, Matthew A., Cuozzo, John W., Huguet, Christelle, Arora, Shilpi
Published in Journal of medicinal chemistry (22.04.2021)
Published in Journal of medicinal chemistry (22.04.2021)
Get full text
Journal Article
SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
CASAUBON REBECCA, KOPPETSCH KARSTEN, SZCZEPANKIEWICZ BRUCE G, CALDWELL RICHARD DANA, OALMANN CHRISTOPHER, BLUM CHARLES A, DISCH JEREMY S, NG PUI YEE, MILLER WILLIAM HENRY, FOX RYAN MICHAEL, PERNI ROBERT B, WHITE BRIAN H
Year of Publication 19.07.2017
Get full text
Year of Publication 19.07.2017
Patent
BENZIMIDAZOLE AS SIRTUIN REGULATOR AND RELATED ANALOG
VU CHI B, DISCH JEREMY S, NG PUI YEE, CHARLES A BLUM, PERNIE ROBERT B
Year of Publication 19.03.2015
Get full text
Year of Publication 19.03.2015
Patent
SUBSTITUTED BRIDGED UREA ANALOGS AS SIRTUIN MODULATORS
CASAUBON REBECCA, KOPPETSCH KARSTEN, SZCZEPANKIEWICZ BRUCE G, CALDWELL RICHARD DANA, OALMANN CHRISTOPHER, BLUM CHARLES A, DISCH JEREMY S, NG PUI YEE, PERNI ROBERT B, FOX RYAN MICHAEL, WHITE BRIAN H
Year of Publication 18.01.2016
Get full text
Year of Publication 18.01.2016
Patent