Zobrazeno 1 - 10
of 57
pro vyhledávání: '"Sergio C Chai"'
Autor:
Daniel C. Scott, Suresh Dharuman, Elizabeth Griffith, Sergio C. Chai, Jarrid Ronnebaum, Moeko T. King, Rajendra Tangallapally, Chan Lee, Clifford T. Gee, Lei Yang, Yong Li, Victoria C. Loudon, Ha Won Lee, Jason Ochoada, Darcie J. Miller, Thilina Jayasinghe, Joao A. Paulo, Stephen J. Elledge, J. Wade Harper, Taosheng Chen, Richard E. Lee, Brenda A. Schulman
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-19 (2024)
Abstract PROTAC® (proteolysis-targeting chimera) molecules induce proximity between an E3 ligase and protein-of-interest (POI) to target the POI for ubiquitin-mediated degradation. Cooperative E3-PROTAC-POI complexes have potential to achieve neo-su
Externí odkaz:
https://doaj.org/article/6c50c513c918469eaf4c94f0f0e0d58b
Autor:
Efren Garcia-Maldonado, Andrew D. Huber, Sergio C. Chai, Stanley Nithianantham, Yongtao Li, Jing Wu, Shyaron Poudel, Darcie J. Miller, Jayaraman Seetharaman, Taosheng Chen
Publikováno v:
Nature Communications, Vol 15, Iss 1, Pp 1-14 (2024)
Abstract Nuclear receptors are ligand-activated transcription factors that can often be useful drug targets. Unfortunately, ligand promiscuity leads to two-thirds of receptors remaining clinically untargeted. PXR is a nuclear receptor that can be act
Externí odkaz:
https://doaj.org/article/c30e189d2e734c8aad1bc9b3e758e589
Publikováno v:
Journal of Medicinal Chemistry. 65:16829-16859
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5259f762799a1cbafd06255d73b46939
https://doi.org/10.1021/acs.jmedchem.2c01640
https://doi.org/10.1021/acs.jmedchem.2c01640
Autor:
Wenwei Lin, Yue-Ming Wang, Sergio C. Chai, Lili Lv, Jie Zheng, Jing Wu, Qijun Zhang, Yong-Dong Wang, Patrick R. Griffin, Taosheng Chen
Publikováno v:
Nature Communications, Vol 8, Iss 1, Pp 1-14 (2017)
The xenobiotic-activated human pregnane X receptor (hPXR) regulates drug metabolism. Here the authors develop hPXR modulators, which are of potential therapeutic interest and functionally and structurally characterize the antagonist SPA70 and the str
Externí odkaz:
https://doaj.org/article/1c0bb2294d6a40f4b4d18bb1cc20c813
Autor:
Philip M. Potter, Anang A. Shelat, Stephen W. White, R. Kiplin Guy, Daniel Savic, Taosheng Chen, Martine F. Roussel, Marie Morfouace, Richard E. Lee, Jun Yang, Vincent A. Boyd, Nagakumar Bharatham, Brandon M. Young, Jeanine E. Price, Jonathan A. Low, Kevin W. Freeman, Rachelle R. Olsen, William R. Shadrick, Zhenmei Li, Geoffrey Neale, Sourav Das, M. Brett Waddell, Michele Connelly, Sergio C. Chai, Barbara Jonchere, Nancy E. Martinez, Lyudmila Tsurkan, Mi-Kyung Yun, Liying Chi, P. Jake Slavish
Inhibition of members of the bromodomain and extraterminal (BET) family of proteins has proven a valid strategy for cancer chemotherapy. All BET identified to date contain two bromodomains (BD; BD1 and BD2) that are necessary for recognition of acety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4b5d71e4e32bd0d5208d4d9130ecd2d2
https://doi.org/10.1158/0008-5472.c.6511882.v1
https://doi.org/10.1158/0008-5472.c.6511882.v1
Autor:
Mladen Koravovic, Anand Mayasundari, Gordana Tasic, Fatemeh Keramatnia, Timothy R. Stachowski, Huarui Cui, Sergio C. Chai, Barbara Jonchere, Lei Yang, Yong Li, Xiang Fu, Ryan Hiltenbrand, Leena Paul, Vibhor Mishra, Jeffery M. Klco, Martine F. Roussel, William CK. Pomerantz, Marcus Fischer, Zoran Rankovic, Vladimir Savic
Publikováno v:
European Journal of Medicinal Chemistry
