Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Jeremy S. Disch"'
Autor:
Alice Shi Ming Li, Serah Kimani, Brian Wilson, Mahmoud Noureldin, Héctor González-Álvarez, Ahmed Mamai, Laurent Hoffer, John P. Guilinger, Ying Zhang, Moritz von Rechenberg, Jeremy S. Disch, Christopher J. Mulhern, Belinda L. Slakman, John W. Cuozzo, Aiping Dong, Gennady Poda, Mohammed Mohammed, Punit Saraon, Manish Mittal, Pratik Modh, Vaibhavi Rathod, Bhashant Patel, Suzanne Ackloo, Vijayaratnam Santhakumar, Magdalena M Szewczyk, Dalia Barsyte-Lovejoy, Cheryl H. Arrowsmith, Richard Marcellus, Marie-Aude Guié, Anthony D. Keefe, Peter J. Brown, Levon Halabelian, Rima Al-awar, Masoud Vedadi
Publikováno v:
Journal of Medicinal Chemistry. 66:5041-5060
Autor:
Anthony D. Keefe, Jeremy S. Disch, Jennifer Duffy, Esther C. Lee, Diana Gikunju, Betty Chan, Benjamin D. Levin, Michael I. Monteiro, Sarah A. Talcott, Anthony Lau, Fei Zhou, Anton Kozhushnyan, Neil E. Westlund, Patrick B. Mullins, Yan Yu, Moritz von Rechenberg, Junyi Zhang, Yelena Arnautova, Yanbin Liu, Ying Zhang, Andrew J. McRiner, Anna Kohlmann, Matthew A. Clark, John W. Cuozzo, Christelle Huguet, Shilpi Arora
Publikováno v:
Cancer Research. 83:5346-5346
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast cancer. Information from DNA-encoded chemical library screening provides a me
Autor:
Diana Gikunju, John W. Cuozzo, Yelena A Arnautova, Sarah A Talcott, Neil Westlund, Andrew J. McRiner, Anthony D. Keefe, Yan Yu, Christelle Huguet, Moritz von Rechenberg, Fei Zhou, Jennifer M Duffy, Shilpi Arora, Esther C.Y. Lee, Ying Zhang, Benjamin Levin, Matthew A. Clark, Jeremy S. Disch, Junyi Zhang, Yanbin Liu, Anton Kozhushnyan, Betty Chan, Anthony C Lau, Michael I Monteiro, Patrick B. Mullins, Anna Kohlmann
Publikováno v:
Journal of Medicinal Chemistry. 64:5049-5066
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast cancer. Information from DNA-encoded chemical library (DECL) screening provid
Autor:
Gavin W. Collie, Louise Barlind, Sana Bazzaz, Ulf Börjesson, Ian L. Dale, Jeremy S. Disch, Sevan Habeshian, Rachael Jetson, Puneet Khurana, Andrew Madin, Iacovos N. Michaelides, Ling Peng, Arjan Snijder, Christopher J. Stubbs
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 75:128948
The c-MET receptor tyrosine kinase has received considerable attention as a cancer drug target yet there remains a need for inhibitors which are selective for c-MET and able to target emerging drug-resistant mutants. We report here the discovery, by
Autor:
Ross Overman, Juli Warwicker, Kristin Goldberg, Alexander Pflug, Jeremy S. Disch, Allison Olszewski, Philip B. Rawlins, John P. Guilinger, William McCoull, Rachael Jetson, Anthony D. Keefe, Simon A. Woodcock, Emma Rivers, Olga Collingwood, Elizabeth Hardaker, Sana Bazzaz, Elizabeth Underwood, Marianne Schimpl, J. Willem M. Nissink, Lindsay McMurray, Carolyn Blackett, Diana Gikunju, Jon Winter-Holt, Edward J. Hennessy, Paul D. Smith, Marian Preston, Caroline Truman, Matthew A. Clark, Ying Zhang
Publikováno v:
Journal of medicinal chemistry. 64(6)
Mer is a member of the TAM (Tyro3, Axl, Mer) kinase family that has been associated with cancer progression, metastasis, and drug resistance. Their essential function in immune homeostasis has prompted an interest in their role as modulators of antit
Autor:
Jill C. Milne, Angela Tornblom, Jean Bemis, Jeremy S. Disch, George P. Vlasuk, Peter Elliot, Amy V. Lynch, Robert B. Perni, Pui Yee Ng, James L. Ellis, Akanksha Gupta, Christopher Oalmann, Joseph J. Nunes, J. Joshua Smith, Kristina Kriksciukaite, Michael R. Jirousek, Marie Yeager, Vipin Suri, David P. Carney, Meghan Duncan, Jeffrey Song, Siva Lavu, Thomas V. Riera, Chi B. Vu
Publikováno v:
Letters in Drug Design & Discovery. 10:793-797
Autor:
Taylor Lg Doyle, Jeremy S. Disch, George P. Vlasuk, Christine Loh, Ana P. Gomes, Basil P. Hubbard, Jun Li, James L. Ellis, Sean M. Armour, David A. Sinclair, Quinn Lu
Publikováno v:
Cell Cycle. 12:2233-2240
SIRT1 is an NAD (+) -dependent deacetylase that counteracts multiple disease states associated with aging and may underlie some of the health benefits of calorie restriction. Understanding how SIRT1 is regulated in vivo could therefore lead to new st
Autor:
Ghotas Evindar, Frank T. Coppo, George P. Vlasuk, Eli Schuman, Charles A. Blum, Cheney Mao, Lei Jin, Han Dai, Robert B. Perni, Jianghe Deng, Svetlana L. Belyanskaya, Todd L. Graybill, John W. Cuozzo, Leah Aquilani, Jeremy S. Disch, Cynthia H. Chiu, Siva Lavu, Kenneth E Lind
Publikováno v:
Journal of Medicinal Chemistry. 56:3666-3679
The sirtuins SIRT1, SIRT2, and SIRT3 are NAD(+) dependent deacetylases that are considered potential targets for metabolic, inflammatory, oncologic, and neurodegenerative disorders. Encoded library technology (ELT) was used to affinity screen a 1.2 m
Autor:
David P. Carney, Amy V. Lynch, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Roger Xie, Michael R. Jirousek, Jill C. Milne, J. Joshua Smith, Lei Jin, Andre Iffland, Joseph J. Nunes, Jean Bemis, Siva Lavu, Chi B. Vu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2350-2353
SIRT1 is an NAD+-dependent protein deacetylase that appears to produce beneficial effects on metabolic parameters such as glucose and insulin homeostasis. Activation of SIRT1 by resveratrol (1) has been shown to modulate insulin resistance, increase
Autor:
Philip D. Lambert, David J. Gagne, Joseph J. Nunes, Jerrold M. Olefsky, Jean Bemis, Chi B. Vu, Jill C. Milne, Amy V. Lynch, J. Joshua Smith, David P. Carney, Michael R. Jirousek, Robert B. Perni, Pui Yee Ng, Jeremy S. Disch, Simon Schenk, Siva Lavu
Publikováno v:
Journal of Medicinal Chemistry. 52:1275-1283
A series of imidazo[1,2-b]thiazole derivatives is shown to activate the NAD(+)-dependent deacetylase SIRT1, a potential new therapeutic target to treat various metabolic disorders. This series of compounds was derived from a high throughput screening