An X-ray structure of a CLICK chemistry-based BET PROTAC bound to BRD2(BD2) inspired synthesis of JQ1 derived heterocyclic amides. This effort led to the discovery of potent BET inhibitors displaying overall improved profiles when compared to JQ1 and
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5648b26b4c7d2361e3341b7c58a3cd9
https://farfar.pharmacy.bg.ac.rs/handle/123456789/4513
https://farfar.pharmacy.bg.ac.rs/handle/123456789/4513
Autor:
Richard E. Lee, Jake Slavish, Brandon Young, Lei Yang, Sergio C. Chai, Marcus Fischer, Taosheng Chen, Zhenmei Li, Stephen W. White, Stanley Nithianantham, Jaeki Min, Gisele Nishiguchi, Seung Wook Yang, Patrick Ryan Potts, Marisa Actis, Shalandus H. Garrett, Jamie Jarusiewicz, Sourav Das, Martine F. Roussel, Barbara Jonchere, Anand Mayasundari, Yong Li, Mi-Kyung Yun, Xiang Fu, Fatemeh Keramatnia, Anang A. Shelat, Zoran Rankovic
Publikováno v:
Angew Chem Int Ed Engl
Targeting cereblon (CRBN) is currently one of the most frequently reported proteolysis-targeting chimera (PROTAC) approaches, owing to favorable drug-like properties of CRBN ligands, immunomodulatory imide drugs (IMiDs). However, IMiDs are known to b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1ffb235e447bf310701a7f1aa84dd193
https://doi.org/10.1002/anie.202108848
https://doi.org/10.1002/anie.202108848
Autor:
Daniel C. Scott, Moeko T. King, Kheewoong Baek, Clifford T. Gee, Ravi Kalathur, Jerry Li, Nicholas Purser, Amanda Nourse, Sergio C. Chai, Sivaraja Vaithiyalingam, Taosheng Chen, Richard E. Lee, Stephen J. Elledge, Gary Kleiger, Brenda A. Schulman
Publikováno v:
Molecular Cell. 83:770-786.e9
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::05d3991b8d1161aca857cde9194d1e4f
https://doi.org/10.1016/j.molcel.2023.01.019
https://doi.org/10.1016/j.molcel.2023.01.019
Bromodomain-Selective BET Inhibitors Are Potent Antitumor Agents against MYC-Driven Pediatric Cancer
Autor:
Barbara Jonchere, Jonathan Low, Michele Connelly, Liying Chi, Sergio C. Chai, R. Kiplin Guy, Kevin W. Freeman, Brandon Young, Jeanine E. Price, Mi-Kyung Yun, Marie Morfouace, Anang A. Shelat, Geoffrey Neale, Rachelle R. Olsen, Nagakumar Bharatham, Daniel Savic, Stephen W. White, P. Jake Slavish, Vincent A. Boyd, Lyudmila Tsurkan, Jun J. Yang, Nancy E. Martinez, Zhenmei Li, Martine F. Roussel, Philip M. Potter, M. Brett Waddell, William R. Shadrick, Richard E. Lee, Taosheng Chen, Sourav Das
Publikováno v:
Cancer Res
Inhibition of members of the bromodomain and extraterminal (BET) family of proteins has proven a valid strategy for cancer chemotherapy. All BET identified to date contain two bromodomains (BD; BD1 and BD2) that are necessary for recognition of acety
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86d687ae06b408a0a8a364651477a03f
https://doi.org/10.1158/0008-5472.can-19-3934
https://doi.org/10.1158/0008-5472.can-19-3934
Autor:
Monicah N Bwayi, Efren Garcia-Maldonado, Sergio C Chai, Boer Xie, Shirish Chodankar, Andrew D Huber, Jing Wu, Kavya Annu, William C Wright, Hyeong-Min Lee, Jayaraman Seetharaman, Jingheng Wang, Cameron D Buchman, Junmin Peng, Taosheng Chen
Publikováno v:
Nucleic acids research. 50(6)
The 48 human nuclear receptors (NRs) form a superfamily of transcription factors that regulate major physiological and pathological processes. Emerging evidence suggests that NR crosstalk can fundamentally change our understanding of NR biology, but
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::025ac0ee2762b893477d7d6fd92904f2
https://pubmed.ncbi.nlm.nih.gov/35212371
https://pubmed.ncbi.nlm.nih.gov/35212